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16 条记录 (耗时 0.032 秒)

    Tetrahydrothienopyridine derivatives, furo and pyrrolo analogs thereof and their preparation and uses for inhibiting blood platelet aggregation
    9.
    发明授权
    Tetrahydrothienopyridine derivatives, furo and pyrrolo analogs thereof and their preparation and uses for inhibiting blood platelet aggregation 失效
    四氢噻吩并吡啶衍生物，呋喃和吡咯类似物及其制备和用途，用于抑制血小板聚集

    公开(公告)号：US5288726A

    公开(公告)日：1994-02-22

    申请号：US941676

    申请日：1992-09-08

    申请人： Hiroyuki Koike ,  Fumitoshi Asai ,  Atsuhiro Sugidachi ,  Tomio Kimura ,  Teruhiko Inoue ,  Shigeyoshi Nishino ,  Yasunori Tsuzaki

    发明人： Hiroyuki Koike ,  Fumitoshi Asai ,  Atsuhiro Sugidachi ,  Tomio Kimura ,  Teruhiko Inoue ,  Shigeyoshi Nishino ,  Yasunori Tsuzaki

    IPC分类号： A61K31/435 ,  A61K31/135 ,  A61K31/365 ,  A61K31/4365 ,  A61P7/02 ,  C07D221/00 ,  C07D333/00 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A01K3/14 ,  C07D513/04

    CPC分类号： C07D471/04 ,  C07D491/04 ,  C07D495/04

    摘要： Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulfonyl, haloalkanesulfonyl or sulfamoyl; R.sup.2 is optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted cycloalkylcarbonyl, substituted benzoyl, or 5,6-dihydro-1,4,2-dioxazin-3-yl; R.sup.3 is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is --NH-- or oxygen or sulfur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.

    摘要翻译： 式（I）化合物：（*化学结构*）（I）其中：R1是氢，烷基，卤素，卤代烷基，羟基，烷氧基，卤代烷氧基，烷硫基，卤代烷硫基，氨基，烷酰基，卤代烷酰基，羧基，烷氧基羰基，氨基甲酰基， 氰基，硝基，烷磺酰基，卤代烷磺酰基或氨磺酰基; R 2是任选取代的烷酰基，任选取代的烯酰基，任选取代的环烷基羰基，取代的苯甲酰基或5,6-二氢-1,4,2-二恶嗪-3-基; R3是氢，羟基，任选取代的烷氧基，芳烷氧基，烷酰氧基，烯酰氧基，环烷基羰基氧基，芳基羰基氧基，烷氧基羰基氧基，芳烷氧基羰基氧基，邻苯二甲酰氧基，（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲氧基，（5- 苯基-2-氧代-1,3-二氧杂环戊烯-4-基）甲氧基，任选取代的氨基或硝基; Y是-NH-或氧或硫; n为1至5; 和所述式（I）化合物的互变异构体和盐具有抑制血小板聚集的能力，因此可用于治疗和预防血栓形成和栓塞。

    Acid addition salts of hydropyridine derivatives
    10.
    发明授权
    Acid addition salts of hydropyridine derivatives 失效
    氢化吡啶衍生物的酸加成盐

    公开(公告)号：US06693115B2

    公开(公告)日：2004-02-17

    申请号：US10329629

    申请日：2002-12-26

    申请人： Fumitoshi Asai ,  Taketoshi Ogawa ,  Hideo Naganuma ,  Naotoshi Yamamura ,  Teruhiko Inoue ,  Kazuyoshi Nakamura

    发明人： Fumitoshi Asai ,  Taketoshi Ogawa ,  Hideo Naganuma ,  Naotoshi Yamamura ,  Teruhiko Inoue ,  Kazuyoshi Nakamura

    IPC分类号： A61K314365

    CPC分类号： C07D495/04

    摘要： Acid addition salts of 2-acetoxy-5-(&agr;-cyclopropyl-carbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]-pyridine. The acid addition salts of tetrahydrothienopyridine derivatives of the present invention exhibit excellent oral absorption, metabolization into the active compound, and platelet aggregation-inhibiting effects, low toxicity, and excellent storage and handling stabilities, and are useful as medicaments, preferably preventive or therapeutic agents (particularly therapeutic agents) for diseases caused by a thrombus or an embolus, still more preferably preventive or therapeutic agents (particularly therapeutic agents) for thrombosis or embolism.

    摘要翻译： 2-乙酰氧基-5-（α-环丙基 - 羰基-2-氟苄基）-4,5,6,7-四氢噻吩并[3,2-c] - 吡啶的酸加成盐。 本发明的四氢噻吩并吡啶衍生物的酸加成盐表现出优异的口服吸收，代谢成活性化合物，抑制血小板聚集作用，毒性低，储存和处理稳定性优异，可用作药物，优选预防或治疗剂 （特别是治疗剂），还优选用于血栓形成或栓塞的预防或治疗剂（特别是治疗剂）。