发明授权
- 专利标题: Benzyloxyquinuclidines as substance P antagonists
- 专利标题(中): 作为P物质拮抗剂的苄氧基亚奎宁
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申请号: US637682申请日: 1996-03-03
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公开(公告)号: US5869499A公开(公告)日: 1999-02-09
- 发明人: Kunio Satake , Hiroaki Wakabayashi
- 申请人: Kunio Satake , Hiroaki Wakabayashi
- 申请人地址: NY New York
- 专利权人: Pfizer Inc
- 当前专利权人: Pfizer Inc
- 当前专利权人地址: NY New York
- 优先权: JPX5-175609 19930715
- 主分类号: A61K31/435
- IPC分类号: A61K31/435 ; A61P1/00 ; A61P1/08 ; A61P11/00 ; A61P25/00 ; A61P25/04 ; A61P25/06 ; A61P29/00 ; A61P37/08 ; C07D453/02 ; A61K31/44 ; C07D401/00
摘要:
A compound of chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein X and Y are each hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, halosubstituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, or tri(C.sub.1 -C.sub.6 alkyl)silyl; Ar.sup.1 and Ar.sup.2 are each independently aryl or heteroaryl, optionally substituted by halogen; A is --CO-- or -(CH.sub.2)-; Z-A- is at the 2 or 3 position on the quinuclidine ring; and Z is --OH, C.sub.1 -C.sub.6 alkoxy, NR.sup.1 R.sup.2 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.
公开/授权文献
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