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1.发明公开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。
公开(公告)号：EP0370498A2
公开(公告)日：1990-05-30
申请号：EP89121587.3
申请日：1989-11-22
发明人： Muro, Tomio , Seki, Toshio , Abe, Masao , Inui, Jun , Sato, Hiroyuki
IPC分类号： C07D213/75 , C07D401/12 , A61K31/44 , C07D213/89 , A61K31/445
CPC分类号： C07D213/75 , C07D213/82 , C07D213/89 , C07D401/12
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.摘要翻译： 下式的反式-4-氨基（烷基）-1-吡啶基氨基甲酰基环己烷化合物：其中R 1和R 2相同或不同，分别表示氢，C 1-10烷基，C 2-5 烷酰基，甲酰基，C 1-4烷氧基 - 羰基，脒基，C 3-7环烷基，C 3-7环烷基羰基，苯基，苯基烷基，苯甲酰基，萘甲酰基，苯基烷氧基羰基，亚苄基，吡啶基羰基，哌啶基，吡咯烷亚基或哌啶基， 或R 1和R 2与相邻的氮原子一起形成5至6元环，其可在该循环中具有氧原子，硫原子或任选取代的氮原子，或与相邻的氮原子一起形成苯二甲酰亚氨基， R 3表示氢或C 1-4烷基，R 4表示氢或C 1-4烷基，R 5表示氢，羟基C 1-4烷基或苯基烷氧基。 R 6表示氢或C 1-4烷基，A表示单键，C 1-5直链亚烷基或被C 1-4烷基取代的亚烷基，n表示0至1，其旋光异构体和药学上可接受的酸 加成盐。 这些化合物具有抗高血压活性和冠心病，脑和肾循环改善活性，可用作抗高血压药和预防和治疗循环系统疾病的药剂。
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2.发明公开PAF-antagonistic thienotriazolodiazepine compounds and pharmaceutical uses thereof 失效PAF拮抗剂Thienotriazoldiazepin-Verbindungen und deren pharmazeutische Anwendung。
公开(公告)号：EP0268242A1
公开(公告)日：1988-05-25
申请号：EP87116880.3
申请日：1987-11-16
发明人： Tahara, Tetsuya , Moriwaki, Minoru , Abe, Masao , Yuasa, Shuji
IPC分类号： C07D495/14 , A61K31/55
CPC分类号： C07D495/14
摘要： A thienotriazolodiazepine compound of the general formula (I):
wherein each symbol is as defined in the specification and a pharmaceutically acceptable acid addition salt thereof, and pharmaceutical uses thereof.
Said compounds exhibit PAF-antagonistic activity and are useful for the prevention or treatment of various PAF-induced diseases.摘要翻译： 通式（I）的噻吩并三氮杂环素类化合物：
其中各符号如说明书中所定义，及其药学上可接受的酸加成盐及其药学用途。 所述化合物表现出PAF拮抗活性，并且可用于预防或治疗各种PAF诱导的疾病。 -
3.发明授权PAF-antagonistic thienotriazolodiazepine compounds and pharmaceutical uses thereof 失效PAF-拮抗性三烯偶氮染料化合物及其药物用途
公开(公告)号：EP0268242B1
公开(公告)日：1992-03-18
申请号：EP87116880.3
申请日：1987-11-16
发明人： Tahara, Tetsuya , Moriwaki, Minoru , Abe, Masao , Yuasa, Shuji
IPC分类号： C07D495/14 , A61K31/55
CPC分类号： C07D495/14
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4.发明公开Trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane compounds and pharmaceutical use thereof 失效TRANS-4-氨基（烷基）-1-吡啶基甲酰基胆碱化合物及其药物用途
公开(公告)号：EP0370498A3
公开(公告)日：1991-05-08
申请号：EP89121587.3
申请日：1989-11-22
发明人： Muro, Tomio , Seki, Toshio , Abe, Masao , Inui, Jun , Sato, Hiroyuki
IPC分类号： C07D213/75 , C07D401/12 , A61K31/44 , C07D213/89 , A61K31/445
CPC分类号： C07D213/75 , C07D213/82 , C07D213/89 , C07D401/12
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.
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