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1. 发明授权

US5948785A Heterocyclic amide compounds and pharmaceutical use of the same 失效
标题翻译：杂环酰胺化合物和药物用途相同
公开(公告)号：US5948785A
公开(公告)日：1999-09-07
申请号：US952319
申请日：1997-10-27
申请人： Fumihiko Akahoshi , Takuya Yoshimura , Masahiro Eda , Atsuyuki Ashimori , Hajime Fukuyama , Masahide Nakajima , Teruaki Imada , Hideki Okunishi , Mizuo Miyazaki
发明人： Fumihiko Akahoshi , Takuya Yoshimura , Masahiro Eda , Atsuyuki Ashimori , Hajime Fukuyama , Masahide Nakajima , Teruaki Imada , Hideki Okunishi , Mizuo Miyazaki
IPC分类号： C07D213/73 , C07D213/75 , C07D239/46 , A61K31/44 , C07D213/64
CPC分类号： C07D213/73 , C07D213/75 , C07D239/47
摘要： Heterocyclic amide compounds of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmacologically acceptable salts thereof, pharmaceutical compositions thereof and pharmaceutical use thereof. The heterocyclic amide compounds and pharmacologically acceptable salts thereof of the present invention have superior inhibitory activity against chymase groups in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be effective for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.
摘要翻译： PCT No.PCT / JP96 / 01171 Sec。 371日期1997年10月27日第 102（e）1997年10月27日PCT PCT 1996年4月26日PCT公布。第WO96 / 33974号公报日期：1996年10月31日式（I）的杂环酰胺化合物，其中每个符号如说明书中所定义，其药理学上可接受的盐，其药物组合物和药物用途。本发明的杂环酰胺化合物及其药理学上可接受的盐对包括人在内的哺乳动物中的食糜酶基具有优异的抑制活性，可以口服或非肠道给药。因此，它们可用作胃促胰酶抑制剂，并且可用于预防和治疗由胃促胰岛素引起的各种疾病，例如由血管紧张素II引起的疾病。

2. 发明授权

US6080738A Heterocyclic amide compounds and medicinal uses thereof 失效
标题翻译：杂环酰胺化合物及其医药用途
公开(公告)号：US6080738A
公开(公告)日：2000-06-27
申请号：US284877
申请日：1999-04-22
申请人： Fumihiko Akahoshi , Atsuyuki Ashimori , Takuya Yoshimura , Masahiro Eda , Hiroshi Sakashita , Masahide Nakajima , Teruaki Imada
发明人： Fumihiko Akahoshi , Atsuyuki Ashimori , Takuya Yoshimura , Masahiro Eda , Hiroshi Sakashita , Masahide Nakajima , Teruaki Imada
IPC分类号： C07D413/12 , A61K31/435 , A61K38/00 , C07K5/078 , A61K31/505 , C07D239/47 , C07D417/12 , C07D498/04 , C07K5/04
CPC分类号： C07K5/06139 , A61K38/00
摘要： A heterocyclic amide compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and a pharmaceutical use thereof. The heterocyclic amide compound and a pharmacologically acceptable salt thereof of the present invention have superior inhibitory action on chymase group in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be used for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.
摘要翻译： PCT No.PCT / JP97 / 03839 Sec。 371日期1999年4月22日 102（e）1999年4月22日PCT 1997年10月22日PCT公布。第WO98 / 18794号公报日期：1998年5月7日一种式（I）的杂环酰胺化合物，其中各符号如说明书中所定义，其药理学上可接受的盐，其药物组合物及其药物用途。本发明的杂环酰胺化合物及其药理学上可接受的盐对包含人的哺乳动物中的胃促胰酶组具有优异的抑制作用，可以口服或肠胃外给药。因此，它们可用作胃促胰酶抑制剂，可用于预防和治疗由胃促胰岛素引起的各种疾病，例如由血管紧张素II引起的疾病。

3. 发明授权

US5635527A Carboxylic acid compound having condensed ring, salt thereof and pharmaceutical use thereof 失效
标题翻译：具有稠环的羧酸化合物及其盐及其药物用途
公开(公告)号：US5635527A
公开(公告)日：1997-06-03
申请号：US591537
申请日：1996-02-06
申请人： Shinichiro Ono , Tomohiro Yoshida , Atsuyuki Ashimori , Keigo Kosaka , Takehiro Okada , Kazuhiro Maeda , Masahiro Eda , Fumio Mori , Yoshihisa Inoue , Hajime Ebisu , Teruaki Imada , Ruriko Ikegawa , Feng Wang , Norifumi Nakamura
发明人： Shinichiro Ono , Tomohiro Yoshida , Atsuyuki Ashimori , Keigo Kosaka , Takehiro Okada , Kazuhiro Maeda , Masahiro Eda , Fumio Mori , Yoshihisa Inoue , Hajime Ebisu , Teruaki Imada , Ruriko Ikegawa , Feng Wang , Norifumi Nakamura
IPC分类号： C07D209/42 , C07D307/84 , C07D307/85 , C07D333/62 , C07D333/68 , C07D491/04 , C07D491/048 , A61K31/715 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/445 , A61K31/55 , C07D401/12 , C07D405/12 , C07D409/12 , C08B37/16
CPC分类号： C07D491/04 , C07D209/42 , C07D307/84 , C07D307/85 , C07D333/62 , C07D333/68
摘要： A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.
摘要翻译： PCT No.PCT / JP95 / 01119 Sec。 371日期1996年2月6日 102（e）日期1996年2月6日PCT归档1995年6月6日PCT公布。 WO95 / 33720 PCT公开日期1995年12月14日一种具有稠环的新型羧酸化合物，其由式（I）表示，其中每个符号如说明书中所定义，其药理学上可接受的盐，其药物组合物及其药物用途。本发明的具有稠环的新型羧酸化合物及其药理学上可接受的盐在包括人的哺乳动物中具有优异的GPIIb / IIIa拮抗作用; 可口服给药; 血液寿命长，毒性低; 并且显示较少的副作用。因此，它们对预防和治疗血栓性疾病等疾病非常有用。

4. 发明授权

US5753670A Carboxylic acid compound having condensed ring, salt thereof and pharmaceutical use thereof 失效
标题翻译：具有稠环的羧酸化合物及其盐及其药物用途
公开(公告)号：US5753670A
公开(公告)日：1998-05-19
申请号：US824541
申请日：1997-03-26
申请人： Shinichiro Ono , Tomohiro Yoshida , Atsuyuki Ashimori , Keigo Kosaka , Takehiro Okada , Kazuhiro Maeda , Masahiro Eda , Fumio Mori , Yoshihisa Inoue , Hajime Ebisu , Teruaki Imada , Ruriko Ikegawa , Feng Wang , Norifumi Nakamura
发明人： Shinichiro Ono , Tomohiro Yoshida , Atsuyuki Ashimori , Keigo Kosaka , Takehiro Okada , Kazuhiro Maeda , Masahiro Eda , Fumio Mori , Yoshihisa Inoue , Hajime Ebisu , Teruaki Imada , Ruriko Ikegawa , Feng Wang , Norifumi Nakamura
IPC分类号： C07D209/42 , C07D307/84 , C07D307/85 , C07D333/62 , C07D333/68 , C07D491/04 , C07D491/048 , A61K31/55 , A61K31/44 , C07D471/02 , C07D498/02
CPC分类号： C07D491/04 , C07D209/42 , C07D307/84 , C07D307/85 , C07D333/62 , C07D333/68
摘要： A novel carboxylic acid compound having a condensed ring; which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.
摘要翻译：具有稠环的新型羧酸化合物; 其由说明书中的式（I）表示，其药理学可接受的盐，其药物组合物和药物用途。本发明的具有稠环的新型羧酸化合物及其药理学上可接受的盐在包括人的哺乳动物中具有优异的GPIIb / IIIa拮抗作用; 可口服给药; 血液寿命长，毒性低; 并且显示较少的副作用。因此，它们对预防和治疗血栓性疾病等疾病非常有用。

5. 发明授权

US4849429A Certain 1,4-dihydro-2,6-dilower-alkyl-4-(mono-substituted pyridyl) useful for treating coronary artery or cerebral artery disease 失效
标题翻译：可用于治疗冠状动脉或脑动脉疾病的某些1,4-二氢-2,6-二氟烷基-4-（单取代吡啶基）
公开(公告)号：US4849429A
公开(公告)日：1989-07-18
申请号：US906268
申请日：1986-09-09
申请人： Chikara Fukaya , Atsuyuki Ashimori , Taizo Ono , Kazumasa Yokoyama
发明人： Chikara Fukaya , Atsuyuki Ashimori , Taizo Ono , Kazumasa Yokoyama
IPC分类号： C07D401/04 , C07D401/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/14
摘要： There is provided a dihydropyridine derivative having the formula ##STR1## wherein R'.sub.1 denotes methyl, chlorine, bromine, fluorine, trifluoromethyl, nitro, cyano or methoxy, R.sub.7 denotes benzyl; and the dihydropyridine links to the 2-, 3-, or 4-position of the pyridine.The compound has an activity as a Ca-antagonist, and is useful for treating vascular disorders such as coronary artery disease, celebral artery disease, hypertension and the like.
摘要翻译：提供具有式“IMAGE”的二氢吡啶衍生物，其中R'1表示甲基，氯，溴，氟，三氟甲基，硝基，氰基或甲氧基，R7表示苄基; 并且二氢吡啶与吡啶的2-，3-或4-位相连。该化合物具有作为Ca拮抗剂的活性，可用于治疗血管疾病如冠状动脉疾病，冠状动脉疾病，高血压等。

6. 发明授权

US4910195A Dihydropyridine derivatives 失效
标题翻译：二氢吡啶衍生物
公开(公告)号：US4910195A
公开(公告)日：1990-03-20
申请号：US113967
申请日：1987-10-29
申请人： Atsuyuki Ashimori , Taizo Ono , Yoshihisa Inoue , Chikara Fukaya , Kazumasa Yokoyama
发明人： Atsuyuki Ashimori , Taizo Ono , Yoshihisa Inoue , Chikara Fukaya , Kazumasa Yokoyama
IPC分类号： C07D211/90 , A61K31/4427 , A61K31/455 , A61P3/00 , A61P7/02 , A61P9/12 , A61P43/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D417/12 , C07D417/14
CPC分类号： C07D401/04 , C07D401/14 , C07D417/12 , C07D417/14
摘要： Dihydropyridine derivatives represented by formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.6, which may be the same or different, each represents an alkyl group, a cycloalkyl group or an alkoxyalkyl group; R.sub.4 and R.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a nitro group, a halogenated alkyl group, an alkylsulfonyl group, a halogenated alkoxy group, an alkylsulfinyl group, an alkyl group, a cycloalkyl group, an alkxoy group, a cyano group, an alkoxycarbonyl group or an alkylthio group (provided that R.sub.4 and R.sub.5 are not hydrogen atoms at the same time); X represents a vinylene group or an azomethine group; A and B are each an alkylene group or an alkenylene group; R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, an aryl group, or a heterocyclic group (provided that R.sub.7 and R.sub.8 may combine with the adjacent nitrogen atom to form a heterocyclic ring), and acid addition salts of the dihydropyridine derivatives of formula (I).
摘要翻译：由式（I）表示的二氢吡啶衍生物：其中R 1，R 2，R 3和R 6可以相同或不同，各自表示烷基，环烷基或烷氧基烷基; R 4和R 5可以相同或不同，各自表示氢原子，卤素原子，硝基，卤代烷基，烷基磺酰基，卤代烷氧基，烷基亚磺酰基，烷基，环烷基基团，烷氧基，氰基，烷氧基羰基或烷硫基（条件是R4和R5不同时为氢原子）; X表示亚乙烯基或偶氮甲碱基; A和B各自为亚烷基或亚烯基; 可以相同或不同的R 7和R 8各自表示氢原子，烷基，烯基，芳烷基，芳基或杂环基（条件是R 7和R 8可以与相邻的氮原子以形成杂环）和式（I）的二氢吡啶衍生物的酸加成盐。

7. 发明授权

US4886819A Dihydropyridine derivatives and pharmaceutical composition thereof 失效
标题翻译：二氢吡啶衍生物及其药物组合物
公开(公告)号：US4886819A
公开(公告)日：1989-12-12
申请号：US87513
申请日：1987-08-20
申请人： Atsuyuki Ashimori , Taizo Ono , Yoshihisa Inoue , Chikara Fukaya , Kazumasa Yokoyama
发明人： Atsuyuki Ashimori , Taizo Ono , Yoshihisa Inoue , Chikara Fukaya , Kazumasa Yokoyama
IPC分类号： C07D211/90 , C07D401/04
CPC分类号： C07D401/04 , C07D211/90
摘要： Dihydropyridine derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, A, B are defined as in the specification and nontoxic acid-addition salts thereof, have an excellent calcium blocking action (Ca-antagonist), and antihypertensive action, a platelet aggregation-inhibiting action, a phosphodiesterase-inhibiting action and the like, and thus are useful as a medicine, such as a coronary vasocilator, a cerebral hyperkinemic, antihypertensive, thrombosis-preventing or -treating agents, phosphodiesterase-inhibitor or the like. Pharmaceutical compositions and methods of use are also disclosed.
摘要翻译：其中R 1，R 2，R 3，R 4，R 5，A，B如说明书中所定义的式（I）的二氢吡啶衍生物及其无毒酸加成盐具有优异的钙阻断作用（Ca-拮抗剂），抗高血压作用，血小板聚集抑制作用，磷酸二酯酶抑制作用等，因此可用作药物，例如冠状动脉血管扩张剂，脑hyperkinemic，抗高血压，预防或预防血栓形成剂，磷酸二酯酶抑制剂等。还公开了药物组合物和使用方法。

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