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Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.

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

Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.

Rempex Pharmaceuticals

(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

Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides as potent and selective dipeptidyl peptidase IV inhibitors.

Toray Industries

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

University Of Antwerp

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

Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.

Sichuan University

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

Matrix Laboratories

Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors.

Merck

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

Merck Research Laboratories

Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.

Merck Research Laboratories

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

(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

Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.

University Of Antwerp (Uia)

Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides.

Boehringer Ingelheim Pharmaceuticals

Development of potent and selective dipeptidyl peptidase II inhibitors.

University Of Antwerp (Uia)

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

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)

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

Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor.

Torrent Pharmaceuticals

The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements.

Santhera Pharmaceuticals (Switzerland)

From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV.

Santhera Pharmaceuticals (Switzerland)

Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.

Merck

Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV.

Santhera Pharmaceuticals (Switzerland)

Piperidinyl-2-phenethylamino inhibitors of DPP-IV for the treatment of type 2 diabetes.

Pfizer

(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

Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.

National Health Research Institutes

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

National Health Research Institutes

Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors.

Korea Research Institute Of Chemical Technology

Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors.

Ranbaxy Research Laboratories

Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.

University Of Antwerp

Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors.

University Of Antwerp

Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.

University Of Antwerp

Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.

Merck Research Laboratories

Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories

Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones.

Lg Life Sciences

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

Merck Research Laboratories

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

Tufts University School Of Medicine

Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines.

Laboratory Of Medicinal Chemistry University Of Antwerp

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

Pfizer

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

Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.

National Health Research Institutes

Potent and selective proline derived dipeptidyl peptidase IV inhibitors.

Merck

Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.

Merck

Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors.

Merck

Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.

Merck Research Laboratories

Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors.

University Of Antwerp

Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories

Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories

4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.

Merck

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

Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor.

Sungkyunkwan University

Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.

Qpex Biopharma

Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.

University Of Warwick

Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.

Ranbaxy Laboratories

Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases.

University Of Anterwerp

4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.

Merck Research Laboratories

Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.

Merck Research Laboratories

(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Merck Research Laboratories

Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.

University Of Antwerp

Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.

National Health Research Institutes

Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.

National Health Research Institutes

Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole.

Merck Research Laboratories

2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.

National Health Research Institutes

Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories

Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories

Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories

Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.

Merck Research Laboratories

(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Merck Research Laboratories

(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Merck Research Laboratories