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    Benzothiepine derivatives, their production and use
    1.
    发明授权
    Benzothiepine derivatives, their production and use 失效
    苯并噻吩衍生物，其生产和使用

    公开(公告)号：US06531604B2

    公开(公告)日：2003-03-11

    申请号：US10044787

    申请日：2002-01-11

    申请人： Tsuneo Yasuma ,  Haruhiko Makino ,  Akira Mori

    发明人： Tsuneo Yasuma ,  Haruhiko Makino ,  Akira Mori

    IPC分类号： C07D21140

    CPC分类号： C07D263/44 ,  C07D211/88 ,  C07D233/74 ,  C07D277/04 ,  C07D295/135 ,  C07D495/04

    摘要： The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

    摘要翻译： 本发明提供下式的化合物：其中环A是任选取代的苯环; R1是任选取代的非芳族杂环基; R2和R3独立地为氢原子或任选取代的烃基; n为0-3的整数; 或其盐，其可用作具有成骨促进作用的药物和软骨素促进作用。本发明涉及具有抑制淀粉样蛋白b蛋白的产生和/或分泌的优异效果的胺化合物及其制备和用途。 特别地，对于预防和/或治疗例如神经变性疾病，淀粉样血管病，由脑血管障碍引起的神经障碍等是有效的。

    Benzothiepin derivatives, process for the preparation of the same and uses thereof
    2.
    发明授权
    Benzothiepin derivatives, process for the preparation of the same and uses thereof 失效
    苯并噻吩衍生物，其制备方法及其用途

    公开(公告)号：US06355672B1

    公开(公告)日：2002-03-12

    申请号：US09744857

    申请日：2001-01-30

    申请人： Tsuneo Yasuma ,  Haruhiko Makino ,  Akira Mori

    发明人： Tsuneo Yasuma ,  Haruhiko Makino ,  Akira Mori

    IPC分类号： C07D33708

    CPC分类号： C07D263/44 ,  C07D211/88 ,  C07D233/74 ,  C07D277/04 ,  C07D295/135 ,  C07D495/04

    摘要： The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

    摘要翻译： 本发明提供下式的化合物：其中环A是任选取代的苯环; R1是任选取代的非芳族杂环基; R2和R3独立地为氢原子或任选取代的烃基; n为0-3的整数; 或其盐，其可用作具有成骨促进作用的药物和软骨素促进作用。本发明涉及具有抑制淀粉样蛋白b蛋白的产生和/或分泌的优异效果的胺化合物及其制备和用途。 特别地，对于预防和/或治疗例如神经变性疾病，淀粉样血管病，由脑血管障碍引起的神经障碍等是有效的。

    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：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
    4.
    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。

    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 derivatives and their use
    7.
    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。

    Thienopyridine derivatives and their use
    9.
    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。