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    Thienopyridine Derivatives, Production Method and Use Thereof
    1.
    发明申请
    Thienopyridine Derivatives, Production Method and Use Thereof 审中-公开
    噻吩并吡啶衍生物，其生产方法和用途

    公开(公告)号：US20080146602A1

    公开(公告)日：2008-06-19

    申请号：US11596634

    申请日：2005-05-13

    申请人： Atsuo Baba ,  Tsuneo Yasuma ,  Hiroyuki Tawada ,  Makoto Yamashita

    发明人： Atsuo Baba ,  Tsuneo Yasuma ,  Hiroyuki Tawada ,  Makoto Yamashita

    IPC分类号： A61K31/4365 ,  C07D471/04 ,  A61P19/02

    CPC分类号： C07D495/04

    摘要： A compound represented by the formula (I) wherein R is a hydrogen atom or a C1-4 alkyl group, and X is CH2, O or S, or a salt thereof. The present invention provides a novel thienopyridine derivative having an anti-inflammatory effect, a bone resorption suppressing effect, an immune cytokine production suppressing effect and the like, and useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of arthritis such as rheumatoid arthritis and the like, and the like, and the like.

    摘要翻译： 由式（I）表示的化合物，其中R是氢原子或C 1-4烷基，X是CH 2，O或S，或 的盐。 本发明提供具有抗炎作用，骨吸收抑制作用，免疫细胞因子产生抑制作用等的新颖的噻吩并吡啶衍生物，可用作预防或治疗关节炎的药剂如 类风湿关节炎等，类似物等。

    Thienopyridine derivatives, their production and use
    2.
    发明授权
    Thienopyridine derivatives, their production and use 失效
    噻吩并吡啶衍生物，其生产和使用

    公开(公告)号：US06653476B2

    公开(公告)日：2003-11-25

    申请号：US10204593

    申请日：2002-08-22

    申请人： Tsuneo Yasuma ,  Atsuo Baba ,  Haruhiko Makino ,  Isao Aoki ,  Toshiaki Nagata

    发明人： Tsuneo Yasuma ,  Atsuo Baba ,  Haruhiko Makino ,  Isao Aoki ,  Toshiaki Nagata

    IPC分类号： A61K314365

    CPC分类号： C07D495/04 ,  C07D495/14

    摘要： The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, —(CH2)q—, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.

    摘要翻译： 本发明提供可用作抗炎药物的噻吩并吡啶衍生物，特别是作为关节炎的补救剂; 制备它们的方法和含有它们的药物组合物。 噻吩并吡啶衍生物由式（I）表示：其中G是卤素原子，羟基，任选取代的氨基等; 烷基是任选取代的低级亚烷基; X是O，S， - （CH 2）q - 等; R是任选取代的氨基等; 环B是任选取代的含有Y的5至8元环，其环组成原子不含氮原子; Y是O，S，（其中Ra，Rb和Rc相同或不同，并且各自为H，卤素原子，任选取代的烃基等）等; 并且环A可以被取代。

    Thienopyridine derivatives, their production and use
    3.
    发明授权
    Thienopyridine derivatives, their production and use 失效
    噻吩并吡啶衍生物，其生产和使用

    公开(公告)号：US07067527B2

    公开(公告)日：2006-06-27

    申请号：US10662165

    申请日：2003-09-03

    申请人： Tsuneo Yasuma ,  Atsuo Baba ,  Haruhiko Makino ,  Isao Aoki ,  Toshiaki Nagata

    发明人： Tsuneo Yasuma ,  Atsuo Baba ,  Haruhiko Makino ,  Isao Aoki ,  Toshiaki Nagata

    IPC分类号： C07D495/14 ,  A61K31/38

    CPC分类号： C07D495/04 ,  C07D495/14

    摘要： The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, —(CH2)q—, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.

    摘要翻译： 本发明提供可用作抗炎药物的噻吩并吡啶衍生物，特别是作为关节炎的补救剂; 制备它们的方法和含有它们的药物组合物。 噻吩并吡啶衍生物由式（I）表示：其中G是卤素原子，羟基，任选取代的氨基等; 烷基是任选取代的低级亚烷基; X是O，S， - （CH 2 CH 2）q - 等; R是任选取代的氨基等; 环B是任选取代的含有Y的5至8元环，其环组成原子不含氮原子; Y是O，S，（其中Ra，Rb和Rc相同或不同，并且各自为H，卤素原子，任选取代的烃基等）等; 并且环A可以被取代。

    Thienopyridine derivatives and their use
    4.
    发明授权
    Thienopyridine derivatives and their use 失效
    噻吩并吡啶衍生物及其用途

    公开(公告)号：US6046189A

    公开(公告)日：2000-04-04

    申请号：US860452

    申请日：1997-06-26

    申请人： Takashi Sohda ,  Haruhiko Makino ,  Atsuo Baba

    发明人： Takashi Sohda ,  Haruhiko Makino ,  Atsuo Baba

    IPC分类号： A61K31/435 ,  C07D495/14 ,  C07D493/14 ,  A61K31/55 ,  C07D223/00

    CPC分类号： C07D495/14

    摘要： There is disclosed a compound of the formula (A): ##STR1## wherein W is C-G or C-G' (G is optionally esterified carboxyl; and G' is halogen); X is oxygen, optionally oxidized sulfur or --(CH.sub.2).sub.q -- (q is 0 to 5); R is optionally substituted amino or heterocyclic group; the ring B is optionally substituted nitrogen-containing 5- to 7-membered ring; L is hydrogen, optionally substituted hydrocarbon residue, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl provided that, when W is C-G, L is hydrogen, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted alkoxycarbonyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl; n is 0 or 1; the ring A may have a substituent. A process for producing the compound (A) and a pharmaceutical composition containing the compound (A) are also disclosed. The pharmaceutical composition is useful for an anti-inflammatory drug, particularly, a drug for preventing or treating arthritis, a drug for inhibiting bone resorption, immunosuppressant or the like.

    摘要翻译： PCT No.PCT / JP97 / 01413 Sec。 371日期：1997年6月26日 102（e）日期1997年6月26日PCT 1997年4月23日提交PCT公布。 公开号WO97 / 40050 PCT 日期：1997年10月30日公开了式（A）的化合物：其中W为C-G或C-G'（G为任意酯化的羧基，G'为卤素）; X为氧，任选氧化硫或 - （CH 2）q - （q为0至5）; R是任选取代的氨基或杂环基; 环B为任选取代的含氮5至7元环; L是氢，任选取代的烃残基，任选取代的酰基，任选取代的氨基甲酰基，任选取代的硫代氨基甲酰基或任选取代的磺酰基，条件是当W为CG时，L为氢，任选取代的酰基，任选取代的氨基甲酰基，任选取代的烷氧基羰基， 硫代氨基甲酰基或任选取代的磺酰基; n为0或1; 环A可以具有取代基。 还公开了制备化合物（A）的方法和含有化合物（A）的药物组合物。 药物组合物可用于抗炎药物，特别是用于预防或治疗关节炎的药物，用于抑制骨吸收的药物，免疫抑制剂等。

    COMPOUND HAVING 6-MEMBERED AROMATIC RING
    5.
    发明申请
    COMPOUND HAVING 6-MEMBERED AROMATIC RING 审中-公开
    具有六层芳香环的化合物

    公开(公告)号：US20110009421A1

    公开(公告)日：2011-01-13

    申请号：US12919400

    申请日：2009-02-27

    申请人： Masaki Setoh ,  Toshitake Kobayashi ,  Toshio Tanaka ,  Atsuo Baba

    发明人： Masaki Setoh ,  Toshitake Kobayashi ,  Toshio Tanaka ,  Atsuo Baba

    IPC分类号： A61K31/497 ,  C07D239/24 ,  C07D401/12 ,  C07D211/72 ,  C07D213/62 ,  C07D413/12 ,  C07D417/12 ,  A61K31/506 ,  A61K31/444 ,  A61K31/4439 ,  A61P25/18

    CPC分类号： C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D239/34 ,  C07D239/42 ,  C07D295/12 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity.[Means] A compound represented by the following formula (I) or salt thereof: wherein A represents —(CH2)n—CO—NRa— (n is an integer of 0 to 3) or —NRa—CO—, B represents a hydrogen atom, halogen atom, cyano group, hydroxy group, or the like, X1, X2, X3, and X4 represent the same or different —CRx═, or —N═, Y represents —O—, —S—, —S(O)—, —S(O)2—, or —NRy—, Z represents a bond, methylene, or ethylene, Ar1 represents a five- to ten-membered aromatic ring (except for thiazole) which may be substituted with one or more substituents selected from halogen atoms, optionally halogenated C1-6 alkyl groups, and the like, Ar2 represents a five- to six-membered aromatic ring which may be substituted with one or more substituents selected from halogen atoms, optionally halogenated C1-6 alkyl groups, and the like, and which may be condensed with an optionally substituted five- to six-membered ring, and Ra, Rb, Rx, and Ry represent the same or different hydrogen atom, halogen atoms, or the like].

    摘要翻译： 本发明的目的是提供一种用于预防或治疗精神分裂症等的药剂，其中本发明的化合物具有GPRS2激动剂活性。 [表示]下式（I）表示的化合物或其盐：其中A表示 - （CH 2）n -CO-NR a - （n为0〜3的整数）或-NR a -CO-，B表示 氢原子，卤素原子，氰基，羟基等，X 1，X 2，X 3和X 4表示相同或不同的-CR x =或-N =，Y表示-O - ， - S-，-S （O） - ， - S（O）2 - 或-NR y - ，Z表示键，亚甲基或亚乙基，Ar 1表示5至10元芳环（噻唑除外），可以被一个 或更多选自卤素原子，任选卤代C 1-6烷基等取代基，Ar 2表示可被一个或多个选自卤素原子，任意卤代C 1-6的取代基取代的五至六元芳环 烷基等，并且其可以与任选取代的五元至六元环稠合，并且R a，R b，R x和R y表示相同或不同的氢 原子，卤素原子等]。

    Thienodipyridine derivatives, production and use thereof
    6.
    发明授权
    Thienodipyridine derivatives, production and use thereof 失效
    噻吩二吡啶衍生物，其生产和使用

    公开(公告)号：US06214838B1

    公开(公告)日：2001-04-10

    申请号：US09355218

    申请日：1999-07-23

    申请人： Takashi Sohda ,  Haruhiko Makino ,  Atsuo Baba ,  Taihei Yamane

    发明人： Takashi Sohda ,  Haruhiko Makino ,  Atsuo Baba ,  Taihei Yamane

    IPC分类号： A61K314365

    CPC分类号： C07D495/14

    摘要： A compound of the formula (I): wherein R is hydrogen or C2-6 alkanoyl; X is halogen; and ring A is benzene ring which is optionally substituted by 1 to 4 substituents selected from {circle around (1)} halogen, {circle around (2)} hydroxy, {circle around (3)} C1-6 alkoxy optionally substituted by halogen or phenyl, {circle around (4)} C1-6 alkylthio optionally substituted by halogen or phenyl, {circle around (5)} C1-6 alkyl optionally substituted by halogen, {circle around (6)} C2-6 alkanoylamino or {circle around (7)} carboxy optionally esterified by C1-6 alkyl, or a salt thereof; which can be used for preventing or treating inflammatory disease, arthritis, chronic rheumatoid arthritis, autoimmune diseases, or rejection after organ transplantation.

    摘要翻译： 式（I）的化合物：其中R是氢或C 2-6烷酰基; X是卤素; 并且环A是苯环，其任选被1至4个选自{（1）}周围的环，（2）}羟基周围的环，[（3）周围的环（任选被卤素取代）的C 1-6烷氧基 或苯基，（任选被（4）周围的环）被卤素或苯基任意取代的C 1-6烷硫基，（（5）周围的环）任选被卤素取代的C 1-6烷基，（绕（6）周围的C 2-6烷酰基氨基或{ （7）}羧基，其任选被C 1-6烷基酯化，或其盐; 其可用于预防或治疗炎症性疾病，关节炎，慢性类风湿性关节炎，自身免疫性疾病或器官移植后的排斥反应。

    Thienopyridine or thienopyrimidine derivatives and their use
    7.
    发明授权
    Thienopyridine or thienopyrimidine derivatives and their use 失效
    噻吩并吡啶或噻吩并嘧啶衍生物及其用途

    公开(公告)号：US5747486A

    公开(公告)日：1998-05-05

    申请号：US571915

    申请日：1995-12-27

    申请人： Takashi Sohda ,  Haruhiko Makino ,  Atsuo Baba

    发明人： Takashi Sohda ,  Haruhiko Makino ,  Atsuo Baba

    IPC分类号： C07D495/04 ,  A61K31/54 ,  A61K31/535 ,  C07D401/02 ,  C07D403/02

    CPC分类号： C07D495/04

    摘要： This invention provides an anti-inflammatory agent, particularly an agent for treating arthritis, and a bone resorption inhibiting agent, containing a thienopyridine or thienopyrimidine derivative or a salt thereof. This invention also provides a novel thienopyridine or thienopyrimidine derivative having anti-inflammatory activity and bone resorption inhibiting activity.

    摘要翻译： PCT No.PCT / JP95 / 02271 Sec。 371 1995年12月27日第 102（e）日期1995年12月27日PCT提交1995年11月7日PCT公布。 第WO96 / 14319号公报 日期1996年5月17日本发明提供了抗炎剂，特别是治疗关节炎的药剂和含有噻吩并吡啶或噻吩并嘧啶衍生物或其盐的骨吸收抑制剂。 本发明还提供具有抗炎活性和骨吸收抑制活性的新型噻吩并吡啶或噻吩并嘧啶衍生物。

    Thienopyridine derivatives and their use
    8.
    发明授权
    Thienopyridine derivatives and their use 失效
    噻吩并吡啶衍生物及其用途

    公开(公告)号：US06403606B1

    公开(公告)日：2002-06-11

    申请号：US09506010

    申请日：2000-02-17

    申请人： Takashi Sohda ,  Haruhiko Makino ,  Atsuo Baba

    发明人： Takashi Sohda ,  Haruhiko Makino ,  Atsuo Baba

    IPC分类号： A61K314353

    CPC分类号： C07D495/14

    摘要： There is disclosed a compound of the formula (A): wherein W is C—G or C—G′ (G is optionally esterified carboxyl; and G′ is halogen); X is oxygen, optionally oxidized sulfur or —(CH2)q—, (q is 0 to 5); R is optionally substituted amino or heterocyclic group; the ring B is optionally substituted nitrogen-containing 5- to 7-membered ring; L is hydrogen, optionally substituted hydrocarbon residue, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl provided that, when W is C—G, L is hydrogen, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted alkoxycarbonyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl; n is 0 or 1; the ring A may have a substituent. A process for producing the compound (A) and a pharmaceutical composition containing the compound (A) are also disclosed. The pharmaceutical composition is useful for an anti-inflammatory drug, particularly, a drug for preventing or treating arthritis, a drug for inhibiting bone resorption, immunosuppressant or the like.

    摘要翻译： 公开了式（A）的化合物：其中W是C-G或C-G'（G任选被酯化的羧基，G'是卤素）; X为氧，任选氧化硫或 - （CH 2）q - ，（q为0至5）; R是任选取代的氨基或杂环基; 环B为任选取代的含氮5至7元环; L是氢，任选取代的烃残基，任选取代的酰基，任选取代的氨基甲酰基，任选取代的硫代氨基甲酰基或任选取代的磺酰基，条件是当W为CG时，L为氢，任选取代的酰基，任选取代的氨基甲酰基，任选取代的烷氧基羰基， 硫代氨基甲酰基或任选取代的磺酰基; n为0或1; 环A可以具有取代基。 还公开了制备化合物（A）的方法和含有化合物（A）的药物组合物。 药物组合物可用于抗炎药物，特别是用于预防或治疗关节炎的药物，用于抑制骨吸收的药物，免疫抑制剂等。