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98 条记录 (耗时 0.04 秒)

    Lactol derivatives, their production and use
    5.
    发明授权
    Lactol derivatives, their production and use 失效
    乳糖衍生物，其生产和使用

    公开(公告)号：US5496834A

    公开(公告)日：1996-03-05

    申请号：US300738

    申请日：1994-09-02

    申请人： Takashi Sohda ,  Yukio Fujisawa ,  Satoru Oi ,  Junji Mizoguchi

    发明人： Takashi Sohda ,  Yukio Fujisawa ,  Satoru Oi ,  Junji Mizoguchi

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/078 ,  A61K31/44 ,  A61K31/35 ,  A61K31/40

    CPC分类号： C07K5/06139 ,  C07K5/06043 ,  A61K38/00

    摘要： The present invention provides novel compound of the formulas (Ia) or (I): ##STR1## wherein Q is one or two amino acid residues which may be substituted; R.sup.3 is a carboxyl group which may be esterified or an acyl group; A is an alkylene group; B is hydrogen or an alkyl group which may be substituted or an acyl group; or a salt thereof; ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a hydrocarbon residue which may be substituted; R.sup.3, A and B have the same definitions as those shown above; m and n each is 0 or 1; provided that where both m and n are both equal to 0, R.sup.3 is a carboxyl group which may be esterified or an acyl group having not less than 7 carbon atoms; or a salt thereof.The compound (Ia) or (I) shows cathepsin L inhibitory and bone resorption inhibitory activities and are useful as a prophylactic/therapeutic agent for osteoporosis.

    摘要翻译： 本发明提供新的式（Ia）或（I）化合物：其中Q是一个或两个可被取代的氨基酸残基; R3是可被酯化的羧基或酰基; A是亚烷基; B是氢或可以被取代的烷基或酰基; 或其盐; （I）其中R 1和R 2可以相同或不同，各自为氢或可被取代的烃残基; R3，A和B具有与上述相同的定义; m和n各自为0或1; 条件是当m和n都等于0时，R 3是可被酯化的羧基或具有不少于7个碳原子的酰基; 或其盐。 化合物（Ia）或（I）表示组织蛋白酶L抑制和骨吸收抑制活性，可用作骨质疏松症的预防/治疗剂。

    Condensed thiadiazole derivative, method of its production, and use thereof
    6.
    发明授权
    Condensed thiadiazole derivative, method of its production, and use thereof 失效
    缩合噻二唑衍生物，其制备方法及其用途

    公开(公告)号：US5550138A

    公开(公告)日：1996-08-27

    申请号：US039579

    申请日：1993-03-23

    申请人： Takashi Sohda ,  Zen-ichi Terashita ,  Yu Momose ,  Yukio Fujisawa ,  Junji Mizoguchi

    发明人： Takashi Sohda ,  Zen-ichi Terashita ,  Yu Momose ,  Yukio Fujisawa ,  Junji Mizoguchi

    IPC分类号： C07D513/04 ,  A61K31/435

    CPC分类号： C07D513/04

    摘要： (1) a compound represented by the following formula (I): ##STR1## wherein R represents a hydrocarbon group or heterocyclic group which may be substituted; the ring A represents a pyridine ring having a substituent or a thiazole ring which may be substituted; or a pharmaceutically acceptable salt thereof, and a method of its production, and(2) an endothelin receptor antagonist, an cathepsin B inhibitor or a bone resorption suppressor having as an active ingredient a compound represented by the following formula (I'): ##STR2## wherein R has the same definition as in term (1); the ring A' represents a pyridine ring or thiazole ring which may be substituted; or a pharmaceutically acceptable salt thereof.

    摘要翻译： （1）由下式（I）表示的化合物：其中R表示可被取代的烃基或杂环基; 环A表示具有取代基的吡啶环或可被取代的噻唑环; 或其药学上可接受的盐及其制备方法，和（2）作为活性成分的下式（I'）表示的化合物的内皮素受体拮抗剂，组织蛋白酶B抑制剂或骨吸收抑制剂： （I'）其中R与术语（1）具有相同的定义; 环A'表示可被取代的吡啶环或噻唑环; 或其药学上可接受的盐。

    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：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。