The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28421763 |
5 |
Synthetic Approaches to the New Drugs Approved During 2015. |
Pfizer |
27560285 |
28 |
Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents. |
Institute of Materia Medica |
27396490 |
41 |
Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes. |
East China University of Science and Technology |
27190600 |
48 |
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
Merck Research Laboratories |
27106708 |
130 |
The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors. |
Merck Research Laboratories |
26546218 |
13 |
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. |
Merck Research Laboratories |
26200936 |
39 |
Applications of Fluorine in Medicinal Chemistry. |
Bristol-Myers Squibb Research and Development |
26372650 |
9 |
Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes. |
National Institute of Pharmaceutical Education and Research-Ahmedabad |
26222445 |
5 |
Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials. |
Glaxosmithkline |
25147615 |
108 |
Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes. |
Xuanzhu Pharma |
25164763 |
95 |
Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors. |
Shanghai Institute of Materia Medica |
26005541 |
33 |
Design, Synthesis, and Pharmacological Evaluation of Fusedß-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors. |
Chinese Academy of Sciences |
25815154 |
13 |
Synthesis of New DPP-4 Inhibitors Based on a Novel Tricyclic Scaffold. |
University Park Nottingham |
25838146 |
5 |
Synthesis and potent inhibitory activities of carboxybenzyl-substituted 8-(3-(R)-aminopiperidin-1-yl)-7-(2-chloro/cyanobenzyl)-3-methyl-3,7-dihydro-purine-2,6-diones as dipeptidyl peptidase IV (DPP-IV) inhibitors. |
Southern Medical University |
25596166 |
4 |
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors: use of a carboxylate prodrug to improve bioavailability. |
Sumitomo Dainippon Pharma |
24948564 |
5 |
Structure based virtual screening of MDPI database: discovery of structurally diverse and novel DPP-IV inhibitors. |
Jamia Hamdard |
25457126 |
55 |
(R)-3-amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives as potent inhibitors of dipeptidyl peptidase-4: design, synthesis, biological evaluation, and molecular modeling. |
Chinese Academy of Sciences |
25443644 |
10 |
Thiophenes, polyacetylenes and terpenes from the aerial parts of Eclipata prostrate. |
TBA |
24617858 |
239 |
Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
University of Antwerp |
24099035 |
5 |
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else? |
Chuv-Unil |
24675378 |
33 |
Design, synthesis and biological evaluation of novel aminomethyl-piperidones based DPP-IV inhibitors. |
M.S. University of Baroda |
24660890 |
12 |
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
Merck |
24044354 |
11 |
A general method for making peptide therapeutics resistant to serine protease degradation: application to dipeptidyl peptidase IV substrates. |
Tufts University |
24900744 |
39 |
Integrated Synthesis and Testing of Substituted Xanthine Based DPP4 Inhibitors: Application to Drug Discovery. |
Sanofi-Aventis |
23434133 |
18 |
Discovery of potent dipeptidyl peptidase IV inhibitors through pharmacophore hybridization and hit-to-lead optimization. |
Chinese Academy of Science |
23594271 |
68 |
Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. |
Tufts University Sackler School of Biomedical Sciences |
23416006 |
28 |
Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors. |
Bristol-Myers Squibb Research and Development |
22503246 |
32 |
Long-acting peptidomimetics based DPP-IV inhibitors. |
Zydus Research Centre |
23072865 |
59 |
Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides as potent and selective dipeptidyl peptidase IV inhibitors. |
Toray Industries |
23121075 |
119 |
P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy. |
University of Antwerp |
23025999 |
33 |
Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors. |
Takeda California |
21780776 |
40 |
Remarkable potential of thea-aminophosphonate/phosphinate structural motif in medicinal chemistry. |
Wroclaw University of Technology |
22959556 |
57 |
Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
Mitsubishi Tanabe Pharma |
22938786 |
86 |
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
Dainippon Sumitomo Pharma |
22850208 |
60 |
Dipeptidyl peptidase-4 inhibitor withß-amino amide scaffold: synthesis, SAR and biological evaluation. |
Dong-A Pharm. |
22853995 |
57 |
4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities. |
Tufts University School of Medicine |
22824762 |
39 |
Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group. |
Mitsubishi Tanabe Pharma |
22525314 |
159 |
Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity. |
University of Antwerp (Ua) |
22475866 |
19 |
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization. |
Chinese Academy of Sciences |
22377519 |
23 |
An example of designed multiple ligands spanning protein classes: dual MCH-1R antagonists/DPPIV inhibitors. |
Prosidion |
21764322 |
33 |
Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554. |
Takeda Pharmaceutical |
21218817 |
52 |
Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor. |
Takeda Pharmaceutical |
21106276 |
18 |
The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes. |
Chinese Academy of Sciences |
20718420 |
167 |
Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein. |
National Health Research Institutes |
20058865 |
59 |
Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors. |
Mcgill University |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
19375196 |
22 |
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors. |
Sichuan University |
19217790 |
68 |
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes. |
Matrix Laboratories |
18243000 |
43 |
Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors. |
Taisho Pharmaceutical |
18485703 |
37 |
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors. |
Boehringer Ingelheim Pharma |
18346892 |
42 |
Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors. |
Takeda California |
17962025 |
24 |
Discovery of long-acting N-(cyanomethyl)-N-alkyl-L-prolinamide inhibitors of dipeptidyl peptidase IV. |
Minase Research Institute |
18331795 |
44 |
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors. |
Merck |
18053726 |
364 |
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
Johnson & Johnson Pharmaceutical Research & Development |
18039579 |
59 |
Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group. |
Ono Pharmaceutical |
18201067 |
276 |
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines. |
Merck Research Laboratories |
17869513 |
112 |
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes. |
Merck Research Laboratories |
17331715 |
19 |
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors. |
Korea Research Institute of Chemical Technology |
17822893 |
61 |
(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. |
Pfizer |
17113301 |
83 |
Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: Indoline compounds as potent DPP-IV inhibitors. |
Mitsubishi Pharma |
15357972 |
30 |
Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents. |
Korea Research Institute of Chemical Technology |
14584950 |
132 |
Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases. |
University of Antwerp (Uia) |
9622551 |
14 |
Specific and irreversible cyclopeptide inhibitors of dipeptidyl peptidase IV activity of the T-cell activation antigen CD26. |
Universit£ |
8642568 |
28 |
Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides. |
Boehringer Ingelheim Pharmaceuticals |
12270155 |
56 |
Development of potent and selective dipeptidyl peptidase II inhibitors. |
University of Antwerp (Uia) |
10915049 |
22 |
1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors. |
Novartis Institute For Biomedical Research |
10098663 |
81 |
Nonpeptide small-molecular inhibitors of dipeptidyl peptidase IV: N-phenylphthalimide analogs. |
University of Tokyo |
| 27 |
2-cyanopyrrolidides as potent, stable inhibitors of dipeptidyl peptidase IV |
TBA |
22177783 |
122 |
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. |
Argenta Discovery |
22019046 |
35 |
Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor. |
Sanwa Kagaku Kenkyusho |
21996520 |
149 |
7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site. |
Bristol-Myers Squibb Research and Development |
21996517 |
5 |
Molecular dynamics simulations and MM/GBSA methods to investigate binding mechanisms of aminomethylpyrimidine inhibitors with DPP-IV. |
Graduate University of The Chinese Academy of Sciences |
21865048 |
29 |
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A. |
Dainippon Sumitomo Pharma |
21711053 |
106 |
Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal? |
University of Antwerp (Ua) |
21741847 |
20 |
Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554. |
Takeda Pharmaceutical |
21570283 |
29 |
Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. |
Dong-A Pharm. |
21478015 |
6 |
Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-relateda-glucosidase inhibitors and liver X receptor antagonists. |
The University of Tokyo |
21388136 |
9 |
Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases. |
Tufts University Sackler School of Graduate Biomedical Sciences |
21435872 |
5 |
Aza-annulation on the 16-dehydropregnenolone, via tandem intermolecular aldol process and intramolecular Michael addition. |
Central Drug Research Institute |
24900243 |
44 |
Design, Synthesis, and in Vitro Evaluation of Novel Aminomethyl-pyridines as DPP-4 Inhibitors. |
TBA |
21334204 |
26 |
Discovery of potent dipeptidyl peptidase IV inhibitors derived fromß-aminoamides bearing substituted [1,2,3]-triazolopiperidines for the treatment of type 2 diabetes. |
Shandong University of Traditional Chinese Medicine |
21324688 |
36 |
1-((3S,4S)-4-amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes. |
Pfizer |
21320777 |
375 |
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors. |
Merck Research Laboratories |
21306895 |
46 |
Discovery ofß-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors. |
Korea Research Institute of Chemical Technology |
21186796 |
83 |
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. |
Takeda California |
21163664 |
24 |
Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125. |
Takeda Pharmaceutical |
21074430 |
53 |
Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore. |
Dainippon Sumitomo Pharma |
20800322 |
10 |
Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors. |
East China University of Science and Technology |
20833042 |
51 |
Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors. |
Bristol-Myers Squibb Research and Development |
20684603 |
101 |
Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors. |
Bristol-Myers Squibb |
20598534 |
105 |
Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes. |
Bristol-Myers Squibb |
20488704 |
28 |
Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes. |
Shanghai Hengrui Pharmaceuticals |
20488702 |
21 |
Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes. |
Shanghai Hengrui Pharmaceuticals |
20483603 |
106 |
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV. |
National Health Research Institutes |
20031408 |
9 |
Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors. |
F. Hoffmann-La Roche |
20031405 |
19 |
Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
F. Hoffmann-La Roche |
20000418 |
1 |
Application of the dipeptidyl peptidase IV (DPPIV/CD26) based prodrug approach to different amine-containing drugs. |
Instituto De Qu£Mica M£Dica (Csic) |
19833514 |
104 |
The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements. |
Santhera Pharmaceuticals (Switzerland) |
19576767 |
142 |
From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV. |
Santhera Pharmaceuticals (Switzerland) |
19539471 |
130 |
Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors. |
Merck |
19515557 |
47 |
Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV. |
Santhera Pharmaceuticals (Switzerland) |
19482472 |
30 |
Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors. |
Phenomix |
| 14 |
4-cyanothiazolidides as very potent, stable inhibitors of dipeptidyl peptidase IV |
TBA |
19285862 |
30 |
Piperidinyl-2-phenethylamino inhibitors of DPP-IV for the treatment of type 2 diabetes. |
Pfizer |
19275964 |
64 |
(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. |
Pfizer |
19269819 |
102 |
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors. |
National Health Research Institutes |
19261480 |
113 |
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors. |
National Health Research Institutes |
18996694 |
30 |
Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors. |
Korea Research Institute of Chemical Technology |
18819797 |
24 |
(3R)-3-amino-4-(2,4,5-trifluorophenyl)-N-{4-[6-(2-methoxyethoxy)benzothiazol-2-yl]tetrahydropyran-4-yl}butanamide as a potent dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. |
Toray Industries |
18783201 |
27 |
Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. |
Tufts University |
18650094 |
12 |
Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor. |
Institut De Recerca BiomèDica De Barcelona |
18602260 |
177 |
Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors. |
Ranbaxy Research Laboratories |
18570365 |
29 |
The many roles for fluorine in medicinal chemistry. |
Merck Research Laboratories |
18556199 |
234 |
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads. |
University of Antwerp |
18556198 |
125 |
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors. |
University of Antwerp |
18524582 |
52 |
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design. |
Merck Research Laboratories |
18457385 |
41 |
Recent developments in fragment-based drug discovery. |
Astex Therapeutics |
18243422 |
35 |
Synthesis and biological evaluation of pyrazoline analogues with beta-amino acyl group as dipeptidyl peptidase IV inhibitors. |
Korea Research Institute of Chemical Technology |
18207285 |
26 |
A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors. |
National Health Research Institutes |
18068977 |
3 |
Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin. |
St. John'S University |
18052023 |
30 |
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. |
Boehringer Ingelheim Pharma |
17977724 |
83 |
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors. |
Pfizer |
17958345 |
75 |
Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates. |
University of Antwerp |
17937986 |
39 |
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors. |
Bristol-Myers Squibb Research and Development |
17883259 |
17 |
Anti-Helicobacter pylori and thrombin inhibitory components from Chinese dragon's blood, Dracaena cochinchinensis. |
Chinese Academy of Sciences |
17851076 |
77 |
4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV. |
Merck Research Laboratories |
17827003 |
68 |
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. |
Merck Research Laboratories |
17562364 |
150 |
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
17544668 |
55 |
Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones. |
Lg Life Sciences |
17502141 |
25 |
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors. |
Merck Research Laboratories |
17434732 |
99 |
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate). |
Merck Research Laboratories |
17433672 |
16 |
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin. |
Merck Research Laboratories |
17418568 |
50 |
1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors. |
F. Hoffmann-La Roche |
17317162 |
60 |
[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors. |
Mitsubishi Pharma |
17293118 |
30 |
Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration. |
Minase Research Institute |
17292611 |
21 |
Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV. |
Minase Research Institute |
17194587 |
106 |
3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes. |
National Health Research Institutes |
17174090 |
50 |
Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP. |
Genentech |
17055271 |
18 |
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
Tufts University School of Medicine |
16844373 |
25 |
Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines. |
Laboratory of Medicinal Chemistry University of Antwerp |
16722626 |
94 |
cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization. |
Pfizer |
16321524 |
8 |
In silico fragment-based discovery of DPP-IV S1 pocket binders. |
Santhera Pharmaceuticals |
16168640 |
82 |
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV. |
Glaxosmithkline |
16115768 |
11 |
New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors. |
Pfizer |
16085416 |
45 |
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7. |
Activx Biosciences |
16084722 |
55 |
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors. |
Activx Biosciences |
15927466 |
52 |
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors. |
National Health Research Institutes |
15863294 |
36 |
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors. |
Mitsubishi Pharma |
15380217 |
87 |
Potent and selective proline derived dipeptidyl peptidase IV inhibitors. |
Merck |
15324904 |
52 |
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors. |
Merck |
15324903 |
49 |
Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors. |
Merck |
15293982 |
12 |
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes. |
Merck Research Laboratories |
15139769 |
87 |
Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors. |
University of Antwerp |
15012982 |
129 |
Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
14980678 |
88 |
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
14684294 |
79 |
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors. |
Merck |
12801240 |
105 |
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. |
Novartis Institute For Biomedical Research |
12036346 |
12 |
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. |
TBA |
32008883 |
41 |
Anti-diabetic drugs recent approaches and advancements. |
Mizoram University |
32452679 |
53 |
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
Haisco Pharmaceutical Group |
30694668 |
5 |
Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes. |
East China University of Science and Technology |
27438064 |
29 |
Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure. |
Boehringer Ingelheim Pharma |
27670099 |
43 |
Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors. |
Merck Research Laboratories |
30642693 |
78 |
Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors. |
Guangxi Medical University |
10090787 |
25 |
Structure-activity relationship of diaryl phosphonate esters as potent irreversible dipeptidyl peptidase IV inhibitors. |
University of Antwerp (Uia) |
31812034 |
17 |
Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities. |
Government Arts College |
31336309 |
68 |
Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study. |
Guangxi Medical University |
31301567 |
3 |
Discovery, synthesis, and in vitro evaluation of a novel bioactive peptide for ACE and DPP-IV inhibitory activity. |
University of Mysore |
9873385 |
3 |
A potent dipeptide inhibitor of dipeptidyl peptidase IV. |
Tanabe Seiyaku |
31393718 |
26 |
Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein ?. |
Mcgill University |
30343953 |
27 |
Synthesis, nitric oxide release, and dipeptidyl peptidase-4 inhibition of sitagliptin derivatives as new multifunctional antidiabetic agents. |
Xi'An Jiaotong University |
31683103 |
16 |
Nitrothiadiazolo[3,2-a]pyrimidines as promising antiglycating agents. |
Ural Federal University Named After The First President of Russia B.N. Eltsin |
24457090 |
2 |
Synthesis and biological evaluation of all eight stereoisomers of DPP-IV inhibitor saxagliptin. |
China Pharmaceutical University |
22707871 |
12 |
Kinetic studies of novel inhibitors of endomorphin degrading enzymes. |
TBA |
17458948 |
16 |
Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines. |
Tufts University School of Medicine |
9464355 |
59 |
Novel potent nonpeptide aminopeptidase N inhibitors with a cyclic imide skeleton. |
University of Tokyo |
30056037 |
4 |
Synthesis and evaluation of camphor and cytisine-based cyanopyrrolidines as DPP-IV inhibitors for the treatment of type 2 diabetes mellitus. |
Siberian Branch of The Russian Academy of Sciences |
29609120 |
44 |
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. |
Chinese Academy of Sciences |
29373269 |
28 |
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors. |
Shanghai Jiao Tong University |
29078995 |
27 |
Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation. |
The First Affiliated Hospital of Guangzhou Medical University |
28826083 |
108 |
Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling. |
University of Warwick |
29773502 |
4 |
Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors. |
Chinese Academy of Sciences |
28128944 |
96 |
Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase? (PI3K?) Inhibitors. |
University Park Nottingham |
28579121 |
35 |
Design of potent dipeptidyl peptidase IV (DPP-4) inhibitors by employing a strategy to form a salt bridge with Lys554. |
Takeda Pharmaceutical |
28442252 |
62 |
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome. |
Ranbaxy Laboratories |
21406033 |
4 |
The evaluation of inhibitive effectiveness of the tumour necrosis factor-a converting enzyme selective inhibitors by HPLC. |
Huazhong University of Science and Technology |
28135235 |
71 |
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. |
Novartis Institutes For Biomedical Research |
28259376 |
11 |
Green synthesis, inhibition studies of yeast a-glucosidase and molecular docking of pyrazolylpyridazine amines. |
University of The Punjab |
24003220 |
1 |
Evaluation of cancer dependence and druggability of PRP4 kinase using cellular, biochemical, and structural approaches. |
Sanofi Oncology |
9195869 |
28 |
Molecular recognition at the thrombin active site: structure-based design and synthesis of potent and selective thrombin inhibitors and the X-ray crystal structures of two thrombin-inhibitor complexes. |
Laboratorium FÜR Organische Chemie |
20017516 |
11 |
Development of near-infrared fluorophore (NIRF)-labeled activity-based probes for in vivo imaging of legumain. |
Stanford University |
19450983 |
74 |
Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamides. |
Universite Degli Studi Di Firenze |
17616632 |
11 |
Identification of a Bis-guanylhydrazone [4,4'-Diacetyldiphenylurea-bis(guanylhydrazone); NSC 109555] as a novel chemotype for inhibition of Chk2 kinase. |
Nih |
15582469 |
16 |
Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases. |
University of Alabama At Birmingham |
18760609 |
66 |
Achiral oligoamines as versatile tool for the development of aspartic protease inhibitors. |
Philipps University Marburg |
19630403 |
19 |
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 |
Pfizer |
19409795 |
186 |
Design, parallel synthesis, and crystal structures of biphenyl antithrombotics as selective inhibitors of tissue factor FVIIa complex. Part 1: Exploration of S2 pocket pharmacophores. |
Biocryst Pharmaceuticals |
19422229 |
125 |
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13. |
Novartis |
19328688 |
12 |
Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist. |
Roche R & D Center(China) |
19457666 |
34 |
Design and optimization of renin inhibitors: Orally bioavailable alkyl amines. |
Vitae Pharmaceuticals |
19464884 |
34 |
Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood. |
Wyeth Research |
19406640 |
58 |
Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics. |
Gsk |
19348415 |
52 |
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta). |
Gsk |
19143533 |
44 |
Discovery and Structure-Activity Relationships of Trisubstituted Pyrimidines/Pyridines as Novel Calcium-Sensing Receptor Antagonists. |
Bristol-Myers Squibb |
19256504 |
18 |
Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. |
Astrazeneca |
19193011 |
49 |
Pyrido[2,3-d]pyrimidin-5-ones: A Novel Class of Antiinflammatory Macrophage Colony-Stimulating Factor-1 Receptor Inhibitors (dagger). |
Johnson & Johnson Pharmaceutical |
19056263 |
34 |
Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase. |
Gsk |
19071018 |
72 |
Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. |
Gsk |
16288880 |
41 |
Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling. |
Fujisawa Pharmaceutical |
16844380 |
76 |
Synthesis and structure activity relationships of novel non-peptidic metallo-aminopeptidase inhibitors. |
Enscmu |
9784112 |
87 |
Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors. |
Parke-Davis Pharmaceutical Research |