发明公开
- 专利标题: ISOXAZOLECARBOXAMIDE DERIVATIVES
- 专利标题(中): 异唑衍生物作为α1 - 肾上腺素能受体的拮抗剂
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申请号: EP00992436.6申请日: 2000-10-16
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公开(公告)号: EP1226131A2公开(公告)日: 2002-07-31
- 发明人: LEONARDI, Amedeo , MOTTA, Gianni , RIVA, Carlo , POGGESI, Elena
- 申请人: RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a. , RECORDATI S.A.CHEMICAL and PHARMACEUTICAL COMPANY
- 申请人地址: Via M. Civitali, 1 20148 Milano IT
- 专利权人: RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a.,RECORDATI S.A.CHEMICAL and PHARMACEUTICAL COMPANY
- 当前专利权人: RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.p.a.,RECORDATI S.A.CHEMICAL and PHARMACEUTICAL COMPANY
- 当前专利权人地址: Via M. Civitali, 1 20148 Milano IT
- 代理机构: McKelvey, Ian Edward
- 优先权: ITMI992173 19991018
- 国际公布: WO0129015 20010426
- 主分类号: C07D261/18
- IPC分类号: C07D261/18 ; A61K31/42 ; A61P13/08
摘要:
Isoxazolecarboxamide derivatives (I) (R=alkyl, alkoxy, polyfluoroalkoxy, OH or CF3SO2O; each of R1 and R2 independently =H, halogen, polyfluoroalkoxy or alkoxy; R3 = one or more substituents selected from H, halogen, alkyl, alkoxy, NO2, NH2, NHacyl, CN, alkoxycarbonyl, carboxamido; R4 = H, alkyl or aralkyl; an n is 0, 1 or 2) and their N-oxides and pharmaceutically acceptable salts are endowed with adrenergic antagonist activity and high selectivity toward the αla adrenergic receptor with respect to the 5-HTlA receptor. This activity profile suggests the use of these derivatives in the treatment of obstructive syndromes of the lower urinary tract, including BPH, without side effects associated with hypotensive activity being present.
公开/授权文献
- EP1226131B1 ISOXAZOLECARBOXAMIDE DERIVATIVES 公开/授权日:2003-12-17
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