Title:
【発明の名称】P物質拮抗剤としてのベンジルオキシキヌクリジン
Document Type and Number:
Japanese Patent JPH08511028
Kind Code:
A
Abstract:
PCT No. PCT/JP94/01092 Sec. 371 Date Mar. 3, 1996 Sec. 102(e) Date Mar. 3, 1996 PCT Filed Jul. 5, 1994 PCT Pub. No. WO95/02595 PCT Pub. Date Jan. 26, 1995A compound of chemical formula (I) and its pharmaceutically acceptable salt: (I) wherein X and Y are each hydrogen, halogen, C1-C6alkyl, halosubstituted C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylsulfinyl, C1-C6alkylsulfonyl, or tri(C1-C6alkyl)silyl; Ar1 and Ar2 are each independently aryl or heteroaryl, optionally substituted by halogen; A is -CO- or -(CH2)-; Z-A- is at the 2 or 3 position on the quinuclidine ring; and Z is -OH, C1-C6alkoxy, NR1R2 or the like. Representative compounds are (3S,4R,5S,6S)-5-[3,5-bis(trifluoromethyl)-benzyloxy]-N,N-dimethyl-6-diphenylmethyl-1-azabicyclo[2.2.2]octan-3-carboxamide, and -3-carboxylic acid. These novel benzyloxyquinuclidines are active as substance P receptor antagonists and are thus useful for treating gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis, migraine, urinary incontinence, or angiogenesis in mammals, especially humans.
Inventors:
Kunio Satake
Hiroaki Wakabayashi
Hiroaki Wakabayashi
Application Number:
JP50446195A
Publication Date:
November 19, 1996
Filing Date:
July 05, 1994
Export Citation:
Assignee:
Pfizer Pharmaceutical Co., Ltd.
International Classes:
A61K31/435; A61P1/00; A61P1/08; A61P11/00; A61P25/00; A61P25/04; A61P25/06; A61P29/00; A61P37/08; C07D453/02; (IPC1-7): C07D453/02; A61K31/435
Attorney, Agent or Firm:
Hiroshi Kobayashi