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    NOVEL NITROGENATED HETEROCYCLIC COMPOUND AND SALT THEREOF
    5.
    发明公开
    NOVEL NITROGENATED HETEROCYCLIC COMPOUND AND SALT THEREOF 审中-公开
    在NALROGENIERTE HETEROCYCLISCHE VERBINDUNG UND SALZ DAVON

    公开(公告)号：EP1900732A1

    公开(公告)日：2008-03-19

    申请号：EP06767173.5

    申请日：2006-06-22

    申请人： TOYAMA CHEMICAL CO., LTD. ,  TAISHO PHARMACEUTICAL CO., LTD

    发明人： KIYOTO, Taro ,  TANAKA, Tadashi ,  TSUTSUI, Yasuhiro ,  ANDO, Junichi ,  MOTONO, Mai ,  KAWAGUCHI, Yasuko ,  NOGUCHI, Toshiya ,  USHIKI, Yasunobu ,  USHIYAMA, Fumihito ,  URABE, Hiroki

    IPC分类号： C07D401/06 ,  A61K31/4709 ,  A61K31/496 ,  A61P31/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D491/056

    CPC分类号： C07D405/14 ,  C07D215/227 ,  C07D401/06 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04 ,  C07D519/00

    摘要： A nitrogen-containing heterocyclic compound represented by the general formula: wherein the dashed line represents a single bond or a double bond; R 1 , R 2 , R 3 , R 4 and R 5 independently represent a hydrogen atom, halogen atom, a lower alkyl, aryl, lower alkoxy or monocyclic heterocyclic group which may be substituted or the like; R 6 represents a lower alkyl, aryl, monocyclic heterocyclic, bicyclic heterocyclic or tricyclic heterocyclic group which may be substituted; X 1 represents a lower alkylene group or the like; X 2 represents a lower alkylene, lower alkenylene or lower alkynylene group which may be substituted; X 3 represents an oxygen atom, sulfur atom, a sulfinyl group, sulfonyl group or the like; Y 1 represents a bivalent cyclic group, containing a nitrogen, which may be substituted or the like; and Z 1 represents a nitrogen atom, a carbon atom which may be substituted or the like, or a salt thereof. The compound or salt has a potent antibacterial activity and a high safety, and is therefore useful as an excellent antibacterial agent.

    摘要翻译： 一种由以下通式表示的含氮杂环化合物：其中虚线表示单键或双键; R 1，R 2，R 3，R 4和R 5独立地表示可以被取代的氢原子，卤素原子，低级烷基，芳基，低级烷氧基或单环杂环基等。 R 6表示可以被取代的低级烷基，芳基，单环杂环，双环杂环或三环杂环基; X 1表示低级亚烷基等; X 2表示可以被取代的低级亚烷基，低级亚烯基或低级亚烷基; X 3表示氧原子，硫原子，亚磺酰基，磺酰基等; Y 1表示可以被取代的氮的二价环状基团， Z 1表示氮原子，可被取代的碳原子等，或其盐。 该化合物或盐具有有效的抗菌活性和高安全性，因此可用作优异的抗菌剂。

    PROCESSES FOR PRODUCING 7-ISOINDOLINEQUINOLONECARBOXYLIC DERIVATIVES AND INTERMEDIATES THEREFOR, SALTS OF 7-ISOINDOLINEQUINOLONECARBOXYLIC ACIDS, HYDRATES THEREOF, AND COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENT
    6.
    发明公开
    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
    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。