UTERINE CONTRACTION INHIBITORS
    91.
    发明授权
    UTERINE CONTRACTION INHIBITORS 有权
    子宫收缩抑制剂的

    公开(公告)号:EP1205185B1

    公开(公告)日:2008-08-06

    申请号:EP00939158.2

    申请日:2000-06-23

    IPC分类号: A61K38/17 A61P15/06 A61P43/00

    CPC分类号: A61K38/22

    摘要: Compositions containing adrenomedulin for inhibiting automatic uterine contraction or contraction caused by bradykinin. These compositions are usable for selectively inhibiting automatic uterine contraction or contraction caused by bradykinin, preventing premature birth, preventing abortion, ceasing delivery before cesarean section, or treating difficult menstruation.

    INDOLE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONIST ACTIVITY
    93.
    发明公开
    INDOLE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONIST ACTIVITY 有权
    INDOLDERIVAT MIT PGD2-REZEPTOR-ANTAGONISTISCHER WIRKUNG

    公开(公告)号:EP1916245A1

    公开(公告)日:2008-04-30

    申请号:EP06781305.5

    申请日:2006-07-20

    摘要: The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases.
    A compound of the generic formula (I)

    wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.;R 1 , R 2 , R 3 , R 4 and R 5 are independently a hydrogen atom or a halogen atom etc.; R 6 is C2-C4 alkyloxy etc.; R 7 is independently a halogen atom etc.; R 8 is independently C1-C4 alkyl etc.; R 9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L 1 , L 2 and L 3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.;
    a pharmaceutically acceptable salt or hydrate thereof.

    摘要翻译: 本发明产生具有DP受体拮抗活性的吲哚衍生物和包含所述化合物作为活性成分的药物组合物,还有用于治疗过敏性疾病的治疗剂。 通式(I)的化合物,其中环A是芳族碳环等; 环B为3〜8元含氮非芳香族杂环等; R 1,R 2,R 3,R 4和R 5独立地为氢原子或卤素原子等; R 6是C 2 -C 4烷氧基等。 R 7独立地为卤素原子等; R 8独立地为C 1 -C 4烷基等。 R 9为羧基等。 Y是单键等; M是磺酰基等。 L 1,L 2和L 3是任选含有一个或两个杂原子等的单键或亚烷基; n为0等 q是0等 其药学上可接受的盐或水合物。

    PROCESS FOR PRODUCTION OF CARBAPENEM DERIVATIVE AND CRYSTALLINE INTERMEDIATE THEREFOR
    95.
    发明公开
    PROCESS FOR PRODUCTION OF CARBAPENEM DERIVATIVE AND CRYSTALLINE INTERMEDIATE THEREFOR 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINES CABAPENEM-DERIVATS UND KRISTALLINES ZWISCHENPRODUKTDAFÜR

    公开(公告)号:EP1852436A1

    公开(公告)日:2007-11-07

    申请号:EP06713624.2

    申请日:2006-02-14

    IPC分类号: C07D477/00

    CPC分类号: C07D207/12 C07D477/00

    摘要: An object of the present invention is to provide a carbapenem synthetic intermediate which is advantageous in an industrial process. There are provided a process for producing Compound (I), or a pharmaceutically acceptable salt, or a solvate, or a crystal thereof, comprising reacting Compound (III) and Compound (IV) in the presence of the secondary amine, and a benzyl alcoholated crystal of Compound (I). There are further provided a method of deprotecting Compound (I) with a Pd catalyst, and a crystal of Compound (IV).

    摘要翻译: 本发明的目的是提供一种在工业过程中有利的碳青霉烯合成中间体。 提供了一种制备化合物(I)或其药学上可接受的盐或其溶剂合物或其结晶的方法,其包括在仲胺存在下使化合物(III)和化合物(IV)与苄醇化的 化合物(I)的晶体。 还提供了使用Pd催化剂和化合物(IV)的结晶使化合物(I)脱保护的方法。

    THERAPEUTIC AGENT FOR CONSTIPATION
    96.
    发明公开
    THERAPEUTIC AGENT FOR CONSTIPATION 审中-公开
    治疗MITTEL GEGEN OBSTIPATION

    公开(公告)号:EP1844792A1

    公开(公告)日:2007-10-17

    申请号:EP05816775.0

    申请日:2005-12-13

    IPC分类号: A61K45/00 A61K31/485 A61P1/10

    CPC分类号: A61K31/485 A61K45/06

    摘要: A therapeutic and/or prophylactic agent for constipation induced by a compound having an opioid µ receptor agonist activity, which agent comprises as an effective ingredient a compound having an opioid δ receptor antagonist activity, e.g., a compound of Formula (I):




    (wherein R 1 represents hydrogen, lower alkyl, cycloalkyl lower alkyl or the like; R 2 and R 3 independently represent hydrogen, hydroxy or the like; R 4 is hydrogen, hydroxy or the like; R 5 is hydrogen; R 4 and R 5 may optionally form -O- or the like; R 6 represents hydrogen, lower alkyl or the like (wherein X represents -O- or -N(R 10 )-or the like; R 7 , R 8 , R 9a and R 9b independently represent hydrogen, lower alkyl, lower alkoxycarbonyl or the like; r represents an integer of 0 to 5; Y represents -CH- or the like; Z represents a crosslinkage composed of 2 to 5 atoms)
    or a pharmaceutically acceptable salt thereof or a solvate of either.

    摘要翻译: 一种由具有阿片样物质μ受体激动剂活性的化合物引起的便秘的治疗和/或预防剂,该药物包含作为有效成分的具有阿片受体拮抗剂活性的化合物,例如式(I)的化合物:(其中 R 1代表氢,低级烷基,环烷基低级烷基等; R 2和R 3独立地代表氢,羟基等; R 4是氢,羟基等; R 5是氢; R 4和R 5可以是 任选形成-O-等; R 6表示氢,低级烷基等(其中X表示-O-或-N(R 10) - 等; R 7,R 8,R 9a和R 9b独立地 表示氢,低级烷基,低级烷氧基羰基等; r表示0〜5的整数,Y表示-CH-等; Z表示2〜5个原子的交联键)或其药学上可接受的盐或溶剂合物 的任何一个。