发明公开
EP0370498A2 Trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane compounds and pharmaceutical use thereof
失效
反式-4-氨基(烷基)-1-吡啶基氨基甲酰基环己烷 - 维生素A和苯并呋喃酮。
- 专利标题: Trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane compounds and pharmaceutical use thereof
- 专利标题(中): 反式-4-氨基(烷基)-1-吡啶基氨基甲酰基环己烷 - 维生素A和苯并呋喃酮。
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申请号: EP89121587.3申请日: 1989-11-22
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公开(公告)号: EP0370498A2公开(公告)日: 1990-05-30
- 发明人: Muro, Tomio , Seki, Toshio , Abe, Masao , Inui, Jun , Sato, Hiroyuki
- 申请人: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
- 申请人地址: 6-9, Hiranomachi 2-chome Chuo-ku Osaka-shi Osaka 541 JP
- 专利权人: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
- 当前专利权人: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
- 当前专利权人地址: 6-9, Hiranomachi 2-chome Chuo-ku Osaka-shi Osaka 541 JP
- 代理机构: von Kreisler, Alek, Dipl.-Chem.
- 优先权: PCT/JP88/01189 19881124
- 主分类号: C07D213/75
- IPC分类号: C07D213/75 ; C07D401/12 ; A61K31/44 ; C07D213/89 ; A61K31/445
摘要:
A trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane compound of the formula:
wherein R¹ and R² are the same or different, and respectively represent hydrogen, C₁₋₁₀ alkyl, C₂₋₅ alkanoyl, formyl, C₁₋₄ alkoxy-carbonyl, amidino, C₃₋₇ cycloalkyl, C₃₋₇ cycloalkylcarbonyl, phenyl, phenylalkyl, benzoyl, naphthoyl, phenylalkoxycarbonyl, benzylidene, pyridylcarbonyl, piperidyl, pyrrolidylidene or piperidylidene which may be optionally substituted on the ring or R¹ and R² together with the adjacent nitrogen atom form 5 to 6-membered cycle which may have oxygen atom, sulfur atom or optionally substituted nitrogen atom in the cycle, or together with the adjacent nitrogen atom form phthalimido, R³ represents hydrogen or C₁₋₄ alkyl, R⁴ represents hydrogen or C₁₋₄ alkyl, R⁵ represents hydrogen, hydroxyl C₁₋₄ alkyl or phenylalkoxy. R⁶ represents hydrogen or C₁₋₄ alkyl, A represents single bond, C₁₋₅ straight chain alkylene, or alkylene which is substituted by C₁₋₄ alkyl, n represents 0 to 1, an optical isomer thereof and a pharmaceutically acceptable acid addition salt thereof.
These compounds possess antihypertensive activity, and coronary, cerebral and kidney circulation-improving activities and are useful as antihypertensive agents and agents for prevention and treatment of circulatory diseases.
wherein R¹ and R² are the same or different, and respectively represent hydrogen, C₁₋₁₀ alkyl, C₂₋₅ alkanoyl, formyl, C₁₋₄ alkoxy-carbonyl, amidino, C₃₋₇ cycloalkyl, C₃₋₇ cycloalkylcarbonyl, phenyl, phenylalkyl, benzoyl, naphthoyl, phenylalkoxycarbonyl, benzylidene, pyridylcarbonyl, piperidyl, pyrrolidylidene or piperidylidene which may be optionally substituted on the ring or R¹ and R² together with the adjacent nitrogen atom form 5 to 6-membered cycle which may have oxygen atom, sulfur atom or optionally substituted nitrogen atom in the cycle, or together with the adjacent nitrogen atom form phthalimido, R³ represents hydrogen or C₁₋₄ alkyl, R⁴ represents hydrogen or C₁₋₄ alkyl, R⁵ represents hydrogen, hydroxyl C₁₋₄ alkyl or phenylalkoxy. R⁶ represents hydrogen or C₁₋₄ alkyl, A represents single bond, C₁₋₅ straight chain alkylene, or alkylene which is substituted by C₁₋₄ alkyl, n represents 0 to 1, an optical isomer thereof and a pharmaceutically acceptable acid addition salt thereof.
These compounds possess antihypertensive activity, and coronary, cerebral and kidney circulation-improving activities and are useful as antihypertensive agents and agents for prevention and treatment of circulatory diseases.
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