公开(公告)号：US4963587A

公开(公告)日：1990-10-16

申请号：US446106

申请日：1989-12-05

申请人： Takeo Iwakuma ,  Yasuo Sekine ,  Yasuhiko Sasaki ,  Katsuo Ikezawa ,  Akio Odawara

发明人： Takeo Iwakuma ,  Yasuo Sekine ,  Yasuhiko Sasaki ,  Katsuo Ikezawa ,  Akio Odawara

IPC分类号： A61K31/195 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  A61P43/00 ,  C07C303/38 ,  C07C311/20

CPC分类号： C07C311/20 ,  C07C2102/08 ,  Y02P20/55

摘要： There are disclosed are glycine derivative of the formula: ##STR1## (wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a carboxyl group which may be protected, Q represents a lower alkylene group and m represents 0 or 1) or a pharmacologically acceptable salt thereof and a process for preparing the same.

公开(公告)号：US4975460A

公开(公告)日：1990-12-04

申请号：US311854

申请日：1989-02-17

申请人： Takeo Iwakuma ,  Harumichi Kohno ,  Yasuhiko Sasaki ,  Katsuo Ikezawa ,  Akio Odawara

发明人： Takeo Iwakuma ,  Harumichi Kohno ,  Yasuhiko Sasaki ,  Katsuo Ikezawa ,  Akio Odawara

IPC分类号： A61K31/19 ,  A61K31/195 ,  A61K31/22 ,  A61K31/38 ,  A61K31/381 ,  A61P7/02 ,  C07C311/07 ,  C07C311/20 ,  C07D333/34

CPC分类号： C07C311/07 ,  C07C311/20 ,  C07C2102/08

摘要： Novel indanoxyacetic acid derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, a substituted or unsubstituted phenyl group, naphtyl group or a sulfur-containing heterocyclic group, R.sup.2 is hydroxy group or a protected hydroxy group, p is an integer of 2 or 3, and q is an integer of 0 or 1, and a salt thereof are disclosed.Said derivative (I) and a salt thereof are useful as a platelet aggregation-inhibiting agent and an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis, embolism, coronary and cerebral vascular smooth muscl vellication, asthma, and the like.

公开(公告)号：US5190975A

公开(公告)日：1993-03-02

申请号：US897412

申请日：1992-06-12

申请人： Takeo Iwakuma ,  Harumichi Kohno ,  Yasuhiko Sasaki ,  Katsuo Ikezawa ,  Akio Odawara

发明人： Takeo Iwakuma ,  Harumichi Kohno ,  Yasuhiko Sasaki ,  Katsuo Ikezawa ,  Akio Odawara

IPC分类号： C07C233/52 ,  C07C311/20 ,  C07C311/29 ,  C07D257/06 ,  C07D333/34 ,  C07D333/36

CPC分类号： C07D333/36 ,  C07C233/52 ,  C07C311/20 ,  C07C311/29 ,  C07D257/06 ,  C07D333/34 ,  C07C2101/14 ,  C07C2102/08

摘要： Method for the treatment or prophylaxis of thromboses or asthma in warm-blooded animal which comprises administering an effective amount of a compound having the formula: ##STR1## wherein R.sup.1 is phenyl group or phenyl group substituted by a member selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, halogen atom, trifluoromethyl, and nitro, or naphthyl group, and R.sup.2 is hydroxymethyl or a group of the formula: ##STR2## wherein R.sup.3 is hydrogen atom or C.sub.1 -C.sub.5 alkyl and R.sup.4 is C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.6 alkoxycarbonyl-phenyl, carboxy-phenyl, C.sub.1 -C.sub.5 alkyl, or C.sub.1 -C.sub.5 alkyl having a substituent selected from C.sub.1 -C.sub.5 alkoxycarbonyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl-phenyl, carboxy-phenyl, C.sub.2 -C.sub.6 alkoxycarbonyl-(C.sub.3 -C.sub.6) cycloalkyl and carboxy-(C.sub.3 -C.sub.6) cycloalkyl, or a pharmaceutically acceptable salt thereof to said warm blooded animal.

摘要翻译： 用于治疗或预防温血动物血栓形成或哮喘的方法，其包括给予有效量的具有下式的化合物：其中R 1是苯基或被选自C1的成员所取代的苯基 -C 5烷基，C 1 -C 5烷氧基，卤素原子，三氟甲基，硝基或萘基，R 2是羟甲基或下式的基团：其中R 3是氢原子或C 1 -C 5烷基， C 6环烷基，C 2 -C 6烷氧基羰基 - 苯基，羧基 - 苯基，C 1 -C 5烷基或具有选自C 1 -C 5烷氧基羰基，羧基，C 2 -C 6烷氧基羰基 - 苯基，羧基 - 苯基，C 2 -C 6 烷氧基羰基 - （C 3 -C 6）环烷基和羧基 - （C 3 -C 6）环烷基或其药学上可接受的盐。

公开(公告)号：US5030652A

公开(公告)日：1991-07-09

申请号：US271324

申请日：1988-11-15

申请人： Takeo Iwakuma ,  Harumichi Kohno ,  Yasuhiko Sasaki ,  Katsuo Ikezawa ,  Akio Odawara

发明人： Takeo Iwakuma ,  Harumichi Kohno ,  Yasuhiko Sasaki ,  Katsuo Ikezawa ,  Akio Odawara

IPC分类号： C07C233/52 ,  C07C311/20 ,  C07C311/29 ,  C07D257/06 ,  C07D333/34 ,  C07D333/36

CPC分类号： C07D333/36 ,  C07C233/52 ,  C07C311/20 ,  C07C311/29 ,  C07D257/06 ,  C07D333/34 ,  C07C2101/14 ,  C07C2102/08

摘要： Indan derivatives of the formula: ##STR1## wherein R.sup.1 is substituted or unsubstituted phenyl, naphthyl or sulfur-containing heterocyclic group, and R.sup.2 is hydroxy-methyl or a group of the formula: ##STR2## wherein R.sup.3 is hydrogen atom or lower alkyl and R.sup.4 is cycloalkyl, lower alkoxycarbonyl-phenyl, carboxy-phenyl, nitrogen-containing heterocyclic group, lower alkyl, or lower alkyl having a substituent selected from lower alkoxycarbonyl, carboxy, lower alkoxycarbonyl-phenyl, carboxy-phenyl, lower alkoxycarbonyl-cycloalkyl and carboxy-cycloalkyl, or a pharmaceutically acceptable salt thereof, which are useful as a platelet aggregation-inhibiting agent and as an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis or embolism, coronary and cerebral vascular smooth muscle vellication, asthma, and the like, processes for the preparation thereof, and pharmaceutical composition containing said compound as an active ingredient.

公开(公告)号：US4579854A

公开(公告)日：1986-04-01

申请号：US684505

申请日：1984-12-21

申请人： Takeo Iwakuma ,  Akira Tsunashima ,  Katsuo Ikezawa ,  Osasi Takaiti

发明人： Takeo Iwakuma ,  Akira Tsunashima ,  Katsuo Ikezawa ,  Osasi Takaiti

IPC分类号： A61K31/47 ,  A61P11/08 ,  A61P25/02 ,  C07D207/48 ,  C07D215/26 ,  C07D215/32 ,  C07D215/60 ,  C07D215/22

CPC分类号： C07D215/26 ,  C07D207/48 ,  C07D215/60 ,  Y02P20/55

摘要： A novel carbostyril derivative of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, and a process for preparing same. The compound (I) shows potent bronchodilating activity and is useful as a bronchodilator.

摘要翻译： 一种新型的喹诺酮衍生物及其制备方法，其具有下式：其中R 1，R 2， 化合物（I）显示有效的支气管扩张活性，可用作支气管扩张剂。

公开(公告)号：USRE33024E

公开(公告)日：1989-08-15

申请号：US071741

申请日：1987-07-09

申请人： Takeo Iwakuma ,  Akira Tsunashima ,  Katsuo Ikezawa ,  Osasi Takaiti

发明人： Takeo Iwakuma ,  Akira Tsunashima ,  Katsuo Ikezawa ,  Osasi Takaiti

IPC分类号： A61K31/47 ,  A61P11/08 ,  A61P25/02 ,  C07D207/48 ,  C07D215/26 ,  C07D215/32 ,  C07D215/60

CPC分类号： C07D215/26 ,  C07D207/48 ,  C07D215/60 ,  Y02P20/55

摘要： A novel carbostyril derivative of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, and a process for preparing same. The compound (I) shows potent bronchodilating activity and is useful as a bronchodilator.

公开(公告)号：US5047555A

公开(公告)日：1991-09-10

申请号：US445059

申请日：1989-12-04

申请人： Hirozumi Inoue ,  Kei Tsuzurahara ,  Katsuo Ikezawa ,  Tomofumi Uchida

发明人： Hirozumi Inoue ,  Kei Tsuzurahara ,  Katsuo Ikezawa ,  Tomofumi Uchida

IPC分类号： C07C233/25 ,  C07C233/27 ,  C07C235/38 ,  C07D207/32 ,  C07D207/337 ,  C07D209/18 ,  C07D209/42 ,  C07D333/24 ,  C07D333/38 ,  C07D333/70

CPC分类号： C07D207/337 ,  C07C233/25 ,  C07C233/27 ,  C07C235/38 ,  C07D209/18 ,  C07D209/42 ,  C07D333/24 ,  C07D333/38 ,  C07D333/70

摘要： There are disclosed a 4-aminophenol derivative of the formula: ##STR1## (wherein R.sup.1 and R.sup.2 each represent a lower alkyl group, Y represents a single bonding arm, a lower alkylene group or a lower alkenylene group, R.sup.3 represents a thienyl group or pyrrolyl group which may be also substituted with a lower alkyl group; benzothienyl group, indolyl group; or a phenol group which is substituted with 1 to 2 groups selected from a lower alkoxy group and a lower alkanoyloxy group; or Y-R.sup.3 represents integrally an alkyl group with 6 to 9 carbon atoms; or a hydrocarbon group with 5 to 14 carbon atoms having 2 or 3 double bonds) or a pharmacologically acceptable salt thereof, and processes for preparing the same.

公开(公告)号：US06214996B1

公开(公告)日：2001-04-10

申请号：US09201820

申请日：1998-12-01

申请人： Tatsuzo Ukita ,  Katsuo Ikezawa ,  Shinsuke Yamagata

发明人： Tatsuzo Ukita ,  Katsuo Ikezawa ,  Shinsuke Yamagata

IPC分类号： C07D29500

CPC分类号： C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D417/04 ,  C07D471/04 ,  C07F7/1804

摘要： Naphthalene derivatives of the formula [I]: wherein R1 and R2 are the same or different and are each H, protected or unprotected OH, one of R3 and R4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R5 and R6 are, the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.

摘要翻译： 式[I]的萘衍生物：其中R 1和R 2相同或不同，各自为H，被保护或未被保护的OH，R 3和R 4中的一个被保护或未被保护的羟甲基，另一个是H，低级烷基或被保护的 或未受保护的羟甲基，R5和R6各自为H，取代或未取代的低级烷基，取代或未取代的苯基或被保护或未被保护的NH 2，或两者与相邻的N一起形成取代或未取代的杂环基， 这些化合物显示优异的支气管收缩抑制活性，因此可用于预防或治疗哮喘。

公开(公告)号：US5342941A

公开(公告)日：1994-08-30

申请号：US19885

申请日：1993-02-19

申请人： Tameo Iwasaki ,  Kazuhiko Kondo ,  Katsuo Ikezawa ,  Hideo Kikkawa ,  Shinsuke Yamagata

发明人： Tameo Iwasaki ,  Kazuhiko Kondo ,  Katsuo Ikezawa ,  Hideo Kikkawa ,  Shinsuke Yamagata

IPC分类号： A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4425 ,  A61K31/443 ,  A61P11/00 ,  A61P11/08 ,  C07C45/63 ,  C07C59/13 ,  C07C59/84 ,  C07C69/00 ,  C07C69/738 ,  C07D20060101 ,  C07D213/30 ,  C07D213/55 ,  C07D213/61 ,  C07D213/63 ,  C07D213/64 ,  C07D213/89 ,  C07D237/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D413/06

CPC分类号： C07D213/30 ,  C07C45/63 ,  C07C69/738 ,  C07D213/61 ,  C07D213/64 ,  C07D213/89 ,  C07D237/14 ,  C07D405/04 ,  C07D405/06 ,  C07D413/06

摘要： Naphthalene derivative of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen atom, hydroxy group, cyclo-lower alkyloxy group, substituted or unsubstituted lower alkoxy group, or both combine each other to form lower alkylenedioxy group, R.sup.3 is substituted or unsubstituted nitrogen-containing 6-membered heterocyclic group, and groups of the formulae: --OR.sup.4 and --OR.sup.5 are the same or different and are protected or unprotected hydroxy group, processes for preparing thereof, and synthetic intermediates therefor, these compounds have excellent bronchodilating activity, and are useful in the prophylaxis and treatment of asthma.

摘要翻译： 式[I]的萘衍生物：其中R 1和R 2相同或不同，为氢原子，羟基，环低级烷氧基，取代或未取代的低级烷氧基或两者相互结合 形成低级亚烷基二氧基，R 3为取代或未取代的含氮6元杂环基，式-OR4和-OR5基团相同或不同，为保护或未保护的羟基，其制备方法和 合成中间体，这些化合物具有优异的支气管扩张活性，可用于预防和治疗哮喘。

公开(公告)号：US06005106A

公开(公告)日：1999-12-21

申请号：US663991

申请日：1996-06-14

申请人： Tatsuzo Ukita ,  Katsuo Ikezawa ,  Shinsuke Yamagata

发明人： Tatsuzo Ukita ,  Katsuo Ikezawa ,  Shinsuke Yamagata

IPC分类号： C07D213/38 ,  C07D213/75 ,  C07D401/04 ,  C07D401/14 ,  C07D407/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D521/00 ,  C07C15/00 ,  C07D237/30 ,  C07D237/00 ,  A61K31/44

CPC分类号： C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D417/04 ,  C07D471/04 ,  C07F7/1856

摘要： Naphthalene derivatives of the formula [I]: wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.

摘要翻译： 式[I]的萘衍生物：其中R 1和R 2相同或不同，各自为H，被保护或未被保护的OH，R 3和R 4中的一个被保护或未被保护的羟甲基，另一个是H，低级烷基或被保护的 或未被保护的羟甲基，R 5和R 6相同或不同，各自为H，取代或未取代的低级烷基，取代或未取代的苯基或被保护或未被保护的NH 2，或两者与相邻的N一起形成取代或未取代的杂环基， 其药学上可接受的盐，这些化合物显示优异的支气管收缩抑制活性，因此可用于预防或治疗哮喘。