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    ACRYLAMIDE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME
    1.
    发明公开
    ACRYLAMIDE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME 失效
    ACRYLAMID-DERIVATE UND VERFAHREN ZU DEREN HERSTELLUNG

    公开(公告)号：EP0799827A1

    公开(公告)日：1997-10-08

    申请号：EP95937194.9

    申请日：1995-11-28

    申请人： KYORIN PHARMACEUTICAL CO., LTD. ,  SAGAMI CHEMICAL RESEARCH CENTER

    发明人： FUKUDA, Yasumichi ,  SETO, Shigeki ,  OOMORI, Yasuo ,  EBISU, Hiroyuki ,  TERASHIMA, Shiro

    IPC分类号： C07D487/04

    CPC分类号： C07D519/00

    摘要： Acrylamide derivatives represented by General Formula (1) below:
    (One specific example of General Formula (1) is methyl (S,S)-3,3,-[3,3'-(1,4-phenylenediacryloyl)]-bis[1-chloromethyl-5-hydroxy-7-trifluoromethyl-1,2,3,6-tetrahydropyrrolo[3,2-e]indole-8-carboxylate.)
    The acrylamide derivatives represented by General Formula (1) is highly selective to cancer cells, less toxic, and highly active also against solid tumor.

    摘要翻译： （1）表示的丙烯酰胺衍生物：通式（1）的一个具体实例是甲基（S，S）-3,3，-a3,3' - （1,4-亚苯基二
    酰基）Ü 由通式（1）表示的丙烯酰胺衍生物对癌细胞是高选择性的， 毒性较小，对实体瘤有较高的活性。

    FUSED BICYCLIC PYRIDINE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS
    4.
    发明公开
    FUSED BICYCLIC PYRIDINE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
    KONDENSIERTE，BICYCLISCHE PYRIDIN DERIVATE ALS TACHYKININREZEPTORANTAGONISTEN

    公开(公告)号：EP1457493A1

    公开(公告)日：2004-09-15

    申请号：EP02786049.3

    申请日：2002-12-06

    申请人： Kyorin Pharmaceutical Co., Ltd.

    发明人： SETO, Shigeki ,  TANIOKA, Asao ,  IKEDA, Makoto ,  IZAWA, Shigeru

    IPC分类号： C07D498/04 ,  A61K31/4353 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/553 ,  A61P1/00 ,  A61P1/02 ,  A61P1/04 ,  A61P1/08 ,  A61P11/06 ,  A61P11/14 ,  A61P13/00 ,  A61P13/10 ,  A61P19/02 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P43/00

    CPC分类号： C07D498/04

    摘要： A novel fused bicyclic pyridine derivative or a salt thereof that acts as a tachykinin receptor antagonist, in particular as an NK1 receptor antagonist, is represented by the following general formula (1):
       wherein the rings A and B are each a benzene'ring which may have 1 to 3 substituents (any adjacent two of which may be bound to one another to form a ring);
       the ring C is a nitrogen-containing ring having a hydrogen atom substituted with a nitrogen atom;
       R 1 and R 2 are each independently a hydrogen atom, a C 1 to C 6 alkyl group, a C 1 to C 6 alkylsulfonyl group, a C 1 to C 6 alkylcarbonyl group, or a C 1 to C 6 alkoxycarbonyl group, or R 1 and R 2 are bound to one another to form the ring D; m is 1 or 2; n is 2 or 3; and q is an integer from 1 to 4.

    摘要翻译： 用作速激肽受体拮抗剂，特别是作为NK1受体拮抗剂的新型稠合双环吡啶衍生物或其盐由以下通式（1）表示：其中环A和B各自为苯 '环，其可以具有1至3个取代基（其中相邻的两个可以彼此结合形成环）; 环C是具有被氮原子取代的氢原子的含氮环; R 1和R 2各自独立地为氢原子，C 1至C 6烷基，C 1至C 6烷基磺酰基，C 1至C 6烷基羰基或C 1至C 6烷氧基羰基，或R 1， 和R 2彼此结合形成环D; m为1或2; n为2或3; q为1〜4的整数。

    PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF
    5.
    发明公开
    PYRAZOLOPYRIDINE DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF 审中-公开
    吡唑并吡啶衍生物

    公开(公告)号：EP2669285A1

    公开(公告)日：2013-12-04

    申请号：EP12739093.8

    申请日：2012-01-25

    申请人： Kyorin Pharmaceutical Co., Ltd. ,  Kissei Pharmaceutical Co., Ltd.

    发明人： SETO, Shigeki ,  UMEI, Kentaro ,  NISHIGAYA, Yosuke ,  TANIOKA, Asao ,  KONDO, Tatsuhiro ,  KONDO, Atsushi ,  TATANI, Kazuya ,  KAWAMURA, Naohiro

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/5377 ,  A61P13/02 ,  A61P43/00

    CPC分类号： C07D471/04

    摘要： A pyrazolopyridine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof exhibits a strong EP 1 receptor antagonistic effect. Thus, the derivative or the pharmacologically acceptable salt is useful as a therapeutic agent for lower urinary tract symptoms (LUTS), particularly, overactive bladder syndrome (OABs), or a prophylactic agent therefor and furthermore, is also useful in the treatment, prevention, or suppression of various pathological conditions in which the EP 1 receptor is involved, such as inflammatory disease, pain disease, osteoporosis, and cancer.

    [A is a benzene ring or the like, Y 1 is C 1-6 alkylene, R 1 is -C(=O)-OZ 1 or the like, Z 1 is H or the like, R 2 is a branched C 3-6 alkyl group or the like, R 3 is H or the like, R 4 is a hydrogen atom or the like, and R 5 is a hydrogen atom or the like].

    摘要翻译： 由下式（I）表示的吡唑并吡啶衍生物或其药理学上可接受的盐表现出强烈的EP 1受体拮抗作用。 因此，衍生物或药理学上可接受的盐可用作下尿路症状（LUTS），特别是膀胱过度活动症（OAB）或其预防剂的治疗剂，此外，还可用于治疗，预防， 或抑制涉及EP 1受体的各种病理状况，例如炎性疾病，疼痛疾病，骨质疏松症和癌症。 [A是苯环等，Y 1是C 1-6亚烷基，R 1是-C（= O）-OZ 1等，Z 1是H等，R 2是支链C 3 -6烷基等，R 3为H等，R 4为氢原子等，R 5为氢原子等）。