Discovery of Potent, orally bioavailable phthalazinone bradykinin B1 receptor antagonists

Journal of Medicinal Chemistry

Volumn 54, Issue 20, 2011, Pages 7232-7246

  Biswas, Kaustav ^a   Peterkin, Tanya A N ^a   Bryan, Marian C ^a   Arik, Leyla ^a   Lehto, Sonya G ^a   Sun, Hong ^a   Hsieh, Feng Yin ^a   Xu, Cen ^a   Fremeau, Robert T ^a   Allen, Jennifer R ^a  

^a AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (1 METHYL 4 OXO 1,4 DIHYDROQUINOLIN 3 YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 3 (4 METHYL 1 OXOPHTHALAZIN 2(1H)YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 3 (4 OXO 4H CHROMEN 3 YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 3 (4 OXO 4H THIOCHROMEN 3 YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 3 (4 OXOQUINAZOLIN 3(4H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (1 METHYL 4 OXO 1,4 DIHYDROQUINOLIN 3 YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (1 OXO 4 (TRIFLUOROMETHYL) 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (1 OXO 4 PHENYLPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (4 ETHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (4 ISOPROPYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (4 METHYL 1 OXOPHTHALAZIN 2(1H)YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (4 OXO 4H CHROMEN 3 YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (4 OXO 4H THIOCHROMEN 3 YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (4 OXOQUINAZOLIN 3(4H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (5,8 DIFLUORO 4 METHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (6 CHLORO 4 METHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (7 CHLORO 4 METHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (8 CHLORO 4 METHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (8 FLUORO 4 METHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 4 (8 METHYL 5 OXOPYRIDO[2,3 D]PYRIDAZIN 6(5H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 5 (8 CHLORO 4 METHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 6 (5,8 DIFLUORO 4 METHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 6 (8 CHLORO 4 METHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 6 (8 DIFLUORO 4 METHYL 1 OXOPHTHALAZIN 2(1H) YL) N (6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1YL)BENZAMIDE; 6 (PIPERIDIN 1 YLMETHYL) 1,2,3,4 TETRAHYDRONAPHTHALEN 1 AMINE DIHYDROCHLORIDE; BRADYKININ B1 RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DOSE INCREASE; DRUG MECHANISM; DRUG STRUCTURE; EXPERIMENTAL RABBIT; NONHUMAN; RAT; RECEPTOR BINDING;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; DOGS; HUMANS; PHTHALAZINES; RABBITS; RATS; RECEPTOR, BRADYKININ B1; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 80054902150     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200808v     Document Type: Article

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