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1. 发明授权

EP1031569B1 SALT OF A 7-ISOINDOLINEQUINOLONECARBOXYLIC ACID DERIVATIVE, MONOHYDRATE THEREOF AND COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENT 有权
标题翻译： SALT 7-ISOINDOLINCHINOLONCARBONSÄURE衍生物，ITS MONOHYDRAT和组合物THESE作为活性成分的含
公开(公告)号：EP1031569B1
公开(公告)日：2010-03-17
申请号：EP98950405.5
申请日：1998-10-27
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： YAMADA, Minoru , HAMAMOTO, Shoichi , HAYASHI, Kazuya , TAKAOKA, Kazuko , MATSUKURA, Hiroko , YOTSUJI, Minako , YONEZAWA, Kenji , OJIMA, Katsuji , TAKAMATSU, Tamotsu , TAYA, Kyoko , YAMAMOTO, Hirohiko , KIYOTO, Taro , KOTSUBO, Hironori
IPC分类号： C07D401/04 , A61K31/47
CPC分类号： C07D401/04 , A61K31/4709 , C07C217/48 , C07D209/44 , C07D215/56 , C07F5/025 , Y02P20/55
摘要： Processes for producing 7-isoindolinequinolonecarboxylic derivatives useful as antibacterials and represented by general formula (1) and intermediates therefor; salts of 7-isoindolinequinolonecarboxylic derivatives represented by formula (1) and hydrates thereof; and compositions containing the same as the active ingredient: (1) wherein R1 represents hydrogen or a carboxyl-protecting group; R2 represents cycloalkyl etc.; R3 represents at least one member selected among hydrogen, halogen, and the like; R4 represents at least one member selected among hydrogen, optionally substituted alkyl, and the like; R5 represents hydrogen, optionally substituted alkyl, etc.; R6 represents hydrogen etc.; and A represents CH or C-R7, wherein R7 represents alkoxy etc.

2. 发明公开

EP1031569A1 PROCESSES FOR PRODUCING 7-ISOINDOLINEQUINOLONECARBOXYLIC DERIVATIVES AND INTERMEDIATES THEREFOR, SALTS OF 7-ISOINDOLINEQUINOLONECARBOXYLIC ACIDS, HYDRATES THEREOF, AND COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENT 有权
标题翻译： SALT 7-ISOINDOLINCHINOLONCARBONSÄURE衍生物，ITS MONOHYDRAT和组合物THESE作为活性成分的含
公开(公告)号：EP1031569A1
公开(公告)日：2000-08-30
申请号：EP98950405.5
申请日：1998-10-27
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： YAMADA, Minoru , HAMAMOTO, Shoichi , HAYASHI, Kazuya , TAKAOKA, Kazuko , MATSUKURA, Hiroko , YOTSUJI, Minako , YONEZAWA, Kenji , OJIMA, Katsuji , TAKAMATSU, Tamotsu , TAYA, Kyoko , YAMAMOTO, Hirohiko , KIYOTO, Taro , KOTSUBO, Hironori
IPC分类号： C07D401/04 , C07D209/44 , C07D215/32 , C07C217/48 , C07C311/04 , C07C311/17 , C07F5/02 , A61K31/47 , B01J23/44 , B01J31/24
CPC分类号： C07D401/04 , A61K31/4709 , C07C217/48 , C07D209/44 , C07D215/56 , C07F5/025 , Y02P20/55
摘要： This invention relates to processes for producing a 7-isoindoline-quinolonecarboxylic acid derivative represented by the general formula [1] which is useful as an antibacterial agent, and an intermediate thereof:
wherein R 1 represents a hydrogen atom or a carboxyl-protecting group; R 2 represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl or heterocyclic group; R 3 represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl, alkoxy or alkylthio groups, nitro group, cyano group, acyl groups, protected or unprotected hydroxyl groups and protected or unprotected or substituted or unsubstituted amino groups; R 4 represents at least one group selected from hydrogen atom, halogen atoms, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aralkyl, aryl, alkoxy or alkylthio groups, protected or unprotected hydroxyl or imino groups, protected or unprotected or substituted or unsubstituted amino groups, alkylidene groups, oxo group and groups each forming a cycloalkane group together with the carbon atom to which R 4 bonds; R 5 represents a hydrogen atom, an amino-protecting group, a substituted or unsubstituted alkyl, cycloalkyl, alkylsulfonyl, arylsulfonyl, acyl or aryl group; R 6 represents a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group, a protected or unprotected hydroxyl or amino group or a nitro group; and A represents CH or C-R 7 in which R 7 represents a halogen atom, a substituted or unsubstituted alkyl, alkoxy or alkylthio group or a protected or unprotected hydroxyl group, and to a salt of a 7-isoindoline-quinolonecarboxylic acid represented by the general formula [1], a hydrate thereof and a composition comprising them as an active ingredient.
摘要翻译：本发明涉及用于生产由通式A1U所有这些是作为抗菌剂有用的，并在中间它们代表一个7哚啉喹诺酮羧酸衍生物： worin - [R <1> darstellt一个氢原子或羧基保护基; [R <2>表示一个substituiertem奥德unsubstituiertem烷基，烯基，环烷基，芳基或杂环基; 选自氢原子，卤原子，substituiertem奥德unsubstituiertem烷基，烯基，环烷基，芳基，烷氧基或烷硫基，硝基，氰基，酰基，保护或未被保护的羟基基团和被保护 - [R <3> darstellt至少一个基团或未受保护的或substituiertem奥德unsubstituiertem氨基; 选自氢原子，卤原子，substituiertem奥德unsubstituiertem烷基，烯基，环烷基，芳烷基，芳基，烷氧基或烷硫基，保护或未保护的羟基或亚氨基团，保护或未保护的或substituiertem奥德unsubstituiertem选择的R <4> darstellt至少一个基团氨基，亚烷基，氧代基团和基团各自的碳原子一起形成的环烷烃基团，其中R <4>键; [R <5>代表氢原子，在氨基保护基，一个substituiertem奥德unsubstituiertem烷基，环烷基，烷基磺酰基，芳基磺酰基，酰基或芳基; [R <6>代表氢原子，卤原子，substituiertem奥德unsubstituiertem烷基，烷氧基或烷硫基，保护或未保护的羟基或氨基或硝基; 和A darstellt CH或CR <7>中R <7> darstellt卤原子，substituiertem奥德unsubstituiertem烷基，烷氧基或烷硫基，或保护或未保护的羟基基团，和一个7哚啉喹诺酮羧酸的盐由通式所表示A1U，其水合物和一组合物，包含它们作为对活性成分。

3. 发明公开

EP0805149A1 NOVEL 2,3-DIKETOPIPERAZINE DERIVATIVE OR SALT THEREOF 失效
标题翻译：缺少2,3-DIKETOPIPERAZINDERIVAT ODER SEIN SALZ
公开(公告)号：EP0805149A1
公开(公告)日：1997-11-05
申请号：EP95937174.1
申请日：1995-11-24
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： ONO, Satoshi , YAMAFUJI, Tetsuo , YAMAMOTO, Hirohiko , EGAWA, Hiroyuki , FURUTA, Yousuke , KAGA, Hidetoshi
IPC分类号： C07D241/08 , A61K31/495
CPC分类号： C07D401/06 , A61K38/00 , C07D241/08 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07K5/06139 , Y02P20/55
摘要： The present invention relates to a 2,3-diketopiperazine derivative or a salt thereof, which has inhibitory effect on platelet aggregation because of glycoprotein IIb/IIIa receptor antagonism and hence is useful as a prophylactic and therapeutic agent for diseases associated with platelet aggregation. General formula:
wherein R 1 represents a protected or unprotected amidino group; R 2 represents a hydrogen atom or a carboxyl-protecting group; A represents a substituted or unsubstituted lower alkylene group; B represents -O-, -CONH-, -NHCO- or -SO 2 NH-; Y represents a substituted or unsubstituted lower alkylene group; and the broken line represents a single bond or a double bond.
摘要翻译：本发明涉及由于糖蛋白IIb / IIIa受体拮抗作用而对血小板聚集具有抑制作用的2,3-二酮哌嗪衍生物或其盐，因此可用作血小板聚集相关疾病的预防和治疗剂。通式：其中R 1表示被保护或未被保护的脒基; R 2表示氢原子或羧基保护基; A表示取代或未取代的低级亚烷基; B表示-O - ， - CONH - ， - NHCO-或-SO 2 NH-; Y表示取代或未取代的低级亚烷基; 虚线表示单键或双键。

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