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    • 22. 发明授权
    • Thienopyridine derivatives and their use
    • 噻吩并吡啶衍生物及其用途
    • US6046189A
    • 2000-04-04
    • US860452
    • 1997-06-26
    • Takashi SohdaHaruhiko MakinoAtsuo Baba
    • Takashi SohdaHaruhiko MakinoAtsuo Baba
    • A61K31/435C07D495/14C07D493/14A61K31/55C07D223/00
    • C07D495/14
    • 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.
    • 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。