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    NOVEL CRYSTAL OF 3-Ý5-Ý4-(CYCLOPENTYLOXY)-2- HYDROXYBENZOYL¨-2-Ý(3-HYDROXY-1,2-BENZISOXAZOL-6- YL)METHOXY¨PHENYL¨PROPIONIC ACID
    1.
    发明公开
    NOVEL CRYSTAL OF 3-Ý5-Ý4-(CYCLOPENTYLOXY)-2- HYDROXYBENZOYL¨-2-Ý(3-HYDROXY-1,2-BENZISOXAZOL-6- YL)METHOXY¨PHENYL¨PROPIONIC ACID 有权
    NEUER KRISTALL VON 3- [5- [4-（环己基）-2-羟基苯甲酰基] -2 - [（3-羟基-1,2-苯并咪唑-6-基）甲氧基]苯基]丙酸

    公开(公告)号：EP2022788A1

    公开(公告)日：2009-02-11

    申请号：EP07744104.6

    申请日：2007-05-25

    申请人： TOYAMA CHEMICAL CO., LTD.

    发明人： YONEZAWA, Kenji ,  KOTSUBO, Hironori ,  BABA, Yasutaka ,  TADA, Yukie

    IPC分类号： C07D261/12

    CPC分类号： C07D261/20

    摘要： The crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.0, 16.0, 23.3, 23.7 and 26.3°and the crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.6, 23.1, 24.7, 25.6 and 26.0° on 2θ of diffraction angle in a powder X-ray diffraction pattern have a small specific volume, are hard to be charged with electricity, are easily handled and are useful for an active pharmaceutical ingredient of excellent anti-rheumatic agents.

    摘要翻译： 3- {5- [4-（环戊氧基）-2-羟基苯甲酰基] -2 - [（3-羟基-1,2-苯并异恶唑-6-基）甲氧基]苯基}丙酸的晶体在 14.0,16.0,23.3,23.7和26.3°，3- {5- [4-（环戊氧基）-2-羟基苯甲酰基] -2 - [（3-羟基-1,2-苯并异恶唑-6-基）甲氧基 ]苯基}丙酸在粉末X射线衍射图中的衍射角在14.6,23.1,24.7,25.6和26.0°处具有峰值，具有小的比容，难以被电荷充电 易于处理，并且可用于优异的抗风湿剂的活性药物成分。

    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。

    NOVEL CRYSTAL OF 3-[5-[4-(CYCLOPENTYLOXY)-2- HYDROXYBENZOYL]-2-[(3-HYDROXY-1,2-BENZISOXAZOL-6-YL)METHOXY]PHENYL]PROPIONIC ACID
    7.
    发明授权
    NOVEL CRYSTAL OF 3-[5-[4-(CYCLOPENTYLOXY)-2- HYDROXYBENZOYL]-2-[(3-HYDROXY-1,2-BENZISOXAZOL-6-YL)METHOXY]PHENYL]PROPIONIC ACID 有权
    新的晶体形式的3- [5- [4-（环戊氧基）-2-羟基苯甲酰基] -2 - [（3-羟基-1,2-苯并异唑-6-基）甲氧基]苯基]丙酸

    公开(公告)号：EP2022788B1

    公开(公告)日：2010-09-01

    申请号：EP07744104.6

    申请日：2007-05-25

    申请人： TOYAMA CHEMICAL CO., LTD.

    发明人： YONEZAWA, Kenji ,  KOTSUBO, Hironori ,  BABA, Yasutaka ,  TADA, Yukie

    IPC分类号： C07D261/12 ,  A61K31/42 ,  A61P19/02

    CPC分类号： C07D261/20

    摘要： Disclosed is a crystal of 3-[5-[4-(cyclopentyloxy)-2- hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6- yl)methoxy]phenyl]propionic acid having refraction angles of 14.0, 16.0, 23.3, 23.7 and 26.3˚ as measured in terms of 2ϑ in powder X-ray diffraction pattern. Also disclosed is a crystal of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3- hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionic acid having refraction angles of 14.6, 23.1, 24.7, 25.6 and 26.0˚ as measured in terms of 2ϑ in powder X-ray diffraction pattern. These crystals have small specific volumes, are hardly charged electrically, can be handled easily, and are useful as excellent active ingredients for anti-rheumatic drugs.