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16 条记录 (耗时 0.05 秒)

    Tetrahydrothienopyridine derivatives, furo and pyrrolo analogs thereof and their preparation and uses for inhibiting blood platelet aggregation
    12.
    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。

    Benzamidine derivatives
    15.
    发明授权
    Benzamidine derivatives 失效
    苄脒衍生物

    公开(公告)号：US07030138B2

    公开(公告)日：2006-04-18

    申请号：US10679215

    申请日：2003-10-03

    申请人： Koichi Fujimoto ,  Naoki Tanaka ,  Ikuko Shimada ,  Fumitoshi Asai

    发明人： Koichi Fujimoto ,  Naoki Tanaka ,  Ikuko Shimada ,  Fumitoshi Asai

    IPC分类号： C07D211/06 ,  A61K31/445

    CPC分类号： C07D451/06 ,  A61K31/402 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/55 ,  C07D207/12 ,  C07D207/22 ,  C07D207/48 ,  C07D211/46 ,  C07D211/72 ,  C07D211/96 ,  C07D223/08 ,  C07D223/12 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

    摘要： A compound of a formula (1) and pharmacologically acceptable salts thereof: wherein R1 represents hydrogen, halogen, alkyl or hydroxyl; R2 represents hydrogen or halogen; R3 represents hydrogen, alkyl, hydroxyl, carboxyalkyl, alkoxycarbonylalkyl, alkylsulfonyl, alkoxycarbonylalkylsulfonyl, craboxyalkylsulfonyl or carboxyalkylcarbonyl; each of R4 and R5 represents hydrogen, halogen, alkyl, carbamoyl, alkoxy, carboxyl, alkoxycarbonyl, monoalkylcarbamoyl or dialkylcarbamoyl; R6 represents a heterocycle, hydrogen, alkyl, cycloalkyl, aralkyl, carboxyalkyl, alkoxycarbonyalkyl, aliphatic or aromatic acyl, carbamoyl, alkylsulfonyl, aryl, formimidoyl, 1-iminoalkyl, N-alkylforminidoyl or iminoarylmethyl; each of R7 and R8 represents hydrogen or alkyl; n represents 0, 1 or 2. The compound exhibits excellent activated blood coagulation factor X inhibitory activity and prevents or treats blood coagulation-related diseases.

    摘要翻译： 式（1）的化合物及其药理学上可接受的盐：其中R 1表示氢，卤素，烷基或羟基; R 2表示氢或卤素; R 3表示氢，烷基，羟基，羧基烷基，烷氧基羰基烷基，烷基磺酰基，烷氧基羰基烷基磺酰基，烷氧基烷基磺酰基或羧基烷基羰基; R 4和R 5各自表示氢，卤素，烷基，氨基甲酰基，烷氧基，羧基，烷氧基羰基，单烷基氨基甲酰基或二烷基氨基甲酰基; R 6表示杂环，氢，烷基，环烷基，芳烷基，羧基烷基，烷氧基羰基烷基，脂族或芳族酰基，氨基甲酰基，烷基磺酰基，芳基，亚氨基，1-亚氨基烷基，N-烷基亚甲酰基或亚氨基芳基甲基; R 7和R 8中的每一个代表氢或烷基; n表示0,1或2.该化合物表现出优异的活化凝血因子X抑制活性并预防或治疗凝血相关疾病。

    Benzamidine derivatives
    16.
    发明授权
    Benzamidine derivatives 失效
    苄脒衍生物

    公开(公告)号：US06555556B1

    公开(公告)日：2003-04-29

    申请号：US10132042

    申请日：2002-04-25

    申请人： Koichi Fujimoto ,  Fumitoshi Asai ,  Hayao Matsuhashi

    发明人： Koichi Fujimoto ,  Fumitoshi Asai ,  Hayao Matsuhashi

    IPC分类号： A61K31445

    CPC分类号： C07D211/46

    摘要： Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: wherein R1 represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; R2 represents a hydrogen atom, a halogen atom or an alkyl group, R3 represents a hydrogen atom, an optionally substituted alkyl group, an aralkyl group, an optionally substituted alkanoyl group or an optionally substituted alkylsulfonyl group, R4 and R5 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group, and R6 represents a substituted pyrrolidine group or substituted piperidine group.

    摘要翻译： 式（I）的苄脒衍生物或其药学上可接受的盐对因子Xa具有优异的抑制活性，可用于治疗或预防凝血障碍：其中R1表示氢原子，卤素原子，烷基或羟基; R2表示氢原子，卤素原子或烷基，R3表示氢原子，可以具有取代基的烷基，芳烷基，可以具有取代基的烷酰基或任意取代的烷基磺酰基，R4和R5与 各自表示氢原子，卤素原子，任选取代的烷基，烷氧基，羧基，烷氧基羰基或任选取代的氨基甲酰基，R 6表示取代的吡咯烷基或取代的哌啶基 。