The following articles (labelled with PubMed ID or TBD) are for your review| PMID | Article Title | Published | Deposition |
|---|
| 34110834 |
Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer. |
08-JUL-2021 |
20-APR-2024 |
| 36793423 |
Macrocyclic Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonists. |
09-FEB-2023 |
18-APR-2024 |
| US20230405002 |
COMBINATIONS OF DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITORS AND ACETYL-COA CARBOXYLASE INHIBITOR |
21-DEC-2023 |
12-FEB-2024 |
| US20230321042 |
COMBINATION THERAPY |
12-OCT-2023 |
22-NOV-2023 |
| US11780853 |
Substituted N-pyrimidin-4-yl-3-aminopyrrolo[3,4-C]pyrazoles as protein kinase C inhibitors |
10-OCT-2023 |
17-NOV-2023 |
| US20230280220 |
Benzimidazole Derivative Compounds and Uses Thereof |
07-SEP-2023 |
17-OCT-2023 |
| US11718603 |
CDK2 inhibitors |
08-AUG-2023 |
15-SEP-2023 |
| US11702424 |
Bicyclic-fused heteroaryl or aryl compounds |
18-JUL-2023 |
18-AUG-2023 |
| US11684616 |
Azalactam compounds as HPK1 inhibitors |
27-JUN-2023 |
31-JUL-2023 |
| US11661419 |
Benzimidazole derivative compounds and uses thereof |
30-MAY-2023 |
02-JUL-2023 |
| US11655252 |
Aminopyrimidinyl derivatives |
23-MAY-2023 |
26-JUN-2023 |
| 35647711 |
A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor. |
23-JUN-2022 |
25-JUN-2023 |
| 36322383 |
Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis. |
24-NOV-2022 |
18-JUN-2023 |
| US11634410 |
Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors |
25-APR-2023 |
02-JUN-2023 |
| US11634425 |
Pharmaceutical compounds |
25-APR-2023 |
02-JUN-2023 |
| US11559538 |
Substituted 1,2-oxaborolan-2-ols as PDE4 inhibitors |
24-JAN-2023 |
19-MAR-2023 |
| 34967602 |
Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1. |
13-JAN-2022 |
07-MAR-2023 |
| 35059124 |
Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators. |
13-JAN-2022 |
05-MAR-2023 |
| WO2022208262 |
ETHER-LINKED ANTIVIRAL COMPOUNDS |
06-OCT-2022 |
31-JAN-2023 |
| US11492346 |
Benzisoxazole sulfonamide derivatives |
08-NOV-2022 |
20-JAN-2023 |
| US11472809 |
Pyrazolo[1,5-a]pyrazin-4-yl derivatives |
18-OCT-2022 |
24-DEC-2022 |
| US11472805 |
Tricyclic compounds and their use as phosphodiesterase inhibitors |
18-OCT-2022 |
24-DEC-2022 |
| US11471458 |
Diacylglycerol acyl transferase 2 inhibitor |
18-OCT-2022 |
23-DEC-2022 |
| WO2022112919 |
(AZA)BENZOTHIAZOLYL SUBSTITUTED PYRAZOLE COMPOUNDS |
02-JUN-2022 |
14-DEC-2022 |
| US11396512 |
CDK2/4/6 inhibitors |
26-JUL-2022 |
17-OCT-2022 |
| US11351149 |
Nitrile-containing antiviral compounds |
07-JUN-2022 |
10-SEP-2022 |
| 34000509 |
Toward the assembly and characterization of an encoded library hit confirmation platform: Bead-Assisted Ligand Isolation Mass Spectrometry (BALI-MS). |
01-JUL-2021 |
23-AUG-2022 |
| 34400299 |
Discovery and evaluation of non-basic small molecule modulators of the atypical chemokine receptor CXCR7. |
15-OCT-2021 |
19-AUG-2022 |
| US11312713 |
Imidazo[4,5-C]quinoline derivatives as LRRK2 inhibitors |
26-APR-2022 |
06-AUG-2022 |
| US11254668 |
Pyrazolo[1,5-A]pyrazin-4-yl and related derivatives |
22-FEB-2022 |
19-JUN-2022 |
| WO2022013684 |
ANTIVIRAL HETEROARYL KETONE DERIVATIVES |
20-JAN-2022 |
09-JUN-2022 |
| US11220494 |
Cyclin dependent kinase inhibitors |
11-JAN-2022 |
14-MAY-2022 |
| US11220518 |
Substituted n-pyrimidin-4-yl-3-amino-pyrrolo[3,4-c]pyrazoles as protein kinase C inhibitors |
11-JAN-2022 |
14-MAY-2022 |
| US11203594 |
Anti-proliferative agents for treating PAH |
21-DEC-2021 |
29-APR-2022 |
| US11197867 |
Aminopyrimidinyl compounds |
14-DEC-2021 |
24-APR-2022 |
| 33356244 |
PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease. |
14-JAN-2021 |
30-MAR-2022 |
| 27275946 |
Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects. |
14-JUL-2016 |
27-MAR-2022 |
| 33356246 |
Structure-Based Drug Design and Synthesis of PI3K?-Selective Inhibitor (PF-06843195). |
14-JAN-2021 |
26-MAR-2022 |
| 33054210 |
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19. |
12-NOV-2020 |
25-MAR-2022 |
| 27766865 |
The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain. |
23-NOV-2016 |
23-MAR-2022 |
| 29570292 |
2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety. |
12-APR-2018 |
23-MAR-2022 |
| 32787094 |
Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases. |
25-NOV-2020 |
22-MAR-2022 |
| 32910646 |
Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose. |
25-NOV-2020 |
22-MAR-2022 |
| 30258534 |
Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
13-SEP-2018 |
22-MAR-2022 |
| 32809824 |
Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting. |
08-OCT-2020 |
21-MAR-2022 |
| US11161844 |
Cyclic substituted imidazo[4,5-c]quinoline derivatives |
02-NOV-2021 |
20-MAR-2022 |
| US11142525 |
Azalactam compounds as HPK1 inhibitors |
12-OCT-2021 |
04-MAR-2022 |
| US11111242 |
Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides |
07-SEP-2021 |
21-FEB-2022 |
| WO2021205290 |
Compounds and method of treating covid-19 |
14-OCT-2021 |
13-JAN-2022 |
| WO2021250648 |
Nitrile-containing antiviral compounds |
16-DEC-2021 |
13-JAN-2022 |
| WO2021205298 |
Compounds and methods for the treatment of covid-19 |
14-OCT-2021 |
13-JAN-2022 |
| US11065249 |
Diacylglycerol acyl transferase 2 inhibitor |
20-JUL-2021 |
19-DEC-2021 |
| US11034678 |
Diacylglycerol acyl transferase 2 inhibitors |
15-JUN-2021 |
05-DEC-2021 |
| US11014909 |
Heteroaromatic compounds and their use as dopamine D1 ligands |
25-MAY-2021 |
22-NOV-2021 |
| US11014911 |
CDK2 inhibitors |
25-MAY-2021 |
22-NOV-2021 |
| TBD |
An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19 |
02-XXX-2021 |
05-NOV-2021 |
| US10988463 |
Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors |
27-APR-2021 |
01-NOV-2021 |
| US10980815 |
Aminopyrimidinyl compounds |
20-APR-2021 |
26-OCT-2021 |
| US10968242 |
Cyclopentane-based modulators of STING (stimulator of interferon genes) |
06-APR-2021 |
09-OCT-2021 |
| US10966980 |
Pyrrolo[2,3-d]pyrimidine derivatives |
06-APR-2021 |
09-OCT-2021 |
| US10945994 |
Combinations comprising a pyrrolidine-2,5-dione IDO1 inhibitor and an anti-body |
16-MAR-2021 |
26-SEP-2021 |
| US10906888 |
Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme |
02-FEB-2021 |
22-AUG-2021 |
| 32462865 |
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H |
09-JUL-2020 |
14-AUG-2021 |
| 32253095 |
Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1. |
15-MAY-2020 |
13-AUG-2021 |
| 32551020 |
Discovery of Diphenylacetamides as CXCR7 Inhibitors with Novel ?-Arrestin Antagonist Activity. |
11-JUN-2020 |
13-AUG-2021 |
| 32550998 |
Characterization of Specific |
11-JUN-2020 |
13-AUG-2021 |
| 32097005 |
Effective Application of Metabolite Profiling in Drug Design and Discovery. |
25-JUN-2020 |
12-AUG-2021 |
| 31497963 |
Designing around Structural Alerts in Drug Discovery. |
25-JUN-2020 |
12-AUG-2021 |
| US10858373 |
Heterocyclic spiro compounds as MAGL inhibitors |
08-DEC-2020 |
11-JUL-2021 |
| US10822341 |
Pyrazolo[1,5-a]pyrazin-4-yl derivatives |
03-NOV-2020 |
21-JUN-2021 |
| US10815213 |
Bruton's tyrosine kinase inhibitors |
27-OCT-2020 |
13-JUN-2021 |
| US10813942 |
Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of ASGPR |
27-OCT-2020 |
13-JUN-2021 |
| US10800783 |
CDK2/4/6 inhibitors |
13-OCT-2020 |
01-JUN-2021 |
| US10793579 |
Bicyclic-fused heteroaryl or aryl compounds |
06-OCT-2020 |
14-MAY-2021 |
| US10787438 |
Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors |
29-SEP-2020 |
09-MAY-2021 |
| US10766884 |
Cyclin dependent kinase inhibitors |
08-SEP-2020 |
26-APR-2021 |
| US10738063 |
6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds |
11-AUG-2020 |
04-APR-2021 |
| US10709709 |
Substituted carbonucleoside derivatives useful as anticancer agents |
14-JUL-2020 |
14-MAR-2021 |
| US10676465 |
GLP-1 receptor agonists and uses thereof |
09-JUN-2020 |
11-MAR-2021 |
| 27381086 |
Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines. |
15-AUG-2016 |
27-FEB-2021 |
| 30113844 |
Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841). |
11-OCT-2018 |
26-FEB-2021 |
| 31415173 |
Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase. |
12-SEP-2019 |
23-FEB-2021 |
| 30655951 |
Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. |
10-JAN-2019 |
23-FEB-2021 |
| US10669279 |
Imidazopyridazine compounds |
02-JUN-2020 |
21-FEB-2021 |
| 30964988 |
Design and Identification of a Novel, Functionally Subtype Selective GABA |
27-JUN-2019 |
20-FEB-2021 |
| 30996784 |
Discovering New Casein Kinase 1d Inhibitors with an Innovative Molecular Dynamics Enabled Virtual Screening Workflow. |
11-APR-2019 |
20-FEB-2021 |
| 30482620 |
Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9. |
15-DEC-2018 |
19-FEB-2021 |
| 30538065 |
The discovery and optimization of benzimidazoles as selective Na |
01-JAN-2019 |
19-FEB-2021 |
| 29672039 |
Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors. |
10-JAN-2019 |
18-FEB-2021 |
| 31223452 |
Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres. |
13-JUN-2019 |
17-FEB-2021 |
| WO2006061714 |
Anticoronaviral compounds and compositions, their pharmaceutical uses and materials for their synthesis |
15-JUN-2006 |
31-JAN-2021 |
| US10570121 |
Substituted dihydroisoquinolinone compounds |
25-FEB-2020 |
30-NOV-2020 |
| US10538523 |
4-(biphen-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I) as GABA receptor modulators for use in the treatment of epilepsy and pain |
21-JAN-2020 |
09-NOV-2020 |
| US10544095 |
3-indol substituted derivatives, pharmaceutical compositions and methods for use |
28-JAN-2020 |
01-NOV-2020 |
| WO2005113580 |
Anticoronviral compounds and compositions, their pharmaceutical uses and materials for their synthesis |
01-DEC-2005 |
17-OCT-2020 |
| 32935104 |
Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19. |
13-SEP-2020 |
21-SEP-2020 |
| US10463675 |
Aminopyrimidinyl compounds |
05-NOV-2019 |
08-SEP-2020 |
| 28139931 |
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. |
09-MAR-2017 |
05-SEP-2020 |
| 25060923 |
Recent progress in sodium channel modulators for pain. |
15-AUG-2014 |
03-SEP-2020 |
| 23597790 |
Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: optimization studies and demonstration of in vivo efficacy. |
01-JUN-2013 |
01-SEP-2020 |
| 23582272 |
Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors. |
01-JUN-2013 |
01-SEP-2020 |
| 23566517 |
Novel quinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV. |
15-MAY-2013 |
31-AUG-2020 |
| US10450297 |
Sulfonyl amide derivatives for the treatment of abnormal cell growth |
22-OCT-2019 |
31-AUG-2020 |
| 23075044 |
Small molecules that target protein misfolding. |
27-DEC-2012 |
30-AUG-2020 |
| 23116892 |
Structural modifications of a 3-methoxy-2-aminopyridine compound to reduce potential for mutagenicity and time-dependent drug-drug interaction. |
15-DEC-2012 |
30-AUG-2020 |
| 22257165 |
Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections. |
23-FEB-2012 |
29-AUG-2020 |
| 21269825 |
Diamide amino-imidazoles: a novel series of ?-secretase inhibitors for the treatment of Alzheimer's disease. |
01-MAY-2011 |
29-AUG-2020 |
| 21269827 |
Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as ?-secretase inhibitors: discovery of PF-3084014. |
01-MAY-2011 |
29-AUG-2020 |
| 21995460 |
Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as ?-secretase inhibitors. |
24-NOV-2011 |
29-AUG-2020 |
| 20660667 |
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
XX-OCT-2010 |
29-AUG-2020 |
| 21446745 |
Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors. |
12-MAY-2011 |
29-AUG-2020 |
| 22420884 |
Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active ?-secretase inhibitor. |
12-APR-2012 |
29-AUG-2020 |
| 21612924 |
Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone. |
15-JUN-2011 |
29-AUG-2020 |
| 22401863 |
Structure based design of an in vivo active hydroxamic acid inhibitor of P. aeruginosa LpxC. |
01-APR-2012 |
29-AUG-2020 |
| 19873974 |
Azaindole hydroxamic acids are potent HIV-1 integrase inhibitors. |
26-NOV-2009 |
27-AUG-2020 |
| 19908836 |
Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone. |
14-JAN-2010 |
27-AUG-2020 |
| 18929486 |
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone. |
01-DEC-2008 |
26-AUG-2020 |
| 17764937 |
Thiazole-diamides as potent gamma-secretase inhibitors. |
15-OCT-2007 |
24-AUG-2020 |
| 11123995 |
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors. |
14-DEC-2000 |
22-AUG-2020 |
| 12086495 |
Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors. |
04-JUL-2002 |
22-AUG-2020 |
| 8568798 |
Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret. |
05-JAN-1996 |
21-AUG-2020 |
| 9632360 |
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase. |
18-JUN-1998 |
21-AUG-2020 |
| 9685230 |
Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene. |
30-JUL-1998 |
21-AUG-2020 |
| 7636876 |
(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses. |
04-AUG-1995 |
21-AUG-2020 |
| 30431269 |
Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. |
27-DEC-2018 |
18-AUG-2020 |
| 30052440 |
Lead-like Drugs: A Perspective. |
13-DEC-2018 |
18-AUG-2020 |
| 30423248 |
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors. |
13-DEC-2018 |
18-AUG-2020 |
| 29348070 |
Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors. |
10-FEB-2018 |
18-AUG-2020 |
| US10426135 |
Methyl- and trifluromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof |
01-OCT-2019 |
17-AUG-2020 |
| US10428104 |
Substituted nucleoside derivatives useful as anticancer agents |
01-OCT-2019 |
17-AUG-2020 |
| 29980357 |
Inducing protein-protein interactions with molecular glues. |
15-AUG-2018 |
17-AUG-2020 |
| 29716781 |
Harnessing biosynthesis and quantitative NMR for late stage functionalization of lead molecules: Application to the M1 positive allosteric modulator (PAM) program. |
15-JUN-2018 |
17-AUG-2020 |
| 30036059 |
Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK). |
23-AUG-2018 |
17-AUG-2020 |
| 29944371 |
Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain. |
09-AUG-2018 |
16-AUG-2020 |
| 30258528 |
Precedence and Promise of Covalent Inhibitors of EGFR and KRAS for Patients with Non-Small-Cell Lung Cancer. |
13-SEP-2018 |
16-AUG-2020 |
| 29029933 |
Highly potent and selective Na |
01-NOV-2017 |
15-AUG-2020 |
| 29613789 |
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation. |
24-MAY-2018 |
15-AUG-2020 |
| 29795756 |
Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1). |
10-MAY-2018 |
14-AUG-2020 |
| 29456800 |
Discovery and in Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors. |
08-FEB-2018 |
22-JUL-2020 |
| 29456790 |
Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189. |
08-FEB-2018 |
20-JUL-2020 |
| US10385036 |
Sulfonamide-substituted indole modulators of RORC2 and methods of use thereof |
20-AUG-2019 |
13-JUL-2020 |
| US10376531 |
Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of ASGPR |
13-AUG-2019 |
06-JUL-2020 |
| US10329302 |
Bicyclic-fused heteroaryl or aryl compounds |
25-JUN-2019 |
31-MAY-2020 |
| 29878763 |
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents. |
12-JUL-2018 |
18-MAY-2020 |
| US10323042 |
6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds |
18-JUN-2019 |
11-MAY-2020 |
| 29718668 |
Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1. |
24-MAY-2018 |
03-MAY-2020 |
| 29589935 |
Lipophilic Efficiency as an Important Metric in Drug Design. |
09-AUG-2018 |
26-APR-2020 |
| US10308615 |
Heterocyclic compounds as inhibitors of Vanin-1 enzyme |
04-JUN-2019 |
15-APR-2020 |
| US10266513 |
Bruton's tyrosine kinase inhibitors |
23-APR-2019 |
07-FEB-2020 |
| US9920054 |
Methyl- and trifluoromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof |
20-MAR-2018 |
04-FEB-2020 |
| 29627981 |
Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis. |
26-APR-2018 |
03-FEB-2020 |
| 29601185 |
Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors. |
26-APR-2018 |
01-FEB-2020 |
| US10227346 |
Methyl- and trifluoromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use therof |
12-MAR-2019 |
27-DEC-2019 |
| US10233188 |
CDK2/4/6 inhibitors |
19-MAR-2019 |
27-DEC-2019 |
| 28696695 |
Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators. |
27-JUL-2017 |
21-DEC-2019 |
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Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation. |
12-APR-2018 |
15-DEC-2019 |
| 28626530 |
Discovery of a Series of Indazole TRPA1 Antagonists. |
08-JUN-2017 |
10-DEC-2019 |
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Heteroaromatic compounds and their use as dopamine D1 ligands |
16-JAN-2018 |
10-DEC-2019 |
| 28610977 |
Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV. |
01-AUG-2017 |
09-DEC-2019 |
| 29148769 |
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase. |
14-DEC-2017 |
26-NOV-2019 |
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Discovery of Potent and Orally Bioavailable Macrocyclic Peptide-Peptoid Hybrid CXCR7 Modulators. |
14-DEC-2017 |
23-NOV-2019 |
| US9856263 |
Heteroaromatic compounds and their use as dopamine D1 ligands |
02-JAN-2018 |
21-NOV-2019 |
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Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay. |
XX-XXX-2017 |
19-NOV-2019 |
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Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists. |
08-FEB-2018 |
02-NOV-2019 |
| 29293004 |
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate. |
08-FEB-2018 |
02-NOV-2019 |
| 29466005 |
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK). |
22-MAR-2018 |
24-OCT-2019 |
| 29298069 |
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. |
08-FEB-2018 |
19-OCT-2019 |
| US9815832 |
Azabenzimidazole compounds |
14-NOV-2017 |
13-OCT-2019 |
| 28853885 |
Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK). |
28-SEP-2017 |
09-OCT-2019 |
| 28817277 |
Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates. |
28-SEP-2017 |
07-OCT-2019 |
| 28598634 |
Design and Synthesis of?- and?-Lactam M |
10-AUG-2017 |
05-OCT-2019 |
| US9802945 |
Imidazopyridazine derivatives as modulators of the GABAA receptor activity |
31-OCT-2017 |
01-OCT-2019 |
| 28574706 |
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor. |
13-JUL-2017 |
26-SEP-2019 |
| 28498658 |
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design. |
13-JUL-2017 |
22-SEP-2019 |
| US10208019 |
GLP-1 receptor agonists and uses thereof |
19-FEB-2019 |
21-SEP-2019 |
| US9789110 |
Diacylglycerol acyltransferase 2 inhibitors |
17-OCT-2017 |
09-SEP-2019 |
| 28421763 |
Synthetic Approaches to the New Drugs Approved During 2015. |
10-AUG-2017 |
31-AUG-2019 |
| 28375629 |
Structure-Based Design of Highly Selective Inhibitors of the CREB Binding Protein Bromodomain. |
13-JUL-2017 |
29-AUG-2019 |
| 24799086 |
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
XX-SEP-2014 |
19-AUG-2019 |
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Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype-Distinct Screening Hits. |
23-MAR-2017 |
13-AUG-2019 |
| 28257199 |
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA). |
13-APR-2017 |
08-AUG-2019 |
| US9771379 |
N-(2-(2-amino-6-substituted-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]OXAZIN-8a(8H)-yl)-thiazol-4-yl) amides |
26-SEP-2017 |
06-AUG-2019 |
| US9758538 |
Pyrimidine derivatives |
12-SEP-2017 |
22-JUL-2019 |
| US9744173 |
2-amino 6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides |
29-AUG-2017 |
05-JUL-2019 |
| US9745317 |
Heterocyclic compounds and their use as dopamine D1 ligands |
29-AUG-2017 |
05-JUL-2019 |
| US9738626 |
Antagonists of prostaglandin EP3 receptor |
22-AUG-2017 |
01-JUL-2019 |
| 27983835 |
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin. |
26-JAN-2017 |
20-JUN-2019 |
| US9663526 |
Aminopyrimidinyl compounds |
30-MAY-2017 |
04-JUN-2019 |
| US10188653 |
Diacylglycerol acyltransferase 2 inhibitors |
29-JAN-2019 |
25-MAY-2019 |
| US10174007 |
Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors |
08-JAN-2019 |
15-MAY-2019 |
| US10174000 |
Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators |
08-JAN-2019 |
15-MAY-2019 |
| US9617258 |
Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides |
11-APR-2017 |
08-MAY-2019 |
| US9605007 |
2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides |
28-MAR-2017 |
24-APR-2019 |
| US10144738 |
Pyrazolo[1,5-A]PYRAZIN-4-YL derivatives |
04-DEC-2018 |
30-MAR-2019 |
| US10144738 |
Pyrazolo[1,5-A]PYRAZIN-4-YL derivatives |
04-DEC-2018 |
30-MAR-2019 |
| US9598421 |
Imidazopyridazine compounds |
21-MAR-2017 |
29-MAR-2019 |
| US9593097 |
Axl inhibitors |
14-MAR-2017 |
15-MAR-2019 |
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Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase. |
XX-FEB-1991 |
29-JAN-2019 |
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Nicotinamide ethers: novel inhibitors of calcium-independent phosphodiesterase and [3H]rolipram binding. |
XX-JAN-1991 |
27-JAN-2019 |
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Calcium-independent phosphodiesterase inhibitors as putative antidepressants: [3-(bicycloalkyloxy)-4-methoxyphenyl]-2-imidazolidinones. |
XX-JAN-1991 |
27-JAN-2019 |
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Heteroaromatic compounds and their use as dopamine D1 ligands |
09-OCT-2018 |
22-JAN-2019 |
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Synthesis, in vitro binding profile, and central nervous system penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole. |
XX-NOV-1990 |
15-JAN-2019 |
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Substituted pyrrolo[3,4-c]pyrazoles as PKC kinase inhibitors |
13-DEC-2016 |
14-JAN-2019 |
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Pyrazolopyridines and pyrazolopyrimidines |
13-DEC-2016 |
14-JAN-2019 |
| US10077272 |
Heteroaromatic compounds and their use as dopamine D1 ligands |
18-SEP-2018 |
11-JAN-2019 |
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Imidazopyridazine compounds |
18-SEP-2018 |
11-JAN-2019 |
| 2894465 |
2,4-Diamino-6,7-dimethoxyquinazolines. 4. 2-[4-(substituted oxyethoxy) piperidino] derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. |
XX-MAR-1988 |
01-JAN-2019 |
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2,4-Diamino-6,7-dimethoxyquinoline derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. |
XX-MAY-1988 |
01-JAN-2019 |
| 2896246 |
1,3-Diamino-6,7-dimethoxyisoquinoline derivatives as potential alpha 1-adrenoceptor antagonists. |
XX-MAY-1988 |
01-JAN-2019 |
| US10022376 |
Pyrazolopyridines and pyrazolopyrimidines |
17-JUL-2018 |
31-DEC-2018 |
| 2888896 |
2,4-Diamino-6,7-dimethoxyquinazolines. 3. 2-(4-Heterocyclylpiperazin-1-yl) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents. |
XX-OCT-1987 |
23-DEC-2018 |
| US10071992 |
Diacylglycerol acyl transferase 2 inhibitors |
11-SEP-2018 |
21-DEC-2018 |
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Discovery of a series of (4,5-dihydroimidazol-2-yl)-biphenylamine 5-HT7 agonists. |
20-JAN-2003 |
16-NOV-2018 |
| 9873435 |
Development of new chromanol antagonists of leukotriene D4. |
21-JUL-1998 |
08-OCT-2018 |
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trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor. |
21-JUL-1998 |
07-OCT-2018 |
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Substituted 1,7-naphthyridines as dopamine D1 ligands |
10-JAN-2017 |
16-AUG-2018 |
| 27641472 |
Investigation of the structure activity relationship of flufenamic acid derivatives at the human TRESK channel K |
15-OCT-2016 |
14-JUL-2018 |
| 27727125 |
Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators. |
01-NOV-2016 |
09-JUL-2018 |
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Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors. |
22-SEP-2016 |
04-JUL-2018 |
| 27490827 |
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy. |
08-SEP-2016 |
26-JUN-2018 |
| US9670201 |
Methyl- and trifluoromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use thereof |
06-JUN-2017 |
19-MAY-2018 |
| 27115555 |
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. |
26-MAY-2016 |
25-SEP-2017 |
| 27297999 |
Systematic N-methylation of oxytocin: Impact on pharmacology and intramolecular hydrogen bonding network. |
19-JUL-2016 |
20-SEP-2017 |
| 27107947 |
Optimization of amide-based EP3 receptor antagonists. |
02-MAY-2016 |
21-AUG-2017 |
| 27043173 |
Discovery of small-molecule nonpeptide antagonists of nociceptin/orphanin FQ receptor: The studies of design, synthesis, and structure-activity relationships for (4-arylpiperidine substituted-methyl)-[bicyclic (hetero)cycloalkanobenzene] derivatives. |
11-APR-2016 |
05-AUG-2017 |
| 26968253 |
Recent progress on third generation covalent EGFR inhibitors. |
26-MAR-2016 |
27-JUL-2017 |
| US9403846 |
Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
02-AUG-2016 |
24-JUL-2017 |
| 26756222 |
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
11-MAR-2016 |
23-JUL-2017 |
| US9394285 |
Indole and indazole compounds that activate AMPK |
19-JUL-2016 |
17-JUL-2017 |
| 27020685 |
Synthetic approaches to the 2014 new drugs. |
15-APR-2016 |
02-JUL-2017 |
| 26734723 |
Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family. |
11-FEB-2016 |
23-JUN-2017 |
| 26653735 |
Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis. |
14-JAN-2016 |
06-JUN-2017 |
| 26631313 |
Design and optimization of selective azaindole amide M1 positive allosteric modulators. |
08-JAN-2016 |
26-MAY-2017 |
| 26617966 |
Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. |
30-NOV-2015 |
25-MAY-2017 |
| US9328096 |
Tropomyosin-related kinase inhibitors |
03-MAY-2016 |
15-MAY-2017 |
| US9315520 |
2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl-1,3-thiazol-4-yl amides |
19-APR-2016 |
01-MAY-2017 |
| US9296745 |
Diacylglycerol acyltransferase 2 inhibitors |
29-MAR-2016 |
06-MAR-2017 |
| US9278953 |
Antagonists of prostaglandin EP3 receptor |
08-MAR-2016 |
13-FEB-2017 |
| 27791347 |
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. |
16-DEC-2016 |
23-JAN-2017 |
| US9260439 |
Dihydropyrrolopyrimidine derivatives |
16-FEB-2016 |
09-JAN-2017 |
| US9260455 |
Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
16-FEB-2016 |
09-JAN-2017 |
| 26509551 |
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases. |
12-NOV-2015 |
22-DEC-2016 |
| 26471092 |
Molecular hybridization yields triazole bronchodilators for the treatment of COPD. |
31-OCT-2015 |
15-DEC-2016 |
| 26411795 |
Discovery of spirocyclic-diamine inhibitors of mammalian acetyl CoA-carboxylase. |
31-OCT-2015 |
14-DEC-2016 |
| 25987375 |
Discovery of a novel Kv7 channel opener as a treatment for epilepsy. |
14-OCT-2015 |
04-DEC-2016 |
| 26271588 |
Recent progress in the development of small-molecule glucagon receptor antagonists. |
10-SEP-2015 |
02-DEC-2016 |
| 26258602 |
Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3. |
24-SEP-2015 |
29-NOV-2016 |
| US9233981 |
Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
12-JAN-2016 |
21-NOV-2016 |
| US9227956 |
Substituted amide compounds |
05-JAN-2016 |
14-NOV-2016 |
| 22328583 |
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. |
18-APR-2012 |
03-NOV-2016 |
| 25582600 |
Discovery of indole-derived pyridopyrazine-1,6-dione¿-secretase modulators that target presenilin. |
04-FEB-2015 |
30-OCT-2016 |
| 26005540 |
Design of Pyridopyrazine-1,6-dione¿-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability. |
25-MAY-2015 |
21-OCT-2016 |
| 26101568 |
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain. |
23-JUN-2015 |
16-OCT-2016 |
| 25893043 |
Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain. |
20-APR-2015 |
08-OCT-2016 |
| 27391855 |
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism. |
16-SEP-2016 |
04-OCT-2016 |
| US9205078 |
N-methyl-2-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-benzamide for the treatment of chronic myelogenous leukemia |
08-DEC-2015 |
27-SEP-2016 |
| US9193726 |
Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders |
24-NOV-2015 |
19-SEP-2016 |
| 26670081 |
Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities. |
17-DEC-2015 |
29-JUL-2016 |
| US9163021 |
Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors |
20-OCT-2015 |
18-JUL-2016 |
| US9156845 |
4-(substituted amino)-7H-pyrrolo[2,3-d] pyrimidines as LRRK2 inhibitors |
13-OCT-2015 |
30-JUN-2016 |
| 22522748 |
Hydralazine as a selective probe inactivator of aldehyde oxidase in human hepatocytes: estimation of the contribution of aldehyde oxidase to metabolic clearance. |
21-JUN-2012 |
08-MAY-2016 |
| 22645092 |
Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs. |
20-AUG-2012 |
08-MAY-2016 |
| 25971770 |
Progress in discovery of small-molecule modulators of protein-protein interactions via fragment screening. |
25-MAY-2015 |
07-MAY-2016 |
| 25728019 |
Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressure. |
26-MAR-2015 |
27-APR-2016 |
| 25746813 |
SAH derived potent and selective EZH2 inhibitors. |
24-MAR-2015 |
08-APR-2016 |
| 25699143 |
Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists. |
20-FEB-2015 |
04-APR-2016 |
| 25353650 |
Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. |
09-JAN-2015 |
02-APR-2016 |
| 25113930 |
Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold. |
26-AUG-2014 |
01-APR-2016 |
| 25091930 |
Structure-based design of novel human Pin1 inhibitors (III): optimizing affinity beyond the phosphate recognition pocket. |
26-AUG-2014 |
31-MAR-2016 |
| 25036503 |
Small molecule ghrelin receptor inverse agonists and antagonists. |
13-NOV-2014 |
27-MAR-2016 |
| 25423286 |
Decreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes. |
29-DEC-2014 |
13-MAR-2016 |
| US9067922 |
Chemical compounds |
30-JUN-2015 |
22-FEB-2016 |
| US9056865 |
Pyridine-2-derivatives as smoothened receptor modulators |
16-JUN-2015 |
09-FEB-2016 |
| US9045498 |
Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
02-JUN-2015 |
11-JAN-2016 |
| US9107923 |
Heteroaromatic compounds and their use as dopamine D1 ligands |
18-AUG-2015 |
11-JAN-2016 |
| US9035074 |
Pyrrolo[2,3-D]pyrimidine derivatives |
19-MAY-2015 |
14-DEC-2015 |
| US8999981 |
3-amido-pyrrolo[3,4-C]pyrazole-5(1H, 4H,6H) carbaldehyde derivatives |
07-APR-2015 |
12-OCT-2015 |
| US8993586 |
N1/N2-lactam acetyl-CoA carboxylase inhibitors |
31-MAR-2015 |
28-SEP-2015 |
| US8962616 |
Heterocyclic substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
24-FEB-2015 |
15-JUL-2015 |
| US8952008 |
Chemical compounds |
10-FEB-2015 |
22-JUN-2015 |
| US8933224 |
Triazine derivatives |
13-JAN-2015 |
08-JUN-2015 |
| US8927577 |
Quinolinyl glucagon receptor modulators |
06-JAN-2015 |
01-JUN-2015 |
| US8933221 |
Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
13-JAN-2015 |
01-JUN-2015 |
| US8933095 |
KAT II inhibitors |
13-JAN-2015 |
01-JUN-2015 |
| US8901310 |
Tricyclic compounds, compositions, and methods |
02-DEC-2014 |
04-MAY-2015 |
| US8895544 |
Indazoles |
25-NOV-2014 |
27-APR-2015 |
| US8865706 |
Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
21-OCT-2014 |
06-APR-2015 |
| US8846698 |
Pyrrolo[2,3-d]pyrimidine tropomysin-related kinase inhibitors |
30-SEP-2014 |
09-MAR-2015 |
| US8853258 |
C-linked hydroxamic acid derivatives useful as antibacterial agents |
07-OCT-2014 |
09-MAR-2015 |
| US8829010 |
Pyrazolo[3,4-d]pyrimidine compounds and their use as PDE2 inhibitors and/or CYP3A4 inhibitors |
09-SEP-2014 |
16-FEB-2015 |
| 24417533 |
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases. |
26-JUN-2014 |
12-FEB-2015 |
| 24878222 |
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT2C) receptor agonists with exquisite functional selectivity over 5-HT2A and 5-HT2B receptors. |
26-JUN-2014 |
11-FEB-2015 |
| 24900864 |
Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. |
06-JUN-2014 |
11-FEB-2015 |
| 24819116 |
Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain expo |
12-JUN-2014 |
11-FEB-2015 |
| 24694215 |
Siderophore receptor-mediated uptake of lactivicin analogues in gram-negative bacteria. |
08-MAY-2014 |
09-FEB-2015 |
| 24738581 |
Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist. |
22-MAY-2014 |
09-FEB-2015 |
| 24512187 |
Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases. |
27-FEB-2014 |
07-FEB-2015 |
| 24527807 |
1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators. |
27-MAR-2014 |
07-FEB-2015 |
| US8822494 |
Heteroaromatic compounds and their use as dopamine D1 ligands |
02-SEP-2014 |
02-FEB-2015 |
| US8791131 |
Imidazo[1,5]naphthyridine compounds, their pharmaceutical use and compositions |
29-JUL-2014 |
16-DEC-2014 |
| 24320749 |
Mechanistic characterization of a 2-thioxanthine myeloperoxidase inhibitor and selectivity assessment utilizing click chemistry--activity-based protein profiling. |
23-DEC-2013 |
30-SEP-2014 |
| US8669380 |
Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives |
11-MAR-2014 |
08-SEP-2014 |
| US8633206 |
Pyrrolo[2,3-D]pyrimidine compounds |
21-JAN-2014 |
06-AUG-2014 |
| US8633204 |
4-methylpyridopyrimidinone compounds |
21-JAN-2014 |
06-AUG-2014 |
| 24392688 |
Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator. |
13-FEB-2014 |
26-JUL-2014 |
| 24432909 |
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
27-FEB-2014 |
26-JUL-2014 |
| 24428186 |
Design, synthesis, and pharmacological evaluation of a novel series of pyridopyrazine-1,6-dione¿-secretase modulators. |
13-FEB-2014 |
26-JUL-2014 |
| 24239482 |
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia. |
02-DEC-2013 |
25-JUL-2014 |
| 24900608 |
Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example. |
14-NOV-2013 |
25-JUL-2014 |
| 24157365 |
Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists. |
01-NOV-2013 |
25-JUL-2014 |
| US8598200 |
KAT II inhibitors |
03-DEC-2013 |
18-APR-2014 |
| US8598155 |
Imidazo[5,1-f][1,2,4]triazines for the treatment of neurological disorders |
03-DEC-2013 |
18-APR-2014 |
| 23953189 |
Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor. |
06-SEP-2013 |
13-APR-2014 |
| 23981033 |
Spirolactam-based acetyl-CoA carboxylase inhibitors: toward improved metabolic stability of a chromanone lead structure. |
12-SEP-2013 |
13-APR-2014 |
| 23944843 |
Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats. |
12-SEP-2013 |
13-APR-2014 |
| 24080460 |
Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists. |
18-OCT-2013 |
13-APR-2014 |
| 23919824 |
Ligand-protein interactions of selective casein kinase 1d inhibitors. |
12-SEP-2013 |
13-APR-2014 |
| 23871442 |
Defining the key pharmacophore elements of PF-04620110: discovery of a potent, orally-active, neutral DGAT-1 inhibitor. |
09-AUG-2013 |
13-APR-2014 |
| 23831135 |
Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. |
24-JUL-2013 |
13-APR-2014 |
| 23562063 |
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus. |
23-APR-2013 |
13-APR-2014 |
| 23622982 |
Discovery of 2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as novel PKM2 activators. |
10-MAY-2013 |
13-APR-2014 |
| 23651455 |
Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand. |
13-JUN-2013 |
13-APR-2014 |
| 23566514 |
Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors. |
23-APR-2013 |
13-APR-2014 |
| 23260349 |
Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation. |
28-JAN-2013 |
13-APR-2014 |
| 23489629 |
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11ß-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
26-MAR-2013 |
12-APR-2014 |
| 23506825 |
Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series. |
15-APR-2013 |
12-APR-2014 |
| US8507533 |
Glucagon receptor modulators |
13-AUG-2013 |
07-OCT-2013 |
| 23265881 |
Design, synthesis, and evaluation of imidazo[4,5-c]pyridin-4-one derivatives with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-¿. |
14-JAN-2013 |
24-SEP-2013 |
| 23298810 |
Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: use of a conformation-based hypothesis to facilitate compound design. |
28-JAN-2013 |
24-SEP-2013 |
| 23312472 |
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
28-JAN-2013 |
24-SEP-2013 |
| 23312943 |
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase. |
28-JAN-2013 |
24-SEP-2013 |
| 23177788 |
From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor. |
18-DEC-2012 |
24-SEP-2013 |
| 23121096 |
Ion channels as therapeutic targets: a drug discovery perspective. |
14-FEB-2013 |
24-SEP-2013 |
| 23466229 |
PF-04859989 as a template for structure-based drug design: identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency. |
18-MAR-2013 |
24-SEP-2013 |
| 23614494 |
Structure-based fragment screening is demonstrated to be a practical lead discovery method for a representative G-protein-coupled receptor. |
09-MAY-2013 |
24-SEP-2013 |
| 23337601 |
Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries. |
15-FEB-2013 |
24-SEP-2013 |
| 23266122 |
Novel benzoxazole inhibitors of mPGES-1. |
14-JAN-2013 |
24-SEP-2013 |
| 24900572 |
Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes. |
10-JAN-2013 |
24-SEP-2013 |
| 24900564 |
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. |
10-JAN-2013 |
24-SEP-2013 |
| 23234271 |
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119. |
10-JAN-2013 |
24-SEP-2013 |
| 24900568 |
Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. |
10-JAN-2013 |
24-SEP-2013 |
| 24900560 |
Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions. |
10-JAN-2013 |
24-SEP-2013 |
| 16290934 |
Highly potent and selective zwitterionic agonists of the delta-opioid receptor. Part 1. |
09-JAN-2006 |
23-SEP-2013 |
| 11551757 |
Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent alpha(4)beta(1) integrin antagonists. |
11-SEP-2001 |
22-SEP-2013 |
| 15616150 |
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1. |
22-MAR-2005 |
22-MAY-2013 |
| 19700321 |
Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease. |
14-SEP-2009 |
21-MAY-2013 |
| 23153798 |
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors. |
26-NOV-2012 |
17-MAY-2013 |
| 21928839 |
Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764). |
03-NOV-2011 |
17-MAY-2013 |
| 22651823 |
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases. |
14-JUN-2012 |
17-MAY-2013 |
| 23079530 |
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides. |
05-NOV-2012 |
17-MAY-2013 |
| 22924734 |
Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of |
28-SEP-2012 |
17-MAY-2013 |
| 22866979 |
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy. |
28-SEP-2012 |
17-MAY-2013 |
| 23089526 |
The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus. |
05-NOV-2012 |
17-MAY-2013 |
| 22780914 |
Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders. |
08-NOV-2012 |
17-MAY-2013 |
| 23046961 |
Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents. |
22-OCT-2012 |
17-MAY-2013 |
| 22834877 |
Current landscape of phosphodiesterase 10A (PDE10A) inhibition. |
13-SEP-2012 |
17-MAY-2013 |
| 23025719 |
Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors. |
08-NOV-2012 |
17-MAY-2013 |
| 22974325 |
Identification of multiple 5-HT4 partial agonist clinical candidates for the treatment of Alzheimer's disease. |
08-NOV-2012 |
17-MAY-2013 |
| 23098091 |
Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay. |
26-NOV-2012 |
17-MAY-2013 |
| 22468999 |
Discovery and optimization of a novel spiropyrrolidine inhibitor ofß-secretase (BACE1) through fragment-based drug design. |
08-NOV-2012 |
17-MAY-2013 |
| 22984865 |
Spirocyclic sulfamides asß-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors. |
08-NOV-2012 |
17-MAY-2013 |
| 22196621 |
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. |
09-FEB-2012 |
17-MAY-2013 |
| 23021994 |
Identification of pyrimidine derivatives as hSMG-1 inhibitors. |
15-OCT-2012 |
17-MAY-2013 |
| 21684740 |
Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide. |
01-JUL-2011 |
17-MAY-2013 |
| 22409598 |
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
14-JUN-2012 |
17-MAY-2013 |
| 23095041 |
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. |
26-NOV-2012 |
17-MAY-2013 |
| 19743875 |
Characterization of the CHK1 allosteric inhibitor binding site. |
20-OCT-2009 |
11-MAR-2013 |
| 20804212 |
Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes. |
05-OCT-2010 |
26-FEB-2013 |
| 22749419 |
Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Ka and mTOR. |
20-JUL-2012 |
08-FEB-2013 |
| 22858141 |
Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes. |
20-AUG-2012 |
08-FEB-2013 |
| 22902656 |
Novel triazines as potent and selective phosphodiesterase 10A inhibitors. |
31-AUG-2012 |
08-FEB-2013 |
| 22898529 |
Discovery of 1-(ß-amino substituted-ß-alanyl)-N,N-dimethylindoline-2-carboxamides as novel nonpeptide antagonists of nociceptin/orphanin FQ receptor: efficient design, synthesis, and structure-activity relationship studies. |
03-SEP-2012 |
08-FEB-2013 |
| 22554206 |
Discovery of pyrroloaminopyrazoles as novel PAK inhibitors. |
24-MAY-2012 |
08-FEB-2013 |
| 22765900 |
Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors. |
20-JUL-2012 |
08-FEB-2013 |
| 22677316 |
Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor. |
15-JUN-2012 |
07-FEB-2013 |
| 22405832 |
Discovery of nor-seco himbacine analogs as thrombin receptor antagonists. |
19-MAR-2012 |
07-FEB-2013 |
| 22424974 |
Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists. |
06-APR-2012 |
07-FEB-2013 |
| 22377517 |
Design of oxobenzimidazoles and oxindoles as novel androgen receptor antagonists. |
19-MAR-2012 |
07-FEB-2013 |
| 22546671 |
Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): a tale of two waters. |
15-MAY-2012 |
07-FEB-2013 |
| 22429469 |
Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active¿-secretase modulators. |
06-APR-2012 |
07-FEB-2013 |
| 22445286 |
Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor. |
06-APR-2012 |
07-FEB-2013 |
| 22313242 |
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists. |
08-MAR-2012 |
07-FEB-2013 |
| 22542194 |
Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring. |
07-MAY-2012 |
07-FEB-2013 |
| 22560471 |
Use of libraries to access new chemical space: applications to CRTH2. |
15-MAY-2012 |
07-FEB-2013 |
| 22583618 |
Kappa agonist CovX-Bodies. |
29-MAY-2012 |
07-FEB-2013 |
| 22429467 |
Medicinal chemistry approaches to avoid aldehyde oxidase metabolism. |
06-APR-2012 |
07-FEB-2013 |
| 21641211 |
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase. |
14-JUN-2011 |
08-JAN-2013 |
| 21438541 |
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyr |
05-MAY-2011 |
07-JAN-2013 |
| 21666860 |
Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. |
21-DEC-2011 |
04-JAN-2013 |
| 20875743 |
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela |
18-OCT-2010 |
04-JAN-2013 |
| 21128663 |
An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798). |
13-JAN-2011 |
04-JAN-2013 |
| 20666458 |
Identification and characterization of acidic mammalian chitinase inhibitors. |
19-AUG-2010 |
01-JAN-2013 |
| 20672820 |
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists. |
19-AUG-2010 |
01-JAN-2013 |
| 20672822 |
Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy. |
19-AUG-2010 |
01-JAN-2013 |
| 20638844 |
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists. |
27-JUL-2010 |
01-JAN-2013 |
| 20663668 |
A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists. |
03-AUG-2010 |
01-JAN-2013 |
| 20471260 |
Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity. |
04-JUN-2010 |
31-DEC-2012 |
| 20558059 |
Structure-activity relationships and hepatic safety risks of thiazole agonists of the thrombopoietin receptor. |
08-JUL-2010 |
31-DEC-2012 |
| 20443228 |
1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. |
04-MAY-2010 |
30-DEC-2012 |
| 20329799 |
Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans. |
15-APR-2010 |
30-DEC-2012 |
| 20363633 |
Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: structure-based drug design, synthesis, and biological evaluation. |
30-APR-2010 |
30-DEC-2012 |
| 20400309 |
1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. |
04-MAY-2010 |
30-DEC-2012 |
| 19751974 |
Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase. |
28-SEP-2009 |
29-DEC-2012 |
| 20153188 |
Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores. |
22-FEB-2010 |
29-DEC-2012 |
| 19683922 |
5-(2-Pyrimidinyl)-imidazo[1,2-a]pyridines are antibacterial agents targeting the ATPase domains of DNA gyrase and topoisomerase IV. |
26-AUG-2009 |
26-DEC-2012 |
| 19775168 |
Discovery of azetidinyl ketolides for the treatment of susceptible and multidrug resistant community-acquired respiratory tract infections. |
03-DEC-2009 |
26-DEC-2012 |
| 19576766 |
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists. |
29-JUL-2009 |
24-DEC-2012 |
| 14593182 |
Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. |
31-OCT-2003 |
20-DEC-2012 |
| 19171484 |
1-Amido-1-phenyl-3-piperidinylbutanes - CCR5 antagonists for the treatment of HIV. Part 1. |
16-FEB-2009 |
20-DEC-2012 |
| 22759374 |
Identification of Type-II Inhibitors Using Kinase Structures. |
XX-NOV-2012 |
20-DEC-2012 |
| 19185490 |
1-Amido-1-phenyl-3-piperidinylbutanes--CCR5 antagonists for the treatment of HIV: part 2. |
23-FEB-2009 |
20-DEC-2012 |
| 19125610 |
Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug. |
05-FEB-2009 |
19-DEC-2012 |
| 18595689 |
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition. |
21-JUL-2008 |
17-DEC-2012 |
| 18440813 |
The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives. |
30-MAY-2008 |
16-DEC-2012 |
| 18396041 |
Molecular features crucial to the activity of pyrimidine benzamide-based thrombopoietin receptor agonists. |
05-MAY-2008 |
15-DEC-2012 |
| 18243699 |
Inhaled adenosine A(2A) receptor agonists for the treatment of chronic obstructive pulmonary disease. |
18-FEB-2008 |
15-DEC-2012 |
| 18417343 |
Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity. |
05-MAY-2008 |
15-DEC-2012 |
| 18356044 |
Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine. |
03-APR-2008 |
15-DEC-2012 |
| 18313294 |
[4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors. |
17-MAR-2008 |
15-DEC-2012 |
| 18338841 |
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections. |
08-APR-2008 |
15-DEC-2012 |
| 17537919 |
Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. |
20-JUN-2007 |
15-DEC-2012 |
| 18251495 |
Quinazolinones and pyrido[3,4-d]pyrimidin-4-ones as orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis. |
21-FEB-2008 |
15-DEC-2012 |
| 18490160 |
Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity. |
10-JUN-2008 |
15-DEC-2012 |
| 18445527 |
P2Y1 receptor antagonists as novel antithrombotic agents. |
30-MAY-2008 |
15-DEC-2012 |
| 18042383 |
Design and synthesis of a fluorescent muscarinic antagonist. |
21-JAN-2008 |
15-DEC-2012 |
| 18400496 |
Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists. |
05-MAY-2008 |
15-DEC-2012 |
| 18063367 |
Substituted oxazolidinones as novel NPC1L1 ligands for the inhibition of cholesterol absorption. |
21-JAN-2008 |
14-DEC-2012 |
| 18240382 |
1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity. |
30-JAN-2008 |
14-DEC-2012 |
| 17434304 |
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases. |
04-JUN-2007 |
13-DEC-2012 |
| 17822893 |
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization. |
18-SEP-2007 |
12-DEC-2012 |
| 17887663 |
Structure-based design and synthesis of (5-arylamino-2H-pyrazol-3-yl)-biphenyl-2',4'-diols as novel and potent human CHK1 inhibitors. |
25-OCT-2007 |
12-DEC-2012 |
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20-AUG-2011 |
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The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part III: the three microdose candidates. |
08-NOV-2010 |
14-JUN-2011 |
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Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK. |
24-NOV-2010 |
14-JUN-2011 |
| 20961062 |
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity. |
04-NOV-2010 |
14-JUN-2011 |
| 21055613 |
The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: the first clinical candidate. |
08-NOV-2010 |
14-JUN-2011 |
| 20934332 |
An in situ oxidation strategy towards overcoming hERG affinity. |
19-OCT-2010 |
13-JUN-2011 |
| 20880704 |
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability. |
19-OCT-2010 |
13-JUN-2011 |
| 20851601 |
Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity. |
19-OCT-2010 |
13-JUN-2011 |
| 20817449 |
4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors. |
20-SEP-2010 |
12-JUN-2011 |
| 20801650 |
6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics. |
13-SEP-2010 |
12-JUN-2011 |
| 20797855 |
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. |
13-SEP-2010 |
12-JUN-2011 |
| 20804199 |
Inhalation by design: novel ultra-long-actingß(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup. |
16-SEP-2010 |
11-JUN-2011 |
| 10980448 |
Human liver glycogen phosphorylase inhibitors bind at a new allosteric site. |
XX-SEP-2000 |
04-MAY-2011 |
| 20656488 |
Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1). |
16-AUG-2010 |
20-MAR-2011 |
| 20674352 |
Inhibition of interleukin-1beta converting enzyme (ICE or caspase 1) by aspartyl acyloxyalkyl ketones and aspartyl amidooxyalkyl ketones. |
16-AUG-2010 |
20-MAR-2011 |
| 20718494 |
Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury. |
19-AUG-2010 |
20-MAR-2011 |
| 20620058 |
Smoothened antagonists for hair inhibition. |
27-JUL-2010 |
19-MAR-2011 |
| 20620059 |
Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors. |
27-JUL-2010 |
19-MAR-2011 |
| 20481595 |
Design of selective, ATP-competitive inhibitors of Akt. |
17-JUN-2010 |
21-NOV-2010 |
| 20529684 |
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates. |
09-JUN-2010 |
20-NOV-2010 |
| 20462217 |
Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery. |
03-JUN-2010 |
20-NOV-2010 |
| 20471258 |
Synthesis and evaluation of azabicyclo[3.2.1]octane derivatives as potent mixed vasopressin antagonists. |
04-JUN-2010 |
20-NOV-2010 |
| 20471256 |
Synthesis and biological evaluation of tricyclic anilinopyrimidines as IKKbeta inhibitors. |
04-JUN-2010 |
20-NOV-2010 |
| 20529685 |
MMP-13 selective isonipecotamide alpha-sulfone hydroxamates. |
09-JUN-2010 |
20-NOV-2010 |
| 20430618 |
Optimisation of a pyrazole series of progesterone antagonists; Part 1. |
21-MAY-2010 |
20-NOV-2010 |
| 20462211 |
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231). |
03-JUN-2010 |
20-NOV-2010 |
| 20395140 |
Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase. |
04-MAY-2010 |
19-NOV-2010 |
| 20443629 |
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists. |
20-MAY-2010 |
19-NOV-2010 |
| 20363126 |
The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
20-APR-2010 |
19-NOV-2010 |
| 20403696 |
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility. |
04-MAY-2010 |
19-NOV-2010 |
| 20392639 |
Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist. |
04-MAY-2010 |
19-NOV-2010 |
| 20408553 |
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines. |
20-MAY-2010 |
19-NOV-2010 |
| 19501510 |
SAR of a series of inhaled A(2A) agonists and comparison of inhaled pharmacokinetics in a preclinical model with clinical pharmacokinetic data. |
14-JUL-2009 |
19-NOV-2010 |
| 20172721 |
Identification of a urea bioisostere of a triazole oxytocin antagonist. |
08-MAR-2010 |
18-NOV-2010 |
| 20202843 |
Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity. |
22-MAR-2010 |
18-NOV-2010 |
| 20227876 |
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase. |
05-APR-2010 |
18-NOV-2010 |
| 20219367 |
Discovery of small molecule isozyme non-specific inhibitors of mammalian acetyl-CoA carboxylase 1 and 2. |
22-MAR-2010 |
18-NOV-2010 |
| 20144869 |
Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template. |
22-FEB-2010 |
18-NOV-2010 |
| 20167488 |
The design and development of 2-aryl-2-hydroxy ethylamine substituted 1H,7H-pyrido[1,2,3-de]quinoxaline-6-carboxamides as inhibitors of human cytomegalovirus polymerase. |
08-MAR-2010 |
18-NOV-2010 |
| 20149653 |
C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization. |
22-FEB-2010 |
18-NOV-2010 |
| 20202838 |
Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors. |
22-MAR-2010 |
18-NOV-2010 |
| 20207139 |
Structure-based design of novel human Pin1 inhibitors (II). |
22-MAR-2010 |
18-NOV-2010 |
| 20189387 |
Identification of amide bioisosteres of triazole oxytocin antagonists. |
22-MAR-2010 |
18-NOV-2010 |
| 19647430 |
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration. |
17-AUG-2009 |
17-NOV-2010 |
| 20137931 |
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode. |
22-FEB-2010 |
17-NOV-2010 |
| 19914076 |
Aminopyridinecarboxamide-based inhibitors: Structure-activity relationship. |
03-FEB-2010 |
02-SEP-2010 |
| 20031410 |
Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists. |
03-FEB-2010 |
02-SEP-2010 |
| 20043678 |
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models. |
04-FEB-2010 |
02-SEP-2010 |
| 20045321 |
An octahydro-cyclopenta[c]pyrrole series of inhibitors of the type 1 glycine transporter. |
03-FEB-2010 |
02-SEP-2010 |
| 20196613 |
Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5). |
18-MAR-2010 |
02-SEP-2010 |
| 20005097 |
Discovery of (pyridin-4-yl)-2H-tetrazole as a novel scaffold to identify highly selective matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis. |
03-FEB-2010 |
01-SEP-2010 |
| 19969459 |
Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition. |
03-FEB-2010 |
01-SEP-2010 |
| 20015649 |
Biaryl piperidines as potent and selective delta opioid receptor ligands. |
03-FEB-2010 |
01-SEP-2010 |
| 20097563 |
Part II: piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation. |
15-FEB-2010 |
01-SEP-2010 |
| 20141147 |
Piperazinyl glutamate pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation. |
04-MAR-2010 |
01-SEP-2010 |
| 20005103 |
Synthesis and in vivo evaluation of bicyclic gababutins. |
03-FEB-2010 |
01-SEP-2010 |
| 19954973 |
Oxygenated analogues of UK-396082 as inhibitors of activated thrombin activatable fibrinolysis inhibitor. |
03-FEB-2010 |
31-AUG-2010 |
| 19963374 |
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent. |
03-FEB-2010 |
31-AUG-2010 |
| 19897364 |
Synthesis and in vivo evaluation of 3-substituted gababutins. |
03-FEB-2010 |
31-AUG-2010 |
| 19914063 |
Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity. |
03-FEB-2010 |
31-AUG-2010 |
| 19900809 |
Thyroid receptor agonists for the treatment of androgenetic alopecia. |
03-FEB-2010 |
31-AUG-2010 |
| 19796941 |
Piperazinyl-glutamate-pyrimidines as potent P2Y12 antagonists for inhibition of platelet aggregation. |
12-OCT-2009 |
30-AUG-2010 |
| 19748783 |
Thienopyrimidine-based P2Y12 platelet aggregation inhibitors. |
28-SEP-2009 |
30-AUG-2010 |
| 19748778 |
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. |
28-SEP-2009 |
30-AUG-2010 |
| 19631533 |
Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one. |
17-AUG-2009 |
30-AUG-2010 |
| 19740658 |
Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2. |
28-SEP-2009 |
30-AUG-2010 |
| 19683918 |
Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: potent, orally-active 1,4-disubstituted imidazoles. |
26-AUG-2009 |
30-AUG-2010 |
| 19692241 |
Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT(2C) agonists. |
26-AUG-2009 |
30-AUG-2010 |
| 19646865 |
Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence. |
17-AUG-2009 |
30-AUG-2010 |
| 19782566 |
Optimising metabolic stability in lipophilic chemical space: the identification of a metabolically stable pyrazolopyrimidine CRF-1 receptor antagonist. |
12-OCT-2009 |
30-AUG-2010 |
| 19716297 |
Design and synthesis of pyridazinone-based 5-HT(2C) agonists. |
14-SEP-2009 |
30-AUG-2010 |
| 19854053 |
Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists. |
05-NOV-2009 |
29-AUG-2010 |
| 19919087 |
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy. |
17-DEC-2009 |
29-AUG-2010 |
| 19616945 |
Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency. |
29-JUL-2009 |
27-AUG-2010 |
| 19540112 |
Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors. |
14-JUL-2009 |
27-AUG-2010 |
| 19604694 |
Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation. |
29-JUL-2009 |
27-AUG-2010 |
| 19616942 |
Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency. |
29-JUL-2009 |
27-AUG-2010 |
| 19616432 |
Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template. |
29-JUL-2009 |
27-AUG-2010 |
| 19500981 |
Rapid assessment of a novel series of selective CB(2) agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis. |
14-JUL-2009 |
27-AUG-2010 |
| 19539468 |
Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system. |
14-JUL-2009 |
26-AUG-2010 |
| 19359175 |
4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships. |
04-MAY-2009 |
26-AUG-2010 |
| 19376698 |
Aryloxypyrazines as highly selective antagonists of Oxytocin. |
04-MAY-2009 |
26-AUG-2010 |
| 19410451 |
The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter. |
15-MAY-2009 |
25-AUG-2010 |
| 19209845 |
Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor. |
03-JUN-2010 |
25-AUG-2010 |
| 19250823 |
Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. |
16-MAR-2009 |
25-AUG-2010 |
| 19285862 |
Piperidinyl-2-phenethylamino inhibitors of DPP-IV for the treatment of type 2 diabetes. |
03-APR-2009 |
11-JAN-2010 |
| 19286380 |
Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production. |
03-APR-2009 |
11-JAN-2010 |
| 18804369 |
Small, non-peptide C5a receptor antagonists: part 2. |
20-OCT-2008 |
11-JAN-2010 |
| 19167884 |
The design and discovery of novel amide CCR5 antagonists. |
16-FEB-2009 |
11-JAN-2010 |
| 19414260 |
6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists. |
15-MAY-2009 |
11-JAN-2010 |
| 19121937 |
Discovery and SAR of benzyl phenyl ethers as inhibitors of bacterial phenylalanyl-tRNA synthetase. |
27-JAN-2009 |
11-JAN-2010 |
| 17623656 |
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects. |
14-SEP-2007 |
11-JAN-2010 |
| 19275964 |
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
16-MAR-2009 |
11-JAN-2010 |
| 19201190 |
4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production. |
23-FEB-2009 |
11-JAN-2010 |
| 19282174 |
Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. |
03-APR-2009 |
11-JAN-2010 |
| 19339180 |
The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents. |
17-APR-2009 |
11-JAN-2010 |
| 18571404 |
Designing rapid onset selective serotonin re-uptake inhibitors. 2: structure-activity relationships of substituted (aryl)benzylamines. |
21-JUL-2008 |
11-JAN-2010 |
| 19269173 |
7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization. |
16-MAR-2009 |
11-JAN-2010 |
| 18951784 |
Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule. |
13-NOV-2008 |
11-JAN-2010 |
| 19246199 |
Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists. |
09-MAR-2009 |
11-JAN-2010 |
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3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization. |
17-APR-2009 |
11-JAN-2010 |
| 19327989 |
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors. |
03-APR-2009 |
11-JAN-2010 |
| 18945617 |
Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents. |
25-NOV-2008 |
11-JAN-2010 |
| 18621528 |
Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity. |
29-JUL-2008 |
11-JAN-2010 |
| 19239259 |
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration. |
19-MAR-2009 |
11-JAN-2010 |
| 19186055 |
The identification of orally bioavailable thrombopoietin agonists. |
23-FEB-2009 |
11-JAN-2010 |
| 19019675 |
Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK? |
26-DEC-2008 |
11-JAN-2010 |
| 18778939 |
Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent. |
23-SEP-2008 |
11-JAN-2010 |
| 18809326 |
Small, non-peptide C5a receptor antagonists: part 1. |
20-OCT-2008 |
11-JAN-2010 |
| 19346127 |
Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists. |
17-APR-2009 |
11-JAN-2010 |
| 18980842 |
Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists. |
25-NOV-2008 |
11-JAN-2010 |
| 18755586 |
Design and synthesis of fluorescent SGLT2 inhibitors. |
15-SEP-2008 |
11-JAN-2010 |
| 18948001 |
Quantitative structure-activity relationship of phenoxyphenyl-methanamine compounds with 5HT2A, SERT, and hERG activities. |
13-NOV-2008 |
11-JAN-2010 |
| 18782666 |
Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: structure-activity relationships of (thioalkyl)phenoxy benzylamines. |
23-SEP-2008 |
11-JAN-2010 |
| 18951788 |
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation. |
13-NOV-2008 |
11-JAN-2010 |
| 18812259 |
3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: a novel series of mGluR2 positive allosteric modulators. |
20-OCT-2008 |
11-JAN-2010 |
| 18799310 |
Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist. |
20-OCT-2008 |
11-JAN-2010 |
| 19394220 |
Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks. |
15-MAY-2009 |
11-JAN-2010 |
| 19231185 |
2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology. |
09-MAR-2009 |
11-JAN-2010 |
| 19231206 |
Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action. |
20-MAR-2009 |
11-JAN-2010 |
| 19147349 |
Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists. |
16-FEB-2009 |
11-JAN-2010 |
| 18639455 |
Design and optimization of potent, selective antagonists of Oxytocin. |
29-JUL-2008 |
11-JAN-2010 |
| 18640044 |
Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'. |
11-AUG-2008 |
11-JAN-2010 |
| 18625557 |
N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors. |
29-JUL-2008 |
11-JAN-2010 |
| 17964000 |
Structure activity relationships of quinoline-containing c-Met inhibitors. |
02-JUN-2008 |
11-JAN-2010 |
| 19097791 |
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor. |
01-FEB-2009 |
25-NOV-2009 |
| 17988109 |
Antibacterial oxazolidinones possessing a novel C-5 side chain. (5R)-trans-3-[3-Fluoro-4- (1-oxotetrahydrothiopyran-4-yl)phenyl]-2- oxooxazolidine-5-carboxylic acid amide (PF-00422602), a new lead compound. |
26-NOV-2007 |
11-NOV-2009 |
| 18155908 |
Synthesis of benzamide derivatives as TRPV1 antagonists. |
05-FEB-2008 |
11-NOV-2009 |
| 17935984 |
Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13. |
06-NOV-2007 |
11-NOV-2009 |
| 17976986 |
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route. |
16-NOV-2007 |
11-NOV-2009 |
| 17967540 |
Stereoselective synthesis of a novel 2-aza-7-oxabicyclo[3.3.0]octane as neurokinin-1 receptor antagonist. |
16-NOV-2007 |
11-NOV-2009 |
| 18155906 |
Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors. |
05-FEB-2008 |
11-NOV-2009 |
| 17990866 |
Discovery of potent& selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis. |
26-NOV-2007 |
11-NOV-2009 |
| 18160289 |
1-Aminoindanes as novel motif with potential atypical antipsychotic properties. |
21-JAN-2008 |
11-NOV-2009 |
| 17936624 |
Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists. |
06-NOV-2007 |
11-NOV-2009 |
| 17977724 |
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors. |
16-NOV-2007 |
11-NOV-2009 |
| 18029177 |
A novel series of highly selective inhibitors of MMP-3. |
13-FEB-2008 |
11-NOV-2009 |
| 17583500 |
Aminopyrrolidineamide inhibitors of site-1 protease. |
30-JUL-2007 |
10-NOV-2009 |
| 17723296 |
Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists. |
18-SEP-2007 |
10-NOV-2009 |
| 17766112 |
Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production. |
18-SEP-2007 |
10-NOV-2009 |
| 17590335 |
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. |
30-JUL-2007 |
10-NOV-2009 |
| 17888659 |
Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists. |
16-OCT-2007 |
10-NOV-2009 |
| 17768047 |
Discovery of novel and orally active NR2B-selective N-methyl-D-aspartate (NMDA) antagonists, pyridinol derivatives with reduced HERG binding affinity. |
18-SEP-2007 |
10-NOV-2009 |
| 17766106 |
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain. |
18-SEP-2007 |
10-NOV-2009 |
| 17562362 |
N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain. |
30-JUL-2007 |
10-NOV-2009 |
| 17632003 |
Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity. |
22-AUG-2007 |
10-NOV-2009 |
| 17764935 |
Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production. |
18-SEP-2007 |
10-NOV-2009 |
| 17591762 |
Potent and selective nonpeptidic inhibitors of procollagen C-proteinase. |
19-JUL-2007 |
10-NOV-2009 |
| 17827014 |
Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor. |
18-SEP-2007 |
10-NOV-2009 |
| 17570666 |
Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). |
30-JUL-2007 |
10-NOV-2009 |
| 17512197 |
Synthesis and SAR of selective benzothiophene, benzofuran, and indole-based peroxisome proliferator-activated receptor delta agonists. |
18-JUN-2007 |
10-NOV-2009 |
| 17827000 |
(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production. |
01-OCT-2007 |
10-NOV-2009 |
| 17566736 |
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa. |
30-JUL-2007 |
10-NOV-2009 |
| 17574412 |
Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors. |
30-JUL-2007 |
10-NOV-2009 |
| 17574411 |
Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors. |
30-JUL-2007 |
10-NOV-2009 |
| 17766107 |
Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation. |
18-SEP-2007 |
10-NOV-2009 |
| 17498950 |
Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) delta agonists. |
18-JUN-2007 |
10-NOV-2009 |
| 17383873 |
Piperazinyl CCR1 antagonists--optimization of human liver microsome stability. |
14-MAY-2007 |
10-NOV-2009 |
| 17387018 |
Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective alphavbeta3 inhibitor: design, synthesis, and optimization. |
10-APR-2007 |
10-NOV-2009 |
| 17267217 |
N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors. |
13-MAR-2007 |
10-NOV-2009 |
| 17303420 |
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents. |
02-APR-2007 |
10-NOV-2009 |
| 17070062 |
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder. |
20-NOV-2006 |
10-NOV-2009 |
| 16722655 |
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist. |
25-MAY-2006 |
10-NOV-2009 |
| 17257843 |
A novel, non-substrate-based series of glycine type 1 transporter inhibitors derived from high-throughput screening. |
23-FEB-2007 |
10-NOV-2009 |
| 17434734 |
Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1. |
04-JUN-2007 |
10-NOV-2009 |
| 17064898 |
Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain. |
15-JAN-2007 |
10-NOV-2009 |
| 17707640 |
Pyrimidine benzamide-based thrombopoietin receptor agonists. |
18-SEP-2007 |
10-NOV-2009 |
| 17049233 |
Design of potent inhibitors of human beta-secretase. Part 2. |
25-DEC-2006 |
10-NOV-2009 |
| 16263283 |
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists. |
26-DEC-2005 |
10-NOV-2009 |
| 16087333 |
8-Substituted 3,4-dihydroquinolinones as a novel scaffold for atypical antipsychotic activity. |
12-SEP-2005 |
10-NOV-2009 |
| 17046251 |
Design of potent inhibitors of human beta-secretase. Part 1. |
25-DEC-2006 |
10-NOV-2009 |
| 16621534 |
Synthesis of pyrazoles and isoxazoles as potent alpha(v)beta3 receptor antagonists. |
08-MAY-2006 |
10-NOV-2009 |
| 17064062 |
3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms. |
26-OCT-2006 |
10-NOV-2009 |
| 16115768 |
New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors. |
26-SEP-2005 |
10-NOV-2009 |
| 16529928 |
Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents. |
24-APR-2006 |
10-NOV-2009 |
| 17399986 |
R-isomers of Arg-Gly-Asp (RGD) mimics as potent alphavbeta3 inhibitors. |
30-APR-2007 |
10-NOV-2009 |
| 17060518 |
Development of a novel dicistronic reporter-selectable hepatitis C virus replicon suitable for high-throughput inhibitor screening. |
21-DEC-2006 |
10-NOV-2009 |
| 17398092 |
The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer. |
14-MAY-2007 |
10-NOV-2009 |
| 16979341 |
Pyridine-2-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents. |
10-NOV-2006 |
10-NOV-2009 |
| 16942871 |
Potent, selective pyrimidinetrione-based inhibitors of MMP-13. |
09-OCT-2006 |
10-NOV-2009 |
| 16219463 |
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands. |
01-NOV-2005 |
10-NOV-2009 |
| 16275071 |
A new chemical tool for exploring the physiological function of the PDE2 isozyme. |
25-NOV-2005 |
10-NOV-2009 |
| 16303301 |
Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties. |
09-JAN-2006 |
10-NOV-2009 |
| 16298127 |
Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists. |
09-JAN-2006 |
10-NOV-2009 |
| 16464581 |
The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor. |
20-MAR-2006 |
10-NOV-2009 |
| 16973358 |
Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents. |
10-NOV-2006 |
10-NOV-2009 |
| 16380252 |
5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers. |
27-JAN-2006 |
10-NOV-2009 |
| 16722626 |
cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization. |
25-MAY-2006 |
10-NOV-2009 |
| 17276061 |
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity. |
13-MAR-2007 |
10-NOV-2009 |
| 16039119 |
Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3-(substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption. |
02-AUG-2005 |
10-NOV-2009 |
| 16824756 |
Identification and structure-based optimization of novel dihydropyrones as potent HCV RNA polymerase inhibitors. |
14-AUG-2006 |
10-NOV-2009 |
| 16821800 |
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder. Synthesis and activity of functionalized glutaramides. |
06-JUL-2006 |
10-NOV-2009 |
| 16821801 |
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship. |
06-JUL-2006 |
10-NOV-2009 |
| 16782336 |
Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc. |
31-JUL-2006 |
10-NOV-2009 |
| 16263279 |
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function. |
26-DEC-2005 |
10-NOV-2009 |
| 16125385 |
The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex. |
26-SEP-2005 |
10-NOV-2009 |
| 15953722 |
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13. |
24-JUN-2005 |
10-NOV-2009 |
| 15482916 |
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease. |
14-OCT-2004 |
10-NOV-2009 |
| 15149647 |
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist. |
19-MAY-2004 |
10-NOV-2009 |
| 15324896 |
3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase. |
24-AUG-2004 |
10-NOV-2009 |
| 15863327 |
5-Lipoxygenase inhibitors: convenient synthesis of 4-[3-(4-heterocyclylphenylthio)phenyl]-3,4,5,6-tetrahydro-2H-pyran-4-carboxamide analogues. |
02-MAY-2005 |
10-NOV-2009 |
| 15481984 |
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase. |
14-OCT-2004 |
10-NOV-2009 |
| 15913999 |
Structure-based design and synthesis of pyrazinones containing novel P1 'side pocket' moieties as inhibitors of TF/VIIa. |
31-MAY-2005 |
10-NOV-2009 |
| 15324876 |
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1. |
24-AUG-2004 |
10-NOV-2009 |
| 15324877 |
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives. |
24-AUG-2004 |
10-NOV-2009 |
| 15149695 |
New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors. |
19-MAY-2004 |
10-NOV-2009 |
| 15324874 |
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies. |
24-AUG-2004 |
10-NOV-2009 |
| 12747787 |
Discovery of a simple picomolar inhibitor of cholesteryl ester transfer protein. |
15-MAY-2003 |
10-NOV-2009 |
| 12668004 |
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors. |
01-APR-2003 |
10-NOV-2009 |
| 16143527 |
Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors. |
26-SEP-2005 |
10-NOV-2009 |
| 16143519 |
The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases. |
20-MAR-2006 |
10-NOV-2009 |
| 15780611 |
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14. |
22-MAR-2005 |
10-NOV-2009 |
| 16314097 |
Designing rapid onset selective serotonin re-uptake inhibitors. Part 1: Structure-activity relationships of substituted (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthaleneamine. |
27-JAN-2006 |
10-NOV-2009 |
| 15911259 |
Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13. |
24-MAY-2005 |
10-NOV-2009 |
| 16002291 |
Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors. |
25-JUL-2005 |
10-NOV-2009 |
| 15863301 |
Inhibitors of HCV NS5B polymerase. Part 1: Evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid. |
02-MAY-2005 |
10-NOV-2009 |
| 15911260 |
Inhibitors of HCV NS5B polymerase. Part 2: Evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid. |
24-MAY-2005 |
10-NOV-2009 |
| 15081001 |
The discovery of structurally novel CCR1 antagonists derived from a hydroxyethylene peptide isostere template. |
14-APR-2004 |
10-NOV-2009 |
| 15081002 |
Potent small molecule CCR1 antagonists. |
14-APR-2004 |
10-NOV-2009 |
| 12657266 |
[3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter. |
26-MAR-2003 |
10-NOV-2009 |
| 12951101 |
Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors. |
02-SEP-2003 |
10-NOV-2009 |
| 12877590 |
A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. |
24-JUL-2003 |
10-NOV-2009 |
| 14552767 |
A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 1,2-benzothiazepines. |
13-OCT-2003 |
10-NOV-2009 |
| 12540233 |
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor. |
23-JAN-2003 |
10-NOV-2009 |
| 16442794 |
Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats. |
27-FEB-2006 |
10-NOV-2009 |
| 12565933 |
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics. |
04-FEB-2003 |
10-NOV-2009 |
| 15745802 |
Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). |
04-MAR-2005 |
10-NOV-2009 |
| 15603973 |
5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization. |
17-DEC-2004 |
10-NOV-2009 |
| 15837327 |
Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors. |
19-APR-2005 |
10-NOV-2009 |
| 14505677 |
Structure-activity relationship studies on 2-heteroaryl-4-arylimidazoles NPY5 receptor antagonists. |
24-SEP-2003 |
10-NOV-2009 |
| 14736252 |
4-[5-Fluoro-3-[4-(2-methyl-1H-imidazol-1-yl)benzyloxy]phenyl]-3,4,5,6- tetrahydro-2H-pyran-4-carboxamide, an orally active inhibitor of 5-lipoxygenase with improved pharmacokinetic and toxicology characteristics. |
22-JAN-2004 |
10-NOV-2009 |
| 14980668 |
Subtype selective NMDA receptor antagonists: evaluation of some novel alkynyl analogues. |
24-FEB-2004 |
10-NOV-2009 |
| 12798336 |
4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK(2)) receptor. |
11-JUN-2003 |
10-NOV-2009 |
| 11992783 |
Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors. |
06-MAY-2002 |
10-NOV-2009 |
| 14684289 |
Design and SAR of thienopyrimidine and thienopyridine inhibitors of VEGFR-2 kinase activity. |
19-DEC-2003 |
10-NOV-2009 |
| 15081003 |
Novel CCR1 antagonists with improved metabolic stability. |
14-APR-2004 |
10-NOV-2009 |
| 14741295 |
The design and synthesis of sulfonamides as caspase-1 inhibitors. |
26-JAN-2004 |
10-NOV-2009 |
| 15125923 |
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists. |
05-MAY-2004 |
10-NOV-2009 |
| 14684306 |
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine. |
19-DEC-2003 |
10-NOV-2009 |
| 15006384 |
Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists. |
09-MAR-2004 |
10-NOV-2009 |
| 14998342 |
Structure-activity relationships of potent, selective inhibitors of neuronal nitric oxide synthase based on the 6-phenyl-2-aminopyridine structure. |
04-MAR-2004 |
10-NOV-2009 |
| 12392732 |
Discovery and biological characterization of capromorelin analogues with extended half-lives. |
23-OCT-2002 |
10-NOV-2009 |
| 11844695 |
Human glucagon receptor antagonists based on alkylidene hydrazides. |
14-FEB-2002 |
10-NOV-2009 |
| 11784155 |
Orally-effective, long-acting sorbitol dehydrogenase inhibitors: synthesis, structure-activity relationships, and in vivo evaluations of novel heterocycle-substituted piperazino-pyrimidines. |
10-JAN-2002 |
10-NOV-2009 |
| 11543683 |
Identification of alkylidene hydrazides as glucagon receptor antagonists. |
06-SEP-2001 |
10-NOV-2009 |
| 11591509 |
alpha-Amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1. |
09-OCT-2001 |
10-NOV-2009 |
| 11591512 |
Small molecule somatostatin receptor subtype-2 antagonists. |
09-OCT-2001 |
10-NOV-2009 |
| 11755336 |
The design and synthesis of a novel series of indole derived selective ET(A) antagonists. |
28-DEC-2001 |
10-NOV-2009 |
| 12408707 |
Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure. |
31-OCT-2002 |
10-NOV-2009 |
| 12781194 |
3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. |
03-JUN-2003 |
10-NOV-2009 |
| 11495581 |
Sorbitol dehydrogenase inhibitors (SDIs): a new potent, enantiomeric SDI, 4-[2-1R-hydroxy-ethyl)-pyrimidin-4-yl]piperazine-1-sulfonic acid dimethylamide. |
09-AUG-2001 |
10-NOV-2009 |
| 12781180 |
Structure-activity relationships in a series of NPY Y5 antagonists: 3-amido-9-ethylcarbazoles, core-modified analogues and amide isosteres. |
03-JUN-2003 |
10-NOV-2009 |
| 12190310 |
Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: synthesis, in vitro characterization, and X-ray crystallography. |
22-AUG-2002 |
10-NOV-2009 |
| 11755349 |
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines. |
28-DEC-2001 |
10-NOV-2009 |
| 11755350 |
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 2: (3-Substituted-5-halo-2-pyridinyl)guanidines. |
28-DEC-2001 |
10-NOV-2009 |
| 12238919 |
A sorbitol dehydrogenase inhibitor of exceptional in vivo potency with a long duration of action: 1-(R)-[4-[4-(4,6-dimethyl[1,3,5]triazin-2-yl)- 2R,6S-dimethylpiperazin-1-yl]pyrimidin-2- yl]ethanol. |
19-SEP-2002 |
10-NOV-2009 |
| 11101348 |
Discovery of chiral N,N-disubstituted trifluoro-3-amino-2-propanols as potent inhibitors of cholesteryl ester transfer protein. |
13-AUG-2001 |
10-NOV-2009 |
| 12036353 |
Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence. |
30-MAY-2002 |
10-NOV-2009 |
| 11985469 |
Structure-based design of a parallel synthetic array directed toward the discovery of irreversible inhibitors of human rhinovirus 3C protease. |
02-MAY-2002 |
10-NOV-2009 |
| 10956225 |
Selective cyclooxygenase-2 inhibitors: heteroaryl modified 1,2-diarylimidazoles are potent, orally active antiinflammatory agents. |
08-SEP-2000 |
10-NOV-2009 |
| 10794682 |
N-[[(5-methyl-3-phenylisoxazol-4-yl)-phenyl]sulfonyl]propanamide, sodium salt, parecoxib sodium: A potent and selective inhibitor of COX-2 for parenteral administration. |
29-JUN-2000 |
10-NOV-2009 |
| 12593645 |
In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist. |
20-FEB-2003 |
10-NOV-2009 |
| 12643929 |
Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase. |
19-MAR-2003 |
10-NOV-2009 |
| 12519059 |
Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. |
09-JAN-2003 |
10-NOV-2009 |
| 10498210 |
A new class of selective and potent inhibitors of neuronal nitric oxide synthase. |
28-OCT-1999 |
10-NOV-2009 |
| 9934474 |
Development of 2,2-dimethylchromanol cysteinyl LT1 receptor antagonists. |
05-APR-1999 |
10-NOV-2009 |
| 9873560 |
N-carbamoyl analogs of Zafirlukast: potent receptor antagonists of leukotriene D4. |
02-FEB-1999 |
10-NOV-2009 |
| 11354379 |
Design and synthesis of 2-oxo-imidazolidine-4-carboxylic acid hydroxyamides as potent matrix metalloproteinase-13 inhibitors. |
16-MAY-2001 |
10-NOV-2009 |
| 11063603 |
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors. |
20-NOV-2000 |
10-NOV-2009 |
| 11277524 |
Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility. |
29-MAR-2001 |
10-NOV-2009 |
| 11229773 |
Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality. |
02-MAR-2001 |
10-NOV-2009 |
| 11229774 |
Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1). |
02-MAR-2001 |
10-NOV-2009 |
| 12031323 |
SAR and species/stereo-selective metabolism of the sorbitol dehydrogenase inhibitor, CP-470,711. |
28-MAY-2002 |
10-NOV-2009 |
| 9873486 |
Thromboxane modulating agents. 4. Design and synthesis of 3-(2-[[(4-chlorophenyl)sulfonyl]-amino]ethyl)benzenepropanoic acid derivatives as potent thromboxane receptor antagonists. |
28-JAN-1999 |
10-NOV-2009 |
| 10882354 |
Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold. |
24-JUL-2000 |
10-NOV-2009 |
| 10509933 |
Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity. |
04-NOV-1999 |
10-NOV-2009 |
| 9871530 |
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist. |
27-JAN-1999 |
10-NOV-2009 |
| 10741545 |
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands. |
13-JUN-2000 |
10-NOV-2009 |
| 10021913 |
Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket. |
11-MAY-1999 |
10-NOV-2009 |
| 10915056 |
Difluoroketones as inhibitors of matrix metalloprotease-13. |
28-NOV-2000 |
10-NOV-2009 |
| 17919904 |
Synthesis of aromatic compounds containing a 1,1-dialkyl-2-trifluoromethyl group, a bioisostere of the tert-alkyl moiety. |
16-OCT-2007 |
10-NOV-2009 |
| 15149680 |
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. |
19-MAY-2004 |
10-NOV-2009 |
| 9171885 |
Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist. |
27-JUN-1997 |
10-NOV-2009 |
| 9685232 |
Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase. |
17-AUG-1998 |
10-NOV-2009 |
| 8568801 |
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. |
01-MAR-1996 |
10-NOV-2009 |
| 9341919 |
Thromboxane modulating agents. 3. 1H-imidazol-1-ylalkyl- and 3-pyridinylalkyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives as dual thromboxane synthase inhibitor/thromboxane receptor antagonists. |
28-NOV-1997 |
10-NOV-2009 |
| 8064800 |
Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. |
22-SEP-1994 |
10-NOV-2009 |
| 8057297 |
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity. |
13-SEP-1994 |
10-NOV-2009 |
| 9544217 |
(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol. |
04-MAY-1998 |
10-NOV-2009 |
| 1378901 |
The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst. |
26-AUG-1992 |
10-NOV-2009 |
| 1282570 |
Discovery of a potent substance P antagonist: recognition of the key molecular determinant. |
08-FEB-1993 |
10-NOV-2009 |
| 8027982 |
Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates. |
09-AUG-1994 |
10-NOV-2009 |
| 9464356 |
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4. |
27-FEB-1998 |
10-NOV-2009 |
| 1447752 |
Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin. |
28-DEC-1992 |
10-NOV-2009 |
| 1433172 |
1-(2-Aminoethyl)-3-methyl-8,9-dihydropyrano[3,2-e]indole: a rotationally restricted phenolic analog of the neurotransmitter serotonin and agonist selective for serotonin (5-HT2-type) receptors. |
18-DEC-1992 |
10-NOV-2009 |
| 7636841 |
5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety. |
12-SEP-1995 |
10-NOV-2009 |
| 7932545 |
(+)-1-(3S,4R)-[3-(4-phenylbenzyl)-4-hydroxychroman-7-yl]cyclopentane carboxylic acid, a highly potent, selective leukotriene B4 antagonist with oral activity in the murine collagen-induced arthritis model. |
03-NOV-1994 |
10-NOV-2009 |
| 7527861 |
Importance of parallel vectors and"hydrophobic collapse" of the aligned aromatic rings: discovery of a potent substance P antagonist. |
13-JAN-1995 |
10-NOV-2009 |
| 8176701 |
Potent, selective, and systemically-available inhibitors of acyl-coenzyme A:cholesterol acyl transferase (ACAT). |
09-JUN-1994 |
10-NOV-2009 |
| 1681106 |
Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds. |
18-NOV-1991 |
10-NOV-2009 |
| 1676427 |
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents. |
06-AUG-1991 |
10-NOV-2009 |
| 1899452 |
Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners. |
12-MAR-1991 |
10-NOV-2009 |
| 7966138 |
5-Phenyl-3-ureidobenzazepin-2-ones as cholecystokinin-B receptor antagonists. |
20-DEC-1994 |
10-NOV-2009 |
| 7520943 |
Aza-tricyclic substance P antagonists. |
23-SEP-1994 |
10-NOV-2009 |
| 1613743 |
Orally active aldose reductase inhibitors: indazoleacetic, oxopyridazineacetic, and oxopyridopyridazineacetic acid derivatives. |
27-JUL-1992 |
10-NOV-2009 |
| 1738141 |
Potent, orally active aldose reductase inhibitors related to zopolrestat: surrogates for benzothiazole side chain. |
17-MAR-1992 |
10-NOV-2009 |
| 2498517 |
Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors. |
11-JUL-1989 |
10-NOV-2009 |
| 2374139 |
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole. |
30-AUG-1990 |
10-NOV-2009 |
| 19729306 |
Structure-based design of novel human Pin1 inhibitors (I). |
01-OCT-2009 |
08-NOV-2009 |
| 18394907 |
Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies. |
01-MAY-2008 |
08-NOV-2009 |
| 19783444 |
Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists. |
15-OCT-2009 |
27-OCT-2009 |
| 19413326 |
Discovery of antibacterial biotin carboxylase inhibitors by virtual screening and fragment-based approaches. |
19-JUN-2009 |
13-OCT-2009 |
| 19630403 |
Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia (dagger) dagger Coordinates of the PDE10A crystal structures have been depo |
24-JUL-2009 |
14-SEP-2009 |
| 17480064 |
Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). |
31-MAY-2007 |
05-JUL-2009 |
| 19438227 |
Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors. |
11-JUN-2009 |
03-JUL-2009 |
| 19473839 |
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
01-JUL-2009 |
01-JUL-2009 |
| 19351113 |
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. |
14-MAY-2009 |
25-MAY-2009 |
| 19346128 |
Synthesis and SAR of tolylamine 5-HT6 antagonists. |
01-MAY-2009 |
05-MAY-2009 |
| 19175319 |
Novel Indazole Non-Nucleoside Reverse Transcriptase Inhibitors Using Molecular Hybridization Based on Crystallographic Overlays (dagger). |
28-JAN-2009 |
24-MAR-2009 |
| 19102698 |
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. |
22-JAN-2009 |
08-MAR-2009 |
| 17949010 |
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. |
13-NOV-2007 |
08-FEB-2009 |
| 18005335 |
Selectivity-determining residues in Plk1. |
XX-DEC-2007 |
24-JAN-2009 |
| 15911271 |
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamides. |
02-JUN-2005 |
18-DEC-2008 |
| 18921992 |
Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications. |
13-NOV-2008 |
21-NOV-2008 |
| 17095227 |
Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinasegamma. |
01-FEB-2007 |
27-OCT-2008 |
| 16632359 |
Discovery of novel isothiazole inhibitors of the TrkA kinase: structure-activity relationship, computer modeling, optimization, and identification of highly potent antagonists. |
01-JUL-2006 |
13-OCT-2008 |
| 18456494 |
Synthesis and structure based optimization of novel Akt inhibitors. |
01-JUN-2008 |
13-OCT-2008 |
| 16451085 |
Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands. |
09-FEB-2006 |
12-JUL-2008 |
| 18260619 |
Synthesis and SAR of 2-Aryloxy-4-alkoxy-pyridines as Potent Orally Active Corticotropin-Releasing Factor 1 Receptor Antagonists. |
13-MAR-2008 |
28-MAR-2008 |
| 18288792 |
2-Aryloxy-4-alkylaminopyridines: Discovery of Novel Corticotropin-Releasing Factor 1 Antagonists. |
13-MAR-2008 |
28-MAR-2008 |
| 18072721 |
Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia. |
10-JAN-2008 |
16-MAR-2008 |
| 17948975 |
Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase. |
15-NOV-2007 |
09-DEC-2007 |
| 17764936 |
Pyrazole inhibitors of HMG-CoA reductase: An attempt to dramatically reduce synthetic complexity through minimal analog re-design. |
15-OCT-2007 |
16-OCT-2007 |
| 17560788 |
Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase. |
15-AUG-2007 |
08-OCT-2007 |
| 15755665 |
Discovery of novel non-peptidic ketopiperazine-based renin inhibitors. |
01-APR-2005 |
19-SEP-2007 |
| 17574423 |
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors. |
01-SEP-2007 |
19-SEP-2007 |
| 17482464 |
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors. |
01-JUL-2007 |
19-SEP-2007 |
| 16480874 |
Ketopiperazine-based renin inhibitors: optimization of the "C" ring. |
01-MAY-2006 |
19-SEP-2007 |
| 15582452 |
The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors. |
03-JAN-2005 |
19-SEP-2007 |
| 17113558 |
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors. |
01-JAN-2007 |
19-SEP-2007 |
| 16190759 |
A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners. |
06-OCT-2005 |
17-JUL-2007 |
| 16759861 |
Structure-activity relationships of triazolopyridine oxazole p38 inhibitors: identification of candidates for clinical development. |
15-AUG-2006 |
02-JUL-2007 |
| 12773033 |
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one. |
05-JUN-2003 |
02-JUL-2007 |
| 17447747 |
Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines. |
17-MAY-2007 |
03-JUN-2007 |
| 16134941 |
Theoretical and experimental design of atypical kinase inhibitors: application to p38 MAP kinase. |
08-SEP-2005 |
07-MAY-2007 |
| 15012994 |
Benzimidazolone p38 inhibitors. |
23-FEB-2004 |
07-MAY-2007 |
| 17228859 |
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors. |
25-JAN-2007 |
09-APR-2007 |
| 16759100 |
A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability. |
15-JUN-2006 |
26-MAR-2007 |
| 11738604 |
Structure-based design of nonpeptide inhibitors of interleukin-1beta converting enzyme (ICE, caspase-1). |
XX-JAN-2002 |
26-NOV-2006 |
| 11591522 |
Structure-based design of caspase-1 inhibitor containing a diphenyl ether sulfonamide. |
22-OCT-2001 |
24-NOV-2006 |
| 16220987 |
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy. |
20-OCT-2005 |
07-NOV-2006 |
| 15801830 |
Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4. |
07-APR-2005 |
02-NOV-2005 |
| 15801831 |
Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. |
07-APR-2005 |
27-OCT-2005 |
| 7518523 |
Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors. |
08-JUL-1994 |
28-APR-2005 |
| 11384237 |
Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity. |
07-JUN-2001 |
02-MAR-2005 |
| TBD |
Inhibiting protein-protein interactions: a model for antagonist design |
26-MAY-2000 |
05-DEC-2000 |
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