Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b] pyridin-6(7H)-yl)-N, N-dimethylacetamide (BMS-767778)

Journal of Medicinal Chemistry

Volumn 56, Issue 18, 2013, Pages 7343-7357

  Devasthale, Pratik ^a   Wang, Ying ^a   Wang, Wei ^a   Fevig, John ^a   Feng, Jianxin ^a   Wang, Aiying ^a   Harrity, Tom ^a   Egan, Don ^a   Morgan, Nathan ^a   Cap, Michael ^a   Fura, Aberra ^a   Klei, Herbert E ^a   Kish, Kevin ^a   Weigelt, Carolyn ^a   Sun, Lucy ^a   Levesque, Paul ^a   Moulin, Frederic ^a   Li, Yi Xin ^a   Zahler, Robert ^a,c   Kirby, Mark S ^a   Hamann, Lawrence G ^a,b   more..

^a BRISTOL MYERS SQUIBB   (United States)

^b Novartis ^*  (United States)

^c PharmD Consulting LLC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [3 (AMINOMETHYL) 4 (2,4 DICHLOROPHENYL) 2 METHYL 5 OXO 5H PYRROLO[3,4 B]PYRIDIN 6(7H) YL] N,N DIMETHYLACETAMIDE; 5 OXOPYRROLOPYRIDINE; BMS 767778; DIPEPTIDYL PEPTIDASE IV INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; DRUG PENETRATION; DRUG SAFETY; DRUG SELECTIVITY; DRUG SYNTHESIS; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ACETAMIDES; ANIMALS; BICYCLO COMPOUNDS, HETEROCYCLIC; CATALYTIC DOMAIN; DIPEPTIDYL PEPTIDASE 4; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DRUG DESIGN; GLUCOSE TOLERANCE TEST; HUMANS; MALE; MICE; MODELS, MOLECULAR; PYRROLES; SUBSTRATE SPECIFICITY;

EID: 84885002952     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm4008906     Document Type: Article

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