PMID
Data
Article Title
Organization
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.

Merck Research Laboratories
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
(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
Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP).

University of Antwerp
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.

Merck
Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.

Chinese Academy of Sciences
Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: profile of clinical candidate (2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine (23).

Merck Research Laboratories
Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold.

University of Antwerp (Ua)
Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.

Tufts University Sackler School of Biomedical Sciences
P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy.

University of Antwerp
Virtual screening and computational optimization for the discovery of covalent prolyl oligopeptidase inhibitors with activity in human cells.

Mcgill University
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.

Dainippon Sumitomo Pharma
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)
Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.

National Health Research Institutes
Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.

Mcgill University
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes.

Matrix Laboratories
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.

Merck Research Laboratories
(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
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.

Argenta Discovery
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
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
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
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
(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
Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.

Phenomix
(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
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.

National Health Research Institutes
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.

Merck Research Laboratories
Development of Long-Acting Dipeptidyl Peptidase-4 Inhibitors: Structural Evolution and Long-Acting Determinants.

Sichuan Normal University
Licochalcone A Derivatives as Selective Dipeptidyl Peptidase 4 Inhibitors with Anti-Inflammatory Effects.

Shanghai University of Traditional Chinese Medicine
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
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
Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.

Genentech
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.

Tufts University School of Medicine
cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization.

Pfizer
Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.

Mcgill University
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV.

Glaxosmithkline
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.

Activx Biosciences
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.

Activx Biosciences
Boron-Containing heterocycles as promising pharmacological agents.

Long Island University
Potent and selective proline derived dipeptidyl peptidase IV inhibitors.

Merck
1H-[1, 2, 3]triazolo[4, 5-h] quinazoline compounds acting as protein kinase inhibitors

Chengdu Cynogen Bio-Pharmaceutical Technology
MODULATORS OF THE INTEGRATED STRESS PATHWAY

Calico Life Sciences
N-SUBSTITUTED INDOLE DERIVATIVES AS SEROTONERGIC AGENTS USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Mindset Pharma
Heterocyclic sulfonamide derivatives and pharmaceutical uses thereof

Metrion Biosciences
PREPARATION OF PHENETHYLAMINES AND CATHINONES AND STEREOISOMERS THEREOF AND PRECURSORS THEREOF

Transcend Therapeutics
THIOPHENE COMPOUND AND APPLICATION THEREOF

Medshine Discovery
FLUORINATED QUINOLINE, QUINOXALINE AND BENZO[B][1,4]OXAZINE DERIVATIVES AS DIHYDROOROTATE DEHYDROGENASE (DHODH) INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNE AND INFLAMMATORY DISEASES

Janssen Biotech, Inc.
Alkynyl(hetero)aromatic compound for inhibiting protein kinase activity

Shenzhen Targetrx
2-AMINOQUINAZOLINES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF

Merck Sharp & Dohme
Agent enhancing antitumor effect using pyrazolo[3,4-d]pyrimidine compound

Taiho Pharmaceutical
Antibacterial agents: arylalkylcarboxamido phloroglucinols

The State University of New Jersey
Kinase inhibitor compounds and compositions and methods of use

Icahn School of Medicine At Mount Sinai
Amido spirocyclic amide and sulfonamide derivatives

Valo Health
Small molecule inhibitors of the JAK family of kinases

Janssen Pharmaceutica
Heterocyclic kinase inhibitors

Bristol-Myers Squibb
Deazaflavin Inhibitors of Tyrosyl-DNA Phosphodiesterase 2 (TDP2) Specific for the Human Enzyme and Active against Cellular TDP2.

National Institutes of Health
Spiro-oxindole MDM2 antagonists

University of Michigan