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    Substituted fused heterocyclic compound
    21.
    发明授权
    Substituted fused heterocyclic compound 有权
    取代稠合杂环化合物

    公开(公告)号：US06432993B1

    公开(公告)日：2002-08-13

    申请号：US09543667

    申请日：2000-04-07

    申请人： Takashi Fujita ,  Kunio Wada ,  Toshihiko Fujiwara

    发明人： Takashi Fujita ,  Kunio Wada ,  Toshihiko Fujiwara

    IPC分类号： A61K31425

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

    摘要： Substituted fused heterocyclic compounds of the formula (I) and pharmacologically acceptable salts thereof: wherein R1 is a group of the formula (II) or (III): R4 is a substituted phenyl or a pyridyl which may have a substituent. R5 is hydrogen or the like. R6 is hydrogen, a C1-6 alkyl group or the like. D is oxygen or sulfur. E is a CH group or nitrogen. R2 is hydrogen or the like. R3 is a 2,4-dioxothiazolidin-5-ylmethyl group or the like. A is a C1-6 alkylene group. B is oxygen or sulfur. These compounds and salts are useful as the active ingredient of pharmaceutical compositions which can be used to treat patients because these compounds and salts have excellent insulin-resistance improving action, lipid-peroxide-production inhibitory action, 5-lipoxygenase inhibitory action and the like.

    摘要翻译： 取代的式（I）的稠合杂环化合物及其药理学上可接受的盐：其中R 1是式（II）或（III）的基团：R 4是可以具有取代基的取代的苯基或吡啶基。 R5是氢等。 R6是氢，C1-6烷基等。 D是氧或硫。 E为CH基或氮。 R2是氢等。 R3是2,4-二氧代噻唑烷-5-基甲基等。 A是C 1-6亚烷基。 B是氧或硫。 这些化合物和盐可用作可用于治疗患者的药物组合物的活性成分，因为这些化合物和盐具有优异的抗胰岛素抵抗改善作用，脂质过氧化物产生抑制作用，5-脂肪氧合酶抑制作用等。

    BENZO-OR PYRIDO-IMIDAZOLE DERIVATIVE
    22.
    发明申请
    BENZO-OR PYRIDO-IMIDAZOLE DERIVATIVE 审中-公开
    苯并或吡唑并咪唑衍生物

    公开(公告)号：US20130165446A1

    公开(公告)日：2013-06-27

    申请号：US13696978

    申请日：2011-05-11

    申请人： Takashi Fujita ,  Hiroyoshi Horikoshi ,  Michael Anthony Cawthorne

    发明人： Takashi Fujita ,  Hiroyoshi Horikoshi ,  Michael Anthony Cawthorne

    IPC分类号： A61K31/5025 ,  A61K31/427 ,  C07D471/04 ,  A61K45/06 ,  C07D403/14 ,  A61K31/4184 ,  C07D487/04 ,  A61K31/4439 ,  C07D417/14 ,  A61K31/437

    CPC分类号： C07D417/14 ,  C07D403/14 ,  C07D471/04

    摘要： The present invention addresses the problem of finding a compound having both PPAR activation activity and angiotensin receptor antagonistic activity. The present invention is a benzo- or pyrido-imidazole derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, or a ester or amide thereof (where A is biphenyl methyl-imidazolyl, biphenyl methyl-benzimidazolyl, or the like, B is divalent benzimidazolyl or the like, C is carboxyl or the like, E is divalent phenyl, naphthyl, or the like, G is a dangling bond, oxygen, or the like, Q is oxygen or sulfur, n is an integer from 1 to 6, p is an integer from 1 to 6, V is a dangling bond, oxygen, or the like, and R is hydrogen, alkyl, or the like).

    摘要翻译： 本发明解决了找到具有PPAR活化活性和血管紧张素受体拮抗作用的化合物的问题。 本发明是由通式（I）表示的苯并或吡啶并咪唑衍生物，其药学上可接受的盐或其酯或酰胺（其中A为联苯甲基 - 咪唑基，联苯甲基 - 苯并咪唑基等， B是二价苯并咪唑基等，C是羧基等，E是二价苯基，萘基等，G是悬挂键，氧等，Q是氧或硫，n是1的整数 至6，p为1至6的整数，V为悬挂键，氧等，R为氢，烷基等）。

    Benzylidenethiazolidine derivatives and their use for the inhibition lipid peroxides
    24.
    发明授权
    Benzylidenethiazolidine derivatives and their use for the inhibition lipid peroxides 失效
    苄基噻唑烷衍生物及其用于抑制脂质过氧化物的用途

    公开(公告)号：US5387596A

    公开(公告)日：1995-02-07

    申请号：US95311

    申请日：1993-07-21

    申请人： Toyonori Takebayashi ,  Takayuki Onodera ,  Kazuo Hasegawa ,  Takashi Fujita ,  Takao Yoshioka

    发明人： Toyonori Takebayashi ,  Takayuki Onodera ,  Kazuo Hasegawa ,  Takashi Fujita ,  Takao Yoshioka

    IPC分类号： C07D417/12 ,  A61K31/425

    CPC分类号： C07D417/12

    摘要： Benzylidenethiazolidine compounds of formula (I): ##STR1## [in which R.sup.1, R.sup.2 and R.sup.5 are each hydrogen or alkyl; R.sup.3 and R.sup.4 are each hydrogen, alkyl, formyl, alkylcarbonyl, arylcarbonyl, carboxy, alkoxycarbonyl, aryloxycarbonyl, hydroxy, alkylcarbonyloxy, formyloxy, arylcarbonyloxy, optionally substituted alkoxy or halogen; W is methylene, carbonyl or a group of formula >C.dbd.N--OV, wherein V is hydrogen, alkylcarbonyl, arylcarbonyl or optionally substituted alkyl; and n is an integer of from 1 to 3] and salts thereof have the ability to inhibit the formation of lipid peroxide in the mammalian body, and can therefore be used for the treatment of arteriosclerosis and other diseases and disorders arising from an imbalance in the lipid peroxide level. They can also be used for the preparation of the corresponding benzylthiazolidine compounds, which have a generally greater hypoglycemic activity. Processes for the preparation of these compounds of formula (I) are also provided.

    摘要翻译： （I）的亚苄基噻唑烷化合物：其中R 1，R 2和R 5各自为氢或烷基; R 3和R 4各自为氢，烷基，甲酰基，烷基羰基，芳基羰基，羧基，烷氧基羰基，芳氧基羰基，羟基，烷基羰基氧基，甲酰氧基，芳基羰氧基，任选取代的烷氧基或卤素; W是亚甲基，羰基或式> C = N-OV的基团，其中V是氢，烷基羰基，芳基羰基或任选取代的烷基; 和_n为1〜3的整数]，其盐具有抑制哺乳动物体内脂质过氧化物形成的能力，因此可用于治疗由于不稳定引起的动脉硬化和其他疾病和障碍 脂质过氧化物水平。 它们也可用于制备相应的具有通常较高的降血糖活性的苄基噻唑烷化合物。 还提供了制备这些式（I）化合物的方法。

    Thiazolidine-2,4-dione hydrochloride salt, pharmaceutical compositions thereof and treatment method therewith
    28.
    发明授权
    Thiazolidine-2,4-dione hydrochloride salt, pharmaceutical compositions thereof and treatment method therewith 失效
    噻唑烷-2,4-二酮盐酸盐，其药物组合物及其处理方法

    公开(公告)号：US06706746B2

    公开(公告)日：2004-03-16

    申请号：US09991100

    申请日：2001-11-21

    申请人： Takashi Fujita ,  Toshihiko Fujiwara ,  Takashi Izumi

    发明人： Takashi Fujita ,  Toshihiko Fujiwara ,  Takashi Izumi

    IPC分类号： A61K31427

    CPC分类号： C07D417/12 ,  A61K31/427

    摘要： The present invention concerns the hydrochloride of the compound (5-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)benzyl]thiazolidin-2,4-dione) of the following structure (I) which exhibits an excellent hypoglycemic activity and the like. Said hydrochloride is useful when administered to patients for the treatment and/or prophylaxis of diabetes mellitus, hyperglycemia, impaired glucose tolerance and the like.

    摘要翻译： 本发明涉及以下结构（I）的化合物（5- [4-（6-甲氧基-1-甲基-1H-苯并咪唑-2-基甲氧基）苄基]噻唑烷-2,4-二酮）的盐酸盐， 表现出优异的降血糖活性等。当给予患者治疗和/或预防糖尿病，高血糖，葡萄糖耐量异常等时，所述盐酸盐是有用的。