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    Pyrrole compounds
    231.
    发明授权
    Pyrrole compounds 有权

    公开(公告)号：US08592597B2

    公开(公告)日：2013-11-26

    申请号：US13061078

    申请日：2009-08-26

    Applicant: Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Ikuo Fujimori

    Inventor： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Ikuo Fujimori

    IPC: C07D401/14

    CPC classification number: A61K31/444 ,  C07D401/14

    Abstract: The present invention relates to a compound represented by the formula: wherein A is pyridyl group having at least one substituent wherein R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, R4 and R6 are each a hydrogen atom, a halogen atom or a C1-6 alkyl group optionally substituted by halogen, R5 is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, and R7 is a hydrogen atom or a C1-6 alkyl group optionally substituted by halogen or a salt thereof, or a pharmaceutical composition containing the same.

    THERAPEUTIC AGENT FOR IRRITABLE BOWEL SYNDROME
    234.
    发明申请
    THERAPEUTIC AGENT FOR IRRITABLE BOWEL SYNDROME 审中-公开
    可治疗性皮肤病综合征的治疗药物

    公开(公告)号：US20130281435A1

    公开(公告)日：2013-10-24

    申请号：US13917770

    申请日：2013-06-14

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： Minoru MARUYAMA

    IPC: A61K31/553 ,  A61K31/498

    CPC classification number: A61K31/553 ,  A61K31/498 ,  C07D241/44 ,  C07D498/04

    Abstract: [Summary][Problem] The present invention aims to provide an agent for the prophylaxis or treatment of irritable bowel syndrome.[Solving Means] An agent for the prophylaxis or treatment of irritable bowel syndrome, containing a compound having a TGR5 receptor agonist activity, a fused ring compound represented by the formula wherein ring A is an optionally substituted aromatic ring, and ring B′ is a 5- to 9-membered ring having one or more substituents, or a salt thereof as an active ingredient.

    Abstract translation: 发明内容本发明旨在提供一种预防或治疗肠易激综合征的药剂。 [解决方案]一种预防或治疗肠易激综合征的药剂，其含有具有TGR5受体激动剂活性的化合物，下式表示的稠环化合物，其中环A为任选取代的芳环，环B'为 具有一个或多个取代基的5-至9-元环或其盐作为活性成分。

    PHARMACEUTICAL COMPOSITION
    236.
    发明申请
    PHARMACEUTICAL COMPOSITION 审中-公开
    药物组合物

    公开(公告)号：US20130261156A1

    公开(公告)日：2013-10-03

    申请号：US13905090

    申请日：2013-05-29

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： Yasuhiro Hiraishi ,  Muneo Nonomura

    IPC: A61K47/12 ,  A61K47/10 ,  A61K47/02

    CPC classification number: A61K47/12 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2853 ,  A61K9/2866 ,  A61K31/4427 ,  A61K47/02 ,  A61K47/10

    Abstract: The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof.According to the present invention, a pharmaceutical composition can be stabilized by containing a nonpeptidic pharmaceutically active ingredient having a primary or secondary amino group, an excipient and an acidic compound. In addition, a solid preparation containing a pharmaceutically active ingredient, titanium oxide, a plasticizer and a chain organic acid can enhance the stability of the pharmaceutically active ingredient during light irradiation.

    Abstract translation: 本发明提供含有稳定的药物活性成分的药物组合物或固体制剂及其稳定化方法。 根据本发明，可以通过含有具有伯氨基或仲氨基的非肽类药物活性成分，赋形剂和酸性化合物来稳定药物组合物。 此外，含有药物活性成分，氧化钛，增塑剂和链状有机酸的固体制剂可以在光照射期间增强药物活性成分的稳定性。

    FUSED HETEROCYCLIC COMPOUNDS
    238.
    发明申请
    FUSED HETEROCYCLIC COMPOUNDS 有权
    熔融杂环化合物

    公开(公告)号：US20130172292A1

    公开(公告)日：2013-07-04

    申请号：US13814073

    申请日：2011-08-03

    Applicant: Joseph Raker ,  Takahiko Taniguchi ,  Masato Yoshikawa ,  Tomoaki Hasui ,  Jun Kunitomo

    Inventor： Joseph Raker ,  Takahiko Taniguchi ,  Masato Yoshikawa ,  Tomoaki Hasui ,  Jun Kunitomo

    IPC: C07D471/04 ,  C07D471/14 ,  C07D519/00

    CPC classification number: C07D471/04 ,  C07D471/14 ,  C07D519/00

    Abstract: The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1′): wherein, Ring A′ represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1′ represents (1) wherein, R1a′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2 represents a bond, —S—, -0-, —CO—, an optionally substituted methylene group, or —NRa′-(Ra′ represents a hydrogen atom, or an optionally substituted C1-6 alkyl group), and Ring B1′ represents an optionally further substituted 6- to 10-membered aromatic hydrocarbon ring, or an optionally further substituted 5- to 10-membered aromatic heterocyclic ring, or alternatively, L′ and R1a′ may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R1b′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2′ represents an optionally substituted benzene ring, an optionally substituted pyridine ring, an optionally substituted pyrimidine ring, an optionally substituted pyrazine ring, or an optionally substituted pyridazine ring, Ring D′ represents an optionally further substituted 5- or 6-membered ring, R2′ represents a hydrogen atom, or a substituent, X′ represents ═N— or ═CRb′—(Rb′ represents a hydrogen atom, or a substituent), - - - - - represents that Rb′ and R2′ may form, taken together with the carbon atom and the nitrogen atom to which they are each adjacent, an optionally substituted 5- to 7-membered ring when.X′ is ═CRb′, or a salt thereof.

    Abstract translation: 本发明提供了具有PDE 10A抑制作用的化合物，其可用作预防或治疗精神分裂症等的药物。 由式（1'）表示的化合物：其中环A'表示任选取代的吡啶环，任选取代的哒嗪环，嘧啶环或吡嗪环，R1'表示（1）其中R1a'表示 任选取代的苯基或任选取代的5至10元杂环基，环B2表示键，-S - ， - O-，-CO-，任选取代的亚甲基或-NR a' - （R a '表示氢原子或任选取代的C 1-6烷基），并且环B1'表示任选进一步取代的6至10元芳族烃环或任选进一步取代的5至10元芳族杂环 ，或者可选地，L'和R 1a'可以一起形成任选取代的双环或三环稠合杂环基，或（2），其中，R 1b'表示任选取代的苯基，或任选取代的5-至10- 环B2'表示 任选取代的苯环，任选取代的吡啶环，任选取代的嘧啶环，任选取代的吡嗪环或任选取代的哒嗪环，环D'表示任选进一步取代的5-或6-元环，R 2' 表示氢原子或取代基，X'表示= N-或= CRb' - （Rb'表示氢原子或取代基）， - - - 表示Rb'和R2'可以一起形成 与它们各自相邻的碳原子和氮原子，当X'= CRb'或其盐时，任选取代的5-至7-元环。

    Nitrogen-containing heterocyclic compound and use thereof
    239.
    发明授权
    Nitrogen-containing heterocyclic compound and use thereof 有权
    含氮杂环化合物及其用途

    公开(公告)号：US08470816B2

    公开(公告)日：2013-06-25

    申请号：US12314015

    申请日：2008-12-02

    Applicant: Yoshinori Ikeura ,  Junya Shirai ,  Hideyuki Sugiyama ,  Yuji Nishikimi ,  Taku Kamei ,  Nobuki Sakauchi

    Inventor： Yoshinori Ikeura ,  Junya Shirai ,  Hideyuki Sugiyama ,  Yuji Nishikimi ,  Taku Kamei ,  Nobuki Sakauchi

    IPC: A61K31/5355 ,  A61K31/445 ,  A61K31/444 ,  A61K31/40 ,  C07D413/04 ,  C07D401/04 ,  C07D211/56 ,  C07D207/14

    CPC classification number: C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D407/12 ,  C07D409/12 ,  C07D417/14

    Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since the compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, gastrointestinal diseases, central nervous system diseases and the like.

    Abstract translation: 本发明涉及一种由下式表示的化合物：其中环A为任选具有取代基的含氮杂环，环B为任选具有取代基的芳环，环C为任选具有取代基的环状基团 R 1为氢原子，任选具有取代基的烃基，酰基，任选具有取代基的杂环基或任选具有取代基的氨基，R2为任选卤代的C1 -6烷基，m和n分别为0〜5的整数，m + n为2〜5的整数，为单键或双键，或其盐等。 由于该化合物具有优异的速激肽受体拮抗作用，并且可用作预防或治疗诸如下尿路疾病，胃肠道疾病，中枢神经系统疾病等各种疾病的药剂。

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