The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28621538 |
63 |
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo. |
Novartis Pharma |
28157311 |
11 |
Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors. |
Novartis Institutes For Biomedical Research |
28012344 |
9 |
An efficient anticoagulant candidate: Characterization, synthesis and in vivo study of a fondaparinux analogue Rrt1.17. |
Nankai University |
28085275 |
53 |
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker. |
Bristol-Myers Squibb |
28197309 |
40 |
Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors. |
Global Blood Therapeutics |
27994741 |
48 |
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors. |
Bristol-Myers Squibb R & D |
27663548 |
7 |
Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element. |
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) |
27612545 |
37 |
Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors. |
Bristol-Myers Squibb Research & Development |
27455395 |
66 |
Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex. |
Bristol-Myers Squibb R & D |
27015008 |
51 |
Atropisomer Control in Macrocyclic Factor VIIa Inhibitors. |
Bristol-Myers Squibb Research & Development |
26985294 |
114 |
Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation. |
Southern Research |
27073051 |
71 |
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group. |
Bristol-Myers Squibb |
26871940 |
7 |
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program. |
Merck Research Laboratories |
26704266 |
80 |
Novel phenylalanine derived diamides as Factor XIa inhibitors. |
Bristol-Myers Squibb |
26421993 |
44 |
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors. |
Aurigene Discovery Technologies |
26318999 |
70 |
Development of a novel tricyclic class of potent and selective FIXa inhibitors. |
Merck Research Laboratories |
25978966 |
65 |
Development of a novel class of potent and selective FIXa inhibitors. |
Merck Research Laboratories |
26114810 |
8 |
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors. |
Southeast University |
25592713 |
37 |
Pyridine and pyridinone-based factor XIa inhibitors. |
Bristol-Myers Squibb |
26151189 |
56 |
Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors. |
TBA |
26005539 |
23 |
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety. |
Bristol-Myers Squibb |
25990761 |
66 |
Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin. |
Institute For Infection Research |
25937013 |
40 |
Rapid development of two factor IXa inhibitors from hit to lead. |
Merck Research Laboratories |
25911624 |
121 |
Design, synthesis and structure-activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors. |
Shenyang Pharmaceutical University |
25839438 |
19 |
Identification of anthranilamide derivatives as potential factor Xa inhibitors: drug design, synthesis and biological evaluation. |
China Pharmaceutical University |
25881820 |
62 |
Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors. |
Bristol-Myers Squibb R & D |
25728130 |
79 |
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties. |
Bristol-Myers Squibb |
25559742 |
6 |
Design, synthesis and evaluation of isoxazolo[5,4-d]pyrimidin-4(5H)-one derivatives as antithrombotic agents. |
Southeast University |
24951330 |
25 |
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties. |
Bristol-Myers Squibb |
25523211 |
18 |
Identification of potent orally active factor Xa inhibitors based on conjugation strategy and application of predictable fragment recommender system. |
Astellas Pharma |
25453807 |
13 |
A simple, general approach of allosteric coagulation enzyme inhibition through monosulfated hydrophobic scaffolds. |
Virginia Commonwealth University |
25438755 |
9 |
Novel strategy to boost oral anticoagulant activity of blood coagulation enzyme inhibitors based on biotransformation into hydrophilic conjugates. |
Astellas Pharma |
25405503 |
109 |
Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity. |
Bristol-Myers Squibb |
25268757 |
16 |
How aß-D-glucoside side chain enhances binding affinity to thrombin of inhibitors bearing 2-chlorothiophene as P1 moiety: crystallography, fragment deconstruction study, and evaluation of antithrombotic properties. |
Consiglio Nazionale Delle Ricerche |
25179681 |
81 |
Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor. |
Chinese Academy of Sciences |
15125936 |
61 |
Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand. |
Aventis Pharma Deutschland |
24405333 |
69 |
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors. |
Bristol-Myers Squibb |
24461292 |
14 |
Heterocyclic core analogs of a direct thrombin inhibitor. |
Merck Research Laboratories |
24418773 |
61 |
Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia. |
Astrazeneca |
24900796 |
42 |
Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors. |
Bristol-Myers Squibb R & D |
24900621 |
48 |
Discovery of Pyridyl Bis(oxy)dibenzimidamide Derivatives as Selective Matriptase Inhibitors. |
Aurigene Discovery Technologies |
24175584 |
35 |
5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor. |
Sanofi-Aventis R&D |
24102612 |
105 |
Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity. |
University of Bari &Quot;Aldo Moro&Quot |
23845220 |
53 |
Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors. |
Bristol-Myers Squibb R & D |
23927973 |
41 |
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold. |
Bristol-Myers Squibb Research & Development |
23899618 |
9 |
Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug. |
Lg Life Sciences |
23478148 |
10 |
Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
23644213 |
57 |
Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores. |
University of Ljubljana |
23602442 |
28 |
Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility. |
Bristol-Myers Squibb |
23416003 |
52 |
Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors. |
Bristol-Myers Squibb R & D |
23376251 |
32 |
Towards dual antithrombotic compounds - balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism. |
University of Ljubljana |
23379567 |
2 |
Torsion angle preferences in druglike chemical space: a comprehensive guide. |
University of Hamburg |
23294255 |
114 |
Development of new cyclic plasmin inhibitors with excellent potency and selectivity. |
Philipps University Marburg |
21443196 |
38 |
Local structural changes, global data views: graphical substructure-activity relationship trailing. |
Rheinische Friedrich-Wilhelms-Universita£T |
16644215 |
52 |
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors. |
Celera Genomics |
12565961 |
177 |
Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors. |
Berlex Biosciences |
21413808 |
170 |
Synopsis of some recent tactical application of bioisosteres in drug design. |
Bristol-Myers Squibb Pharmaceutical Research and Development |
22788964 |
2 |
Designing allosteric regulators of thrombin. Monosulfated benzofuran dimers selectively interact with Arg173 of exosite 2 to induce inhibition. |
Virginia Commonwealth University |
21732671 |
4 |
Polysulfated xanthones: multipathway development of a new generation of dual anticoagulant/antiplatelet agents. |
Universidade Do Porto (Cequimed-Up) |
23124211 |
22 |
Synthesis and structure-activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: application of weakly basic sulfoximine group as novel S4 binding element. |
Zydus Research Centre |
22770607 |
54 |
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold. |
Virginia Commonwealth University |
22276953 |
63 |
A new strategy for the development of highly potent and selective plasmin inhibitors. |
Philipps University Marburg |
20503967 |
138 |
Factor Xa inhibitors: next-generation antithrombotic agents. |
Bristol-Myers Squibb |
20121198 |
63 |
Studies of benzothiophene template as potent factor IXa (FIXa) inhibitors in thrombosis. |
Trigen |
19861238 |
14 |
Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one. |
Takeda Pharmaceutical |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
18424044 |
32 |
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties. |
Bristol-Myers Squibb Research and Development |
18164204 |
24 |
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors. |
Takeda Pharmaceutical |
18329876 |
53 |
Sulfonamidolactam inhibitors of coagulation factor Xa. |
Bristol-Myers Squibb |
18053726 |
364 |
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
Johnson & Johnson Pharmaceutical Research & Development |
18053714 |
20 |
Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs. |
Glaxosmithkline |
18039572 |
22 |
Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor. |
Daiichi Sankyo |
18077174 |
31 |
Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors. |
Takeda Pharmaceutical |
18054227 |
45 |
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors. |
Bristol-Myers Squibb Research and Development |
18052026 |
97 |
Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties. |
University of Antwerp |
17588746 |
103 |
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa. |
Bristol-Myers Squibb |
16876411 |
17 |
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa. |
Daiichi Asubio Medical Research Laboratories |
16517159 |
45 |
Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. |
Abbott |
15887966 |
58 |
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring. |
Central Pharmaceutical Research Institute |
15837303 |
52 |
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors. |
Berlex Biosciences |
15261287 |
44 |
Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa. |
Central Pharmaceutical Research Institute |
15163182 |
47 |
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors. |
Merck Research Laboratories |
14640539 |
112 |
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1). |
Pharmaceutical Research Institute |
12954057 |
113 |
Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors. |
Pharmacia |
12904065 |
30 |
Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide. |
Lg Life Sciences |
12036356 |
234 |
Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups. |
Berlex Biosciences |
11170646 |
106 |
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa. |
Dupont Pharmaceuticals |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
10956211 |
14 |
GRID/CPCA: a new computational tool to design selective ligands. |
Boehringer Ingelheim Pharma |
10479288 |
141 |
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa. |
Rh£Ne-Poulenc Rorer |
10464012 |
5 |
New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures. |
Rh£Ne-Poulenc Rorer |
10425086 |
83 |
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1. |
Dupont Pharmaceuticals |
9836616 |
92 |
Tetrahydro-isoquinoline-based factor Xa inhibitors. |
Boehringer Mannheim |
9357536 |
47 |
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position. |
Merck Research Laboratories |
1527787 |
11 |
Synthesis and biological activity of ketomethylene pseudopeptide analogues as thrombin inhibitors. |
Thrombosis Research Institute |
15081015 |
91 |
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
14980679 |
30 |
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid. |
Maxim Pharmaceuticals |
12639557 |
7 |
Exploring new non-sugar sulfated molecules as activators of antithrombin. |
Virginia Commonwealth University |
12824035 |
39 |
Polymer-assisted solution-phase (PASP) parallel synthesis of an alpha-ketothiazole library as tissue factor VIIa inhibitors. |
Pharmacia |
11909707 |
69 |
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1. |
Life Science R & D, Lgci |
11858993 |
60 |
Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds. |
Corvas International |
10698459 |
41 |
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand. |
Dupont Pharmaceuticals |
10915051 |
43 |
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position. |
Novartis Horsham Research Centre |
10340604 |
22 |
Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety. |
Research and Development |
| 43 |
S1 heterocyclic thrombin inhibitors |
TBA |
22365562 |
154 |
Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold. |
University of Ljubljana |
22192588 |
9 |
Structure-based library design and the discovery of a potent and selective mast cellß-tryptase inhibitor as an oral therapeutic agent. |
Sanofi Pharmaceuticals |
22047802 |
8 |
The arginine mimickingß-amino acidß³hPhe(3-H2N-CH2) as S1 ligand in cyclotheonamide-basedß-tryptase inhibitors. |
Universit£T Bielefeld |
22044620 |
36 |
Orally active zwitterionic factor Xa inhibitors with long duration of action. |
Daiichi Sankyo |
22041058 |
44 |
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors. |
Bristol-Myers Squibb |
21995444 |
32 |
Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor. |
Astellas Pharma |
21741839 |
83 |
Development of substrate analogue inhibitors for the human airway trypsin-like protease HAT. |
Philipps University Marburg |
21641796 |
30 |
Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors. |
Technical University of Denmark |
21345673 |
33 |
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors. |
Daiichi Sankyo |
21349711 |
19 |
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs. |
Glaxosmithkline |
21349710 |
21 |
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs. |
Glaxosmithkline |
21316975 |
23 |
2-aminomethylphenylamine as a novel scaffold for factor Xa inhibitor. |
Daiichi Sankyo |
21168329 |
47 |
New furin inhibitors based on weakly basic amidinohydrazones. |
Philipps University Marburg |
20650636 |
118 |
Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate. |
F. Hoffmann-La Roche |
20355714 |
26 |
Discovery of a tetrahydropyrimidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor. |
Takeda Pharmaceutical |
20102150 |
35 |
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif. |
Johnson & Johnson Pharmaceutical Research and Development |
20121197 |
148 |
Structure based drug design: development of potent and selective factor IXa (FIXa) inhibitors. |
Trigen |
20100660 |
28 |
Phenyltriazolinones as potent factor Xa inhibitors. |
Bristol-Myers Squibb |
20006499 |
24 |
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs. |
Glaxosmithkline |
20038105 |
50 |
Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics. |
Philipps University Marburg |
19541481 |
57 |
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors. |
Bristol-Myers Squibb |
19200624 |
32 |
Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit. |
F. Hoffmann-La Roche |
19181521 |
69 |
Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor. |
University of Montpellier |
19193009 |
25 |
Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation. |
University of Bari |
| 15 |
Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moiety |
TBA |
| 37 |
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors |
TBA |
| 32 |
Bisbenzamidine isoxazoline derivatives as factor Xa inhibitors |
TBA |
| 27 |
Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3---P4 quaternary lactam dipeptide surrogates |
TBA |
| 25 |
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates |
TBA |
19297158 |
30 |
Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR. |
Millennium Pharmaceuticals |
19297154 |
88 |
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. |
Millennium Pharmaceuticals |
19250826 |
100 |
Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors. |
The Medicines Company (Leipzig) |
19231206 |
20 |
Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action. |
Pfizer |
19128974 |
28 |
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa. |
Daiichi Sankyo |
19046881 |
61 |
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties. |
Bristol-Myers Squibb |
19036586 |
128 |
Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors. |
Curacyte Discovery |
18729445 |
70 |
3,4-Dihydro-2H-1,4-benzoxazine derivatives combining thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activity as a novel class of antithrombotic compounds with dual function. |
University of Ljubljana |
18675545 |
9 |
Stereoselective synthesis and biological evaluation of 3,4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors. |
Daiichi Sankyo |
18674905 |
58 |
Factor VIIa inhibitors: target hopping in the serine protease family using X-ray structure determination. |
Chugai Pharmaceutical |
18667303 |
27 |
Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy. |
Kissei Pharmaceutical |
18644722 |
36 |
Synthesis and evaluation of acylguanidine FXa inhibitors. |
Bristol-Myers Squibb Research and Development |
18550370 |
33 |
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa. |
Bristol-Myers Squibb |
18507371 |
24 |
Discovery of imidazo[1,5-c]imidazol-3-ones: weakly basic, orally active factor Xa inhibitors. |
Takeda Pharmaceutical |
18412326 |
16 |
Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold. |
University of Ljubljana |
9834152 |
29 |
Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade. |
National University of Singapore |
18159923 |
24 |
7-fluoroindazoles as potent and selective inhibitors of factor Xa. |
Johnson & Johnson Pharmaceutical Research and Development |
18054228 |
23 |
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs. |
Glaxosmithkline |
17933529 |
35 |
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17855089 |
25 |
Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17643988 |
92 |
Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications. |
Bristol-Myers Squibb |
17583500 |
31 |
Aminopyrrolidineamide inhibitors of site-1 protease. |
Pfizer |
17566736 |
60 |
Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa. |
Pfizer |
17555959 |
27 |
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors. |
Daiichi Pharmaceutical |
17462889 |
110 |
From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3. |
Curacyte Discovery |
17420122 |
18 |
Selective and dual action orally active inhibitors of thrombin and factor Xa. |
Glaxosmithkline |
17416533 |
39 |
Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors. |
Astellas Pharma |
17064913 |
29 |
Design, synthesis and biological activity of selective and orally available TF/FVIIa complex inhibitors containing non-amidine P1 ligands. |
Astellas Pharma |
16793264 |
13 |
Potent 4-amino-5-azaindole factor VIIa inhibitors. |
Celera Genomics |
16714109 |
40 |
Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles. |
Celera |
16540315 |
23 |
Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors. |
Mochida Pharmaceutical |
16460935 |
39 |
A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s. |
Johnson & Johnson Pharmaceutical Research and Development |
16257204 |
37 |
Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation. |
Celera |
16213711 |
37 |
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16137886 |
88 |
Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization. |
Merck Research Laboratories |
16125385 |
55 |
The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex. |
Pfizer |
15501047 |
75 |
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa. |
Merck |
15456260 |
21 |
Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 binding element. |
Daiichi Pharmaceutical |
15203158 |
84 |
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa. |
Merck |
15203149 |
72 |
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition. |
Aventis Pharma Deutschland |
15149685 |
55 |
Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties. |
University of Ljubljana |
15149641 |
44 |
A novel series of potent and selective small molecule inhibitors of the complement component C1s. |
3-Dimensional Pharmaceuticals |
15125963 |
20 |
Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives. |
Daiichi Pharmaceutical |
15115382 |
16 |
Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator. |
University of Antwerp |
15081014 |
35 |
Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase. |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
15080981 |
72 |
N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors. |
Millennium Pharmaceuticals |
15013007 |
319 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity. |
Millennium Pharmaceuticals |
15013006 |
69 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs. |
Millennium Pharmaceuticals |
15006404 |
56 |
Thrombin inhibitors built on an azaphenylalanine scaffold. |
University of Ljubljana |
14980671 |
78 |
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors. |
Millennium Pharmaceuticals |
14980670 |
107 |
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs. |
Millennium Pharmaceuticals |
14698147 |
60 |
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase. |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
14667222 |
74 |
Analyses of activity for factor Xa inhibitors based on Monte Carlo simulations. |
Yale University |
14552766 |
12 |
Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex. |
Pharmacia |
14552764 |
5 |
A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic factor Xa inhibitors. |
Merck |
12951087 |
23 |
Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics. |
University of Ljubljana |
12824026 |
14 |
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex. |
Pharmacia |
12824021 |
39 |
Heterocyclic thrombin inhibitors. Part 2: quinoxalinone derivatives as novel, potent antithrombotic agents. |
Boehringer Ingelheim Pharma |
12824020 |
31 |
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives. |
Boehringer Ingelheim Pharma |
12729667 |
47 |
Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library. |
Bristol-Myers Squibb |
12723948 |
30 |
Rational design, synthesis, and structure-activity relationships of novel factor Xa inhibitors: (2-substituted-4-amidinophenyl)pyruvic and -propionic acids. |
Ajinomoto |
12668020 |
29 |
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors. |
3-Dimensional Pharmaceuticals |
12668013 |
42 |
Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors. |
Aventis Pharma Deutschland |
12643903 |
81 |
Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors. |
Bristol-Myers Squibb |
12639568 |
52 |
Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state factor Xa inhibitors. |
Millennium Pharmaceuticals |
12639567 |
135 |
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors. |
Millennium Pharmaceuticals |
12617892 |
43 |
Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics. |
University of Ljubljana |
12593666 |
30 |
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor. |
Senju Pharmaceutical |
12593648 |
53 |
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand. |
Aventis Pharmaceuticals |
12565972 |
69 |
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors. |
Millennium Pharmaceuticals |
12565931 |
37 |
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors. |
Bristol-Myers Squibb |
12482444 |
38 |
Design and synthesis of factor Xa inhibitors and their prodrugs. |
Millennium Pharmaceuticals |
12372529 |
21 |
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12113838 |
36 |
Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification. |
Millennium Pharmaceuticals |
12113833 |
183 |
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors. |
Celera |
12113832 |
120 |
2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors. |
Celera |
12039587 |
39 |
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity. |
Aventis Pharmaceuticals |
12039586 |
42 |
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency. |
Aventis Pharmaceuticals |
12039584 |
59 |
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors. |
Millennium Pharmaceuticals |
12039583 |
140 |
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides. |
Millennium Pharmaceuticals |
12031331 |
48 |
Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors. |
Millennium Pharmaceuticals |
11965378 |
78 |
Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity. |
Berlex Biosciences |
11965377 |
66 |
Design and synthesis of aminophenol-based factor Xa inhibitors. |
Berlex Biosciences |
11960487 |
30 |
Structure-based design of novel potent nonpeptide thrombin inhibitors. |
Boehringer Ingelheim Pharma |
11958994 |
31 |
Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors. |
Aventis Pharmaceuticals |
11934589 |
57 |
Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. |
Corvas International |
11934583 |
20 |
Novel bicyclic lactam inhibitors of thrombin: highly potent and selective inhibitors. |
Shire Biochem |
11881991 |
21 |
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors. |
Protherics Molecular Design |
11844691 |
107 |
4-amidinobenzylamine-based inhibitors of urokinase. |
Universitat Jena |
11689072 |
49 |
Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator. |
Axys Pharmaceuticals |
11677132 |
65 |
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors. |
Cor Therapeutics |
11527714 |
66 |
Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors. |
Cor Therapeutics |
11527709 |
19 |
Optimization of a screening lead for factor VIIa/TF. |
Axys Pharmaceuticals |
11495587 |
198 |
Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa. |
Axys Pharmaceuticals |
11459634 |
94 |
Development of potent and selective factor Xa inhibitors. |
Axys Pharmaceuticals |
11266180 |
74 |
The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa. |
Prosthetics Molecular Design |
11266160 |
57 |
Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core. |
Dupont Pharmaceuticals |
11206465 |
13 |
Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors. |
Aventis Pharma |
11087565 |
86 |
Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors. |
Dupont Pharmaceuticals |
11063603 |
53 |
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors. |
Pfizer |
11055344 |
37 |
Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties. |
Corvas International |
10937736 |
35 |
Nonbenzamidine compounds as selective factor Xa inhibitors. |
Aventis Pharmaceuticals |
10866393 |
24 |
Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors. |
Dupont Pharmaceuticals |
10853669 |
102 |
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors. |
Berlex Biosciences |
10853668 |
52 |
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors. |
Berlex Biosciences |
10782677 |
73 |
Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa. |
Corvas International |
10782664 |
42 |
Isoxazolines and isoxazoles as factor Xa inhibitors. |
Dupont Pharmaceuticals |
10698439 |
68 |
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa. |
Rhone-Poulenc Rorer |
10639283 |
135 |
Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors. |
Berlex Biosciences |
10636250 |
20 |
Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines. |
3-Dimensional Pharmaceuticals |
10636232 |
58 |
Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: structures based on the (D)-Arg-Gly-Arg tripeptide sequence. |
Cor Therapeutics |
10617091 |
73 |
Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates. |
Corvas International |
10509929 |
116 |
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors. |
RhôNe-Poulenc Rorer |
10508439 |
4 |
Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations. |
Washington University |
10498211 |
42 |
Novel benzo-fused lactam scaffolds as factor Xa inhibitors. |
Corvas International |
10425087 |
110 |
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2. |
Dupont Pharmaceuticals |
10397495 |
49 |
Thrombin inhibitors based on [5,5] trans-fused indane lactams. |
Glaxo Wellcome Research and Development |
10346927 |
114 |
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors. |
Berlex Biosciences |
10328312 |
27 |
Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa. |
Dupont Pharmaceuticals |
10230630 |
36 |
Thrombin inhibitors based on a propargylglycine template. |
Biotech Research Institute |
10212122 |
35 |
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors. |
Molecumetics |
10206557 |
36 |
Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals. |
Corvas International |
9934495 |
26 |
Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues. |
Corvas International |
9873654 |
37 |
5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor. |
Glaxo Wellcome Research and Development |
9873607 |
21 |
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies. |
Dupont Pharmaceuticals |
9873569 |
16 |
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates. |
Corvas International |
9873520 |
27 |
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors. |
Berlex Biosciences |
9873451 |
19 |
Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors. |
Berlex Biosciences |
9873397 |
37 |
In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors. |
3-Dimensional Pharmaceuticals |
9871674 |
34 |
Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile. |
Dupont Pharmaceuticals |
9871573 |
15 |
Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor. |
Biotech Research Institute |
9871540 |
100 |
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors. |
Dupont Pharmaceuticals |
9822554 |
14 |
1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
9784099 |
84 |
Design of benzamidine-type inhibitors of factor Xa. |
Institut FüR Biochemie |
9733491 |
21 |
Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors. |
Novartis Pharma |
9733480 |
93 |
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa. |
Berlex Biosciences |
9733479 |
18 |
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa. |
Berlex Biosciences |
9484495 |
74 |
Identification and initial structure-activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa. |
Collegeville |
9438022 |
55 |
Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors. |
Dupont Pharmaceuticals |
9371237 |
69 |
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position. |
Merck Research Laboratories |
9171866 |
12 |
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy. |
Merck Research Laboratories |
8917639 |
50 |
Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties. |
Corvas International |
8917638 |
26 |
Potent and selective thrombin inhibitors incorporating the constrained arginine mimic l-3-piperidyl(N-guanidino)alanine at P1. |
Corvas International |
8426361 |
111 |
Highly selective tripeptide thrombin inhibitors. |
Eli Lilly |
8164262 |
38 |
Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. |
Daiichi Pharmaceutical |
8035417 |
23 |
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
7739010 |
118 |
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. |
Thrombosis Research Institute |
28389110 |
3 |
Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity. |
Shenyang Pharmaceutical University |
28460818 |
29 |
Neutral macrocyclic factor VIIa inhibitors. |
Bristol-Myers Squibb Research and Development |
28408226 |
51 |
Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors. |
Mochida Pharmaceutical |
| 18 |
Novel multi-targeted agents for Alzheimer's disease: Synthesis, biological evaluation, and molecular modeling of novel 2-[4-(4-substitutedpiperazin-1-yl)phenyl]benzimidazoles |
Hacettepe University |
12065740 |
8 |
8-Carboxamidocyclazocine: a long-acting, novel benzomorphan. |
University of Rochester |
12065738 |
9 |
Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4,4,4-trifluoro-1-sulfonate (BAY 38-7271) as a potent cannabinoid receptor agonist with neuroprotective properties. |
Bayer |
11714875 |
18 |
Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists. |
Vrije Universiteit |
9802391 |
31 |
The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4. |
Uppsala University |
19895505 |
11 |
Synthesis and pharmacological evaluation of analogs of indole-based cannabimimetic agents. |
UniversitÀ |
9383464 |
20 |
Molecular design and biological activity of potent and selective protein kinase inhibitors related to balanol. |
University of California San Diego |
9195867 |
15 |
Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D. |
University of California Berkeley |
18030989 |
56 |
Picomolar inhibitors as transition-state probes of 5'-methylthioadenosine nucleosidases. |
Albert Einstein College of Medicine |
20383151 |
2 |
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. |
Dana-Farber Cancer Institute |
19648931 |
16 |
Design, synthesis and selection of DNA-encoded small-molecule libraries. |
Praecis Pharmaceuticals |
19305397 |
22 |
Molecular docking and ligand specificity in fragment-based inhibitor discovery. |
University of California San Francisco |
| 28 |
A Thermodynamic Study of the Reactions of Cyclodextrins with Primary and Secondary Aliphatic Alcohols, with D- and L-Phenylalanine, and with L-Phenylalanine Amide |
Nist |
19645448 |
48 |
ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines |
Wyeth Research |
19884013 |
98 |
5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCtheta: optimization of enzymatic and functional activity. |
Wyeth Research |
19162487 |
34 |
Biarylether amide quinolines as liver X receptor agonists. |
Wyeth Research |
19842661 |
140 |
Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases. |
Abbott Laboratories |
19699645 |
12 |
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase. |
Northern Kentucky University |
17184135 |
28 |
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site. |
Rutgers University |
19572549 |
30 |
Identification of inhibitors of checkpoint kinase 1 through template screening. |
The Institute of Cancer Research |
17350258 |
27 |
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids. |
Abbott Laboratories |
12657282 |
13 |
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. |
Abbott Laboratories |