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1. 发明公开

EP1070713A1 QUINOLONECARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF 有权
标题翻译： CHINOLONCARBONSAUREDERIVATE ODER DEREN SALZE
公开(公告)号：EP1070713A1
公开(公告)日：2001-01-24
申请号：EP99912111.4
申请日：1999-04-06
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： HAYASHI, Kazuya , KITO, Tokunori , MITSUYAMA, Junichi , YAMAKAWA, Tetsumi , KURODA, Hiroshi , KAWAFUCHI, Hiroyo
IPC分类号： C07D401/04 , A61K31/47
CPC分类号： C07D401/04 , Y02P20/55
摘要： Novel quinolonecarboxylic acid derivatives represented by general formula (1) which have potent antibacterial effects on gram-positive bacteria, in particular, Propionibacterium acnes , wherein R 1 represents hydrogen or a carboxyl-protective group; R 2 represents optionally substituted cycloalkyl; R 3 represents hydrogen, halogeno, optionally substituted alkyl, alkoxy or alkylthio, optionally protected hydroxy or amino, or nitro; R 4 represents optionally substituted alkyl or alkoxy; Z represents halogeno, optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, amino or pyridin-4-yl or pyridin-3-yl optionally having one or more substituents selected from among optionally substituted hydroxy and amino.
摘要翻译：对通式（1）表示的新型喹诺酮羧酸衍生物，其对革兰氏阳性细菌，特别是痤疮丙酸杆菌具有强力的抗菌作用，其中R 1表示氢或羧基保护基; R 2表示任选取代的环烷基; R 3表示氢，卤代，任选取代的烷基，烷氧基或烷硫基，任选保护的羟基或氨基或硝基; R 4表示任选取代的烷基或烷氧基; Z表示卤代，任选取代的烷基，烯基，环烷基，烷氧基，烷硫基，氨基或吡啶-4-基或任选具有一个或多个选自任选取代的羟基和氨基的取代基的吡啶-3-基。

2. 发明公开

EP0882725A1 QUINOLONECARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF 失效
标题翻译： CHINOLIN CARBONSAURE-DERIVATE UND IHRE SALZE
公开(公告)号：EP0882725A1
公开(公告)日：1998-12-09
申请号：EP97902618.4
申请日：1997-02-07
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： TODO, Yozo , HAYASHI, Kazuya , TAKAHATA, Masahiro , WATANABE, Yasuo , NARITA, Hirokazu
IPC分类号： C07D401/04 , A61K31/475 , C07F5/02
CPC分类号： C07D401/04 , C07F5/025
摘要： Quinolonecaboxylic acid derivatives represented by general formula (I) or salts of these. Preferred are compounds wherein R 2 represents optionally substituted cycloalkyl, R 3 represents at least one member selected among hydrogen, halogeno, optionally substituted lower alkyl or alkoxy, and optionally protected hydroxy or amino, R 4 represents hydrogen or optionally substituted lower alkyl, R 5 and R 6 each represents hydrogen, and A represents C-Y (where Y represents halogeno, lower alkyl or alkoxy each optionally substituted by halogeno, or optionally protected hydroxy).
摘要翻译：由通式（I）表示的喹诺酮五羧酸衍生物或它们的盐。优选的是其中R 2表示任选取代的环烷基的化合物，R 3表示选自氢，卤代，任选取代的低级烷基或烷氧基中的至少一个，和任选保护的羟基或氨基，R 4表示氢或任选地取代的低级烷基，R 5和R 6各自表示氢，A表示CY（其中Y表示卤代，低级烷基或烷氧基，各自任选被卤代取代或任意被保护的羟基）。

3. 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.

4. 发明授权

EP0775702B1 NOVEL QUINOLONE- OR NAPHTHYRIDONECARBOXYLIC ACID DERIVATIVE OR SALT THEREOF 失效
标题翻译：新喹诺酮或NAPHTHYRIDONCARBONSÄUREDERIVATE或其盐
公开(公告)号：EP0775702B1
公开(公告)日：2003-07-23
申请号：EP95927967.0
申请日：1995-08-04
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： TODO, Yozo , HAYASHI, Kazuya , TAKAHATA, Masahiro , WATANABE, Yasuo , NARITA, Hirokazu
IPC分类号： C07D401/04 , C07D471/04 , C07F7/22 , A61K31/47 , A61K31/435 , C07D498/08
CPC分类号： C07D401/04 , C07D471/04 , C07F7/2212
摘要： A quinolone- or naphthyridonecarboxylic acid derivative having a skeleton represented by general formula (I) at the 7-position and being useful as an antibacterial or a salt thereof, wherein R3 represents at least one group selected from among hydrogen, halogen, optionally substituted lower alkyl, lower alkoxy, lower alkylthio, nitro, cyano, optionally protected hydroxy and optionally protected amino; R4 represents at least one group selected from among hydrogen, optionally substituted lower alkyl, lower alkylidene and a group which forms a cycloalkane ring together with the carbon atom to which R4 is bonded; and R5 represents hydrogen, optionally substituted lower alkyl or cycloalkyl.

5. 发明公开

EP0775702A1 NOVEL QUINOLONE- OR NAPHTHYRIDONECARBOXYLIC ACID DERIVATIVE OR SALT THEREOF 失效
标题翻译：新型喹诺酮或萘并二羧酸衍生物或其盐
公开(公告)号：EP0775702A1
公开(公告)日：1997-05-28
申请号：EP95927967.0
申请日：1995-08-04
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： TODO, Yozo , HAYASHI, Kazuya , TAKAHATA, Masahiro , WATANABE, Yasuo , NARITA, Hirokazu
IPC分类号： C07D401/04 , C07D471/04 , C07F7/22 , A61K31/47 , A61K31/435
CPC分类号： C07D401/04 , C07D471/04 , C07F7/2212
摘要： This invention relates to a novel quinolone- or naphthyridone-carboxylic acid derivative or its salt useful as an antibacterial agent, said derivative has a substituent represented by the following formula at the 7 position:
wherein preferably R 3 represents at least one member selected from the group consisting of a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl, lower alkoxy or lower alkylthio group, a nitro group, a cyano group, a protected or unprotected hydroxyl group and a protected or unprotected amino group; R 4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a lower alkylidene group and a group forming a cycloalkane ring together with the carbon atom to which R 4 is bonded; and R 5 represents a hydrogen atom or a substituted or unsubstituted lower alkyl or cycloalkyl group.
摘要翻译：本发明涉及可用作抗菌剂的新的喹诺酮 - 或萘啶酮 - 羧酸衍生物或其盐，所述衍生物在7位具有由下式表示的取代基：其中优选地，R 3表示选自组的至少一个成员其由氢原子，卤原子，取代或未取代的低级烷基，低级烷氧基或低级烷硫基，硝基，氰基，保护或未保护的羟基和保护或未保护的氨基组成; R4表示氢原子，取代或未取代的低级烷基，低级亚烷基和与R4键合的碳原子一起形成环烷烃环的基团; R5代表氢原子或取代或未取代的低级烷基或环烷基。

6. 发明授权

EP1767526B1 ARYLAMIDINE DERIVATIVE, SALT THEREOF AND ANTIFUNGAL CONTAINING THESE 有权转让
标题翻译： ARYLAMIDINDERIVAT，盐，以及那些含有杀菌剂
公开(公告)号：EP1767526B1
公开(公告)日：2012-10-24
申请号：EP05765373.5
申请日：2005-06-28
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： HAYASHI, Kazuya , KUNITANI, Kazuto , UEHARA, Sayuri , MORITA, Teiichi
IPC分类号： C07D211/22 , A61K31/445 , A61P31/10
CPC分类号： C07D211/22

7. 发明公开

EP1481966A1 NOVEL ARYLAMIDINE DERIVATIVE OR SALT THEREOF 有权转让
标题翻译：新的芳基脒衍生物或其盐
公开(公告)号：EP1481966A1
公开(公告)日：2004-12-01
申请号：EP03743600.3
申请日：2003-03-04
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： HAYASHI, Kazuya , OJIMA, Katsuji , HORI, Kozo , OKUJO, Hiroyuki , MITSUYAMA, Junichi , KUNITANI, Kazuto , TOHDO, Keisuke
IPC分类号： C07C257/18 , C07D241/08 , A61K31/155 , A61K31/197 , A61K31/198 , A61K31/495 , A61K31/445 , A61K31/551 , A61P31/10
CPC分类号： C07D413/06 , C07C257/18 , C07C259/18 , C07C271/64 , C07C323/62 , C07D207/14 , C07D211/22 , C07D211/26 , C07D211/58 , C07D213/78 , C07D213/85 , C07D241/04 , C07D241/08 , C07D243/08 , C07D245/02 , C07D261/12 , C07D295/088 , C07D295/13 , C07D401/06 , Y02P20/55
摘要： An arylamidine derivative represented by a general formula described below or a salt thereof has an excellent antifungal action and high safety, and it is useful as an antifungal agent with good pharmacokinetics and pharmacodynamic properties:
wherein X represents an unsubstituted or substituted lower alkylene or alkenylene group; G 1 represents an oxygen atom, a sulfur atom, or an imino group; G 2 represents a carbon atom or a nitrogen atom; R a represents at least one group selected from the group consisting of a hydrogen atom, a halogen atom, and unsubstituted or substituted alkyl, cycloalkyl and alkoxy groups; R 1 represents an unprotected or protected or unsubstituted or substituted amidino group; and R 2 represents a substituted amino or substituted cyclic amino group, or the like.
摘要翻译：由下述通式表示的芳基脒衍生物或其盐具有优异的抗真菌作用和高安全性，并且其可用作具有良好药代动力学和药效学性质的抗真菌剂：其中X表示未取代或取代的低级亚烷基或亚烯基 ; G1代表氧原子，硫原子或亚氨基; G2代表碳原子或氮原子; Ra表示至少一个选自氢原子，卤素原子和未取代或取代的烷基，环烷基和烷氧基的基团; R1表示未被保护或被保护或未被取代或被取代的脒基; 并且R2表示取代的氨基或取代的环状氨基等。

8. 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。

9. 发明授权

EP1481966B1 NOVEL ARYLAMIDINE DERIVATIVE OR SALT THEREOF 有权转让
标题翻译：新的芳基脒衍生物或其盐
公开(公告)号：EP1481966B1
公开(公告)日：2011-07-20
申请号：EP03743600.3
申请日：2003-03-04
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： HAYASHI, Kazuya , OJIMA, Katsuji , HORI, Kozo , OKUJO, Noriyuki , MITSUYAMA, Junichi , KUNITANI, Kazuto , TOHDO, Keisuke
IPC分类号： C07C257/18 , C07D241/08 , A61K31/155 , A61K31/197 , A61K31/198 , A61K31/495 , A61K31/445 , A61K31/551 , A61P31/10
CPC分类号： C07D413/06 , C07C257/18 , C07C259/18 , C07C271/64 , C07C323/62 , C07D207/14 , C07D211/22 , C07D211/26 , C07D211/58 , C07D213/78 , C07D213/85 , C07D241/04 , C07D241/08 , C07D243/08 , C07D245/02 , C07D261/12 , C07D295/088 , C07D295/13 , C07D401/06 , Y02P20/55
摘要： An arylamidine derivative represented by the general formula (1) (wherein X means optionally substituted lower alkylene or alkenylene; G1 means oxygen, sulfur, or imino; G2 means carbon or nitrogen; Ra means at least one member selected among hydrogen, halogeno, and optionally substituted alkyl, cycloalkyl, and alkoxy; R1 means optionally protected or substituted amidino; and R2 means substituted amino, substituted cyclic amino, etc.) or a salt of the derivative. The derivative or salt has excellent antifungal activity and is highly safe. It is hence useful as a fungicide with satisfactory behavior in the body.
摘要翻译：由通式（1）表示的芳基脒衍生物（其中X表示任选取代的低级亚烷基或亚烯基; G1表示氧，硫或亚氨基; G2表示碳或氮; Ra表示选自氢，卤素和任选取代的烷基，环烷基和烷氧基; R 1表示任选被保护的或取代的脒基;并且R 2表示取代的氨基，取代的环状氨基等）或该衍生物的盐。该衍生物或盐具有优异的抗真菌活性并且高度安全。因此，它在体内具有令人满意的行为，是一种有效的杀菌剂。

10. 发明公开

EP1767526A1 NOVEL ARYLAMIDINE DERIVATIVE, SALT THEREOF, AND ANTIFUNGAL CONTAINING THESE 有权转让
标题翻译： ARYLAMIDINDERIVAT，SALZ DAVON UND DIEE ENTHALTENDES FUNGIZID
公开(公告)号：EP1767526A1
公开(公告)日：2007-03-28
申请号：EP05765373.5
申请日：2005-06-28
申请人： TOYAMA CHEMICAL CO., LTD.
发明人： HAYASHI, Kazuya , KUNITANI, Kazuto , UEHARA, Sayuri , MORITA, Teiichi
IPC分类号： C07D211/22 , A61K31/445 , A61P31/10
CPC分类号： C07D211/22
摘要： An arylamidine derivative represented by the general formula (wherein R 1 represents optionally protected or substituted amidino; and R 2 and R 3 are the same or different and each represents hydrogen or halogeno) or a salt of the derivative. The derivative and salt have potent activity against fungi including ones having tolerance to azole type drugs and further have high safety and excellent properties in a repeated dose toxicity test. They are hence useful as an excellent antifungal.
摘要翻译：由通式（其中R 1表示任选保护或取代的脒基，R 2和R 3相同或不同，各自表示氢或卤素）表示的芳基脒衍生物或衍生物的盐。衍生物和盐对具有对唑类药物耐受性的真菌具有有效的活性，并且在重复剂量毒性试验中具有高安全性和优异性能。因此它们作为优良的抗真菌剂是有用的。

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