公开(公告)号：US4992432A

公开(公告)日：1991-02-12

申请号：US478378

申请日：1990-02-12

申请人： Erno Mohacsi ,  Jay P. O'Brien

发明人： Erno Mohacsi ,  Jay P. O'Brien

IPC分类号： C07D281/06

CPC分类号： C07D281/06

摘要： Compounds of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 substituents selected from the group consisting of halogen and lower alkoxy; R.sub.2 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkanoyl, ##STR2## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 ro 4; m is 1 to 2; and pharmaceutically acceptable acid addition salts thereof, with the proviso that when R.sub.1 is 4-methoxyphenyl, R.sub.2 is hydrogen and R.sub.3 and R.sub.4 are methyl; and n is 2, the compound of formula I cannot be in the (-)-cis form,are described. The compounds of formula I are active as calcium channel blockers and accordingly, are useful as agents for treating ischemia.

摘要翻译： 其中R 1是被1至3个选自卤素和低级烷氧基的取代基取代的苯基; R2是氢，低级烷基，低级烷酰基，低级环烷酰基，R3和R4独立地是低级烷基，苯基低级烷基或一起形成哌啶或吡咯烷环; n为2 ro 4; m为1〜2; 其中R 1为4-甲氧基苯基，R 2为氢，R 3和R 4为甲基; 并且n为2，式I化合物不能为（ - ） - 顺式）。 式I化合物作为钙通道阻滞剂是有活性的，因此可用作治疗缺血的药剂。

公开(公告)号：US4912102A

公开(公告)日：1990-03-27

申请号：US286789

申请日：1988-12-22

申请人： Erno Mohacsi ,  Jay P. O'Brien

发明人： Erno Mohacsi ,  Jay P. O'Brien

IPC分类号： C07D281/10 ,  A61K31/55 ,  A61K31/554 ,  A61K31/70 ,  A61K31/7028 ,  A61P3/06 ,  A61P3/14 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D281/08 ,  C07D417/12 ,  C07H9/04 ,  C07H15/26

CPC分类号： C07D417/12 ,  C07D281/08 ,  C07H9/04

摘要： (+)-Cis compounds of the formula ##STR1## wherein R is lower alkyl; R.sub.1 is ##STR2## wherein R.sub.3 is pyridyl, ##STR3## or phenyl unsubstituted or substituted by up to 3 substituents selected from the group consisting of hydroxy, halogen, lower alkoxy, and lower alkanoyloxy;(-)cis enantiomers, and (.+-.)-cis racemates thereof; or pharmaceutically acceptable acid addition salts thereof are described.

公开(公告)号：US4640930A

公开(公告)日：1987-02-03

申请号：US843317

申请日：1986-03-24

申请人： Erno Mohacsi ,  Jay P. O'Brien

发明人： Erno Mohacsi ,  Jay P. O'Brien

IPC分类号： A61K31/395 ,  A61K31/40 ,  A61K31/445 ,  A61P3/00 ,  A61P3/14 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07D281/18 ,  A61K31/55

CPC分类号： C07D281/18

摘要： A compound of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 lower alkoxy groups, or 1 to 3 halogens; R.sub.2 is hydroxy or lower alkanoyloxy; R.sub.3 and R.sub.4 are each independently lower alkyl or together form a pyrrolidine or piperidine ring; and n is 2 to 4, and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I are active as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.

公开(公告)号：US4808580A

公开(公告)日：1989-02-28

申请号：US134282

申请日：1987-12-17

申请人： Erno Mohacsi ,  Jay P. O'Brien

发明人： Erno Mohacsi ,  Jay P. O'Brien

IPC分类号： C07D281/10 ,  A61K31/55 ,  A61K31/554 ,  A61P3/00 ,  A61P3/14 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  C07D281/08 ,  A61K31/33 ,  C07D281/14

CPC分类号： C07D281/08

摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 substituents selected from the group consisting of lower alkoxy and halogen; R.sub.2 is hydroxy, lower alkoxy, lower alkanoyloxy, lower cycloalkylcarbonyloxy; ##STR2## or ##STR3## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 to 4; m is 1 to 2; or pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I have activity as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.

摘要翻译： 下式的化合物：其中R 1是被1至3个选自低级烷氧基和卤素的取代基取代的苯基; R2是羟基，低级烷氧基，低级烷酰氧基，低级环烷基羰氧基; R 3和R 4独立地为低级烷基，苯基低级烷基或一起形成哌啶或吡咯烷环; n为2〜4; m为1〜2; 或其药学上可接受的酸加成盐。 式I的化合物具有作为钙通道阻断剂的活性，因此可用作降低血压的药剂和作为治疗缺血的药剂。

公开(公告)号：US4559403A

公开(公告)日：1985-12-17

申请号：US705262

申请日：1985-02-25

申请人： Hans Bruderer ,  Richard W. Kierstead ,  John G. Mullin, Jr. ,  Keiji Nakamura ,  Mitsuru Tateishi ,  Sidney Teitel ,  Jay P. O'Brien

发明人： Hans Bruderer ,  Richard W. Kierstead ,  John G. Mullin, Jr. ,  Keiji Nakamura ,  Mitsuru Tateishi ,  Sidney Teitel ,  Jay P. O'Brien

IPC分类号： C07D217/20 ,  C07D217/26 ,  C07D241/08 ,  C07D295/205 ,  C07D295/24 ,  C07D401/06 ,  C07D217/16

CPC分类号： C07D295/205 ,  C07D217/20 ,  C07D217/26 ,  C07D241/08 ,  C07D295/24 ,  C07D401/06

摘要： Substituted isoquinolines of the formula ##STR1## wherein R is a lower alkoxy, n is the integer zero or 1, andA is ##STR2## wherein R.sub.1 is phenyl halophenyl, lower-alkylphenyl or lower-alkoxyphenyl, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of cerebral and cardiac ischemias.

摘要翻译： 取代的下式其中R为低级烷氧基的异喹啉，n为整数0或1，A为苯基卤代苯基，低级烷基苯基或低级烷基苯基， 烷氧基苯基及其药学上可接受的酸加成盐。 式I化合物可用于治疗脑和心脏缺血。

公开(公告)号：US4652561A

公开(公告)日：1987-03-24

申请号：US834178

申请日：1986-02-26

申请人： Erno Mohacsi ,  Jay P. O'Brien

发明人： Erno Mohacsi ,  Jay P. O'Brien

IPC分类号： C07D281/10 ,  A61K31/55 ,  A61K31/554 ,  A61P3/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D281/08 ,  C07D281/02

CPC分类号： C07D281/08

摘要： Compounds of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 lower alkoxy groups or 1 to 3 halogens; R.sub.2 is hydroxy, lower alkoxy, lower alkanoyloxy, lower cycloalkylcarbonyloxy; ##STR2## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 to 4; m is 1 to 2; or pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I have activity as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.

摘要翻译： 式Ⅰ的化合物，其中R1是被1〜3个低级烷氧基或1〜3个卤素取代的苯基; R2是羟基，低级烷氧基，低级烷酰氧基，低级环烷基羰氧基; R3和R4独立地是低级烷基，苯基低级烷基或一起形成哌啶或吡咯烷环; n为2〜4; m为1〜2; 或其药学上可接受的酸加成盐。 式I的化合物具有作为钙通道阻断剂的活性，因此可用作降低血压的药剂和作为治疗缺血的药剂。

公开(公告)号：US4544657A

公开(公告)日：1985-10-01

申请号：US496327

申请日：1983-05-19

申请人： Hans Bruderer ,  Richard W. Kierstead ,  John G. Mullin, Jr. ,  Keiji Nakamura ,  Mitsuru Tateishi ,  Teitel Sidney ,  Jay P. O'Brien

发明人： Hans Bruderer ,  Richard W. Kierstead ,  John G. Mullin, Jr. ,  Keiji Nakamura ,  Mitsuru Tateishi ,  Teitel Sidney ,  Jay P. O'Brien

IPC分类号： C07D295/20 ,  A61K31/47 ,  A61K31/472 ,  A61K31/495 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P25/02 ,  C07C233/45 ,  C07D217/18 ,  C07D217/20 ,  C07D217/26 ,  C07D241/04 ,  C07D241/08 ,  C07D295/205 ,  C07D295/22 ,  C07D295/24 ,  C07D401/06

CPC分类号： C07D295/205 ,  C07D217/20 ,  C07D217/26 ,  C07D241/08 ,  C07D295/24 ,  C07D401/06

摘要： Substituted isoquinolines of the formula ##STR1## wherein R is lower alkoxy, n is the integer zero or 1, and A is ##STR2## wherein R.sub.1 is phenyl, halophenyl, lower-alkylphenyl or lower-alkoxyphenyl, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of cerebral and cardiac ischemias.

摘要翻译： 其中R是低级烷氧基，n是整数0或1的取代的异喹啉，其中R 1是苯基，卤代苯基，低级烷基苯基或低级烷氧基苯基， 和其药学上可接受的酸加成盐。 式I化合物可用于治疗脑和心脏缺血。

公开(公告)号：US4959359A

公开(公告)日：1990-09-25

申请号：US418369

申请日：1989-10-06

申请人： Erno Mohacsi ,  Jay P. O'Brien

发明人： Erno Mohacsi ,  Jay P. O'Brien

IPC分类号： C07D281/06

CPC分类号： C07D281/06

摘要： Compounds of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 substituents selected from the group consisting of halogen and lower alkoxy; R.sub.2 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkanoyl, ##STR2## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 to 4; m is 1 to 2; and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I are active as calcium channel blockers and accordingly, are useful as agents for treating ischemia.

摘要翻译： 其中R 1是被1至3个选自卤素和低级烷氧基的取代基取代的苯基; R 2是氢，低级烷基，低级烷酰基，低级环烷酰基，R 3和R 4分别是低级烷基，苯基低级烷基或一起形成哌啶或吡咯烷环; n为2〜4; m为1〜2; 及其药学上可接受的酸加成盐。 式I化合物作为钙通道阻滞剂是有活性的，因此可用作治疗缺血的药剂。