Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[(3-substituted)-1-azetidinyl]ethyl} -2-piperidones. 1. Selective antagonists of the neurokinin-2 receptor

Journal of Medicinal Chemistry

Volumn 45, Issue 24, 2002, Pages 5365-5377

  MacKenzie, A Roderick ^a,b   Marchington, Allan P ^a,c   Middleton, Donald S ^a   Newman, Sandra D ^a   Jones, Barry C ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b PFIZER INC   (United States)

^c MILLENNIUM PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (CYCLOPROPYLMETHYL) 5 (3,4 DICHLOROPHENYL) 5 [2 [3 (1 PIPERAZINYL) 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 (CYCLOPROPYLMETHYL) 5 (3,4 DICHLOROPHENYL) 5 [2 [3 (4 MORPHOLINYL) 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 (CYCLOPROPYLMETHYL) 5 (3,4 DICHLOROPHENYL) 5 [2 [3 [4 (METHYLSULFONYL) 1 PIPERAZINYL] 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 (1 PIPERAZINYL) 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 (2 PHENYL 4 MORPHOLINYL) 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 (3 HYDROXY 1 PIPERIDINYL) 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 (3 HYDROXY 1 PYRROLIDINYL) 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 (3 HYDROXY 8 AZABICYLO[3.2.1]OCT 8 YL) 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 (4 HYDROXY 1 PIPERIDINYL) 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 (4 METHYL 1 PIPERAZINYL) 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 [(2 HYDROXYETHYL)(METHYL)AMINO] 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 [3 (4 THIOMORPHOLINYL)] 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 1 BENZYL 5 (3,4 DICHLOROPHENYL) 5 [2 [3 [4 (METHYLSULFONYL) 1 PIPERANIZYL] 1 AZETIDINYL]ETHYL] 2 PIPERIDONE; 4 [1 [2 [1 (CYCLOPROPYLMETHYL) 3 (3,4 DICHLOROPHENYL) 6 OXOPIPERIDINYL]ETHYL] 3 AZETIDINYL] 1 PIPERAZINE CARBOXAMIDE; 4 [1 [2 [1 (CYCLOPROPYLMETHYL) 3 (3,4 DICHLOROPHENYL) 6 OXOPIPERIDINYL]ETHYL] 3 AZETIDINYL] 1 PIPERAZINE SULFONAMIDE; 4 [1 [2 [1 (CYCLOPROPYLMETHYL) 3 (3,4 DICHLOROPHENYL) 6 OXOPIPERIDINYL]ETHYL] 3 AZETIDINYL] N METHYL 1 PIPERAZINESULFONIDE; 4 [1 [2 [1 (CYCLOPROPYLMETHYL) 3 (3,4 DICHLOROPHENYL) 6 OXOPIPERIDINYL]ETHYL] 3 AZETIDINYL] N,N DIMETHYL 1 PIPERAZINESULFONAMIDE; 4 [1 [2 [1 BENZYL 3 (3,4 DICHLOROPHENYL) 6 OXO 3 PIPERIDINYL]ETHYL] 3 AZETIDINYL] 1,4 THIAZINAN 1 ONE; 4 [1 [2 [1 BENZYL 3 (3,4 DICHLOROPHENYL) 6 OXO 3 PIPERIDINYL]ETHYL] 3 AZETIDINYL] 1,4 THIAZINAN 1,1 DIONE; 4 [1 [2 [1 BENZYL 3 (3,4 DICHLOROPHENYL) 6 OXO 3 PIPERIDINYL]ETHYL] 3 AZETIDYL] 3 MORPHOLINONE; 5 [2 [3 (4 ACETYL 1 PIPERANIZYL) 1 AZATIDINYL]ETHYL] 1 BENZYL 5 (3,4 DICHLOROPHENYL) 2 PIPERIDONE; 5 [2 [3 (4 AMINO 1 PIPERIDINYL) 1 AZETIDINYL]ETHYL] 1 (CYCLOPROPYLMETHYL) 5 (3,4 DICHLOROPHENYL) 2 PIPERIDONE; AMIDE; BENZYL DERIVATIVE; LACTAM; N [1 [1 [2 [1 (CYCLOPROPYLMETHYL) 3 (3,4 DICHLOROPHENYL) 6 OXOPIPERIDINYL]ETHYL] 3 AZETIDINYL] 4 PIPERIDINYL]ACETAMIDE; NEUROKININ 2 RECEPTOR ANTAGONIST; PIPERIDONE DERIVATIVE; SAREDUTANT; UK 224671; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG DESIGN; DRUG IDENTIFICATION; DRUG POTENCY; DRUG STABILITY; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IN VITRO STUDY; LIPOPHILICITY; MASS SPECTROMETRY; NONHUMAN; PROTON NUCLEAR MAGNETIC RESONANCE; PULMONARY ARTERY; RABBIT; STRUCTURE ACTIVITY RELATION; THIN LAYER CHROMATOGRAPHY;

ANIMALS; AZETIDINES; CHO CELLS; CRICETINAE; DRUG STABILITY; HUMANS; MICROSOMES, LIVER; MUSCLE CONTRACTION; MUSCLE, SMOOTH; PIPERAZINES; PIPERIDONES; PULMONARY ARTERY; RABBITS; RADIOLIGAND ASSAY; RECEPTORS, NEUROKININ-2; RECEPTORS, NEUROKININ-3; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0037153202     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0209331     Document Type: Article

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