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    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。

    CYCLIC AMINE DERIVATIVE HAVING SUBSTITUTED ALKYL GROUP
    10.
    发明申请
    CYCLIC AMINE DERIVATIVE HAVING SUBSTITUTED ALKYL GROUP 审中-公开
    具有取代的烷基的环胺衍生物

    公开(公告)号：US20090306059A1

    公开(公告)日：2009-12-10

    申请号：US11915522

    申请日：2006-05-26

    申请人： Tomio Kimura ,  Naoki Tanaka ,  Hiroyuki Kobayashi ,  Atsuhiro Sugidachi

    发明人： Tomio Kimura ,  Naoki Tanaka ,  Hiroyuki Kobayashi ,  Atsuhiro Sugidachi

    IPC分类号： A61K31/541 ,  C07D413/06 ,  A61K31/5377 ,  C07D417/06 ,  C07D401/06 ,  A61K31/4545 ,  A61P7/02

    CPC分类号： F16D3/2233 ,  F16D2003/22309 ,  Y10T403/32655

    摘要： A compound having the general formula (I), pharmacologically acceptable salts thereof or prodrugs thereof: [wherein R1 represents a hydrogen atom, a C1-C6 alkyl group which may be substituted, a C3-C6 cycloalkyl group which may be substituted, a C1-C6 alkoxy group which may be substituted or a C6-C10 aryl group which may be substituted; R2 represents a hydrogen atom, a halogen atom, a carboxy group, a C2-C7 alkoxycarbonyl group, a carbamoyl group, a cyano group, a C1-C6 alkyl group, a halogeno C1-C6 alkyl group, a C1-C6 alkyl group substituted by a heteroaryl group, a C1-C6 alkoxy group, a halogeno C1-C6 alkoxy group, a hydroxy C1-C6 alkyl group, a C2-C12 alkoxyalkyl group, a formyl group, a C2-C7 alkanoyl group, a C4-C7 cycloalkylcarbonyl group, a C2-C7 alkylcarbamoyl group, a di(C1-C6 alkyl)carbamoyl group, a group of formula R4—CO—CR5R6—(CH2)m—, a group of formula R7—CO—(CH2)l—N(R8)— or a sulfamoyl C1-C6 alkyl group; R3 represents a substituted C1-C6 alkyl group, a heterocyclyl group or a heterocyclyl group substituted with 1 to 5 substituents; X1, X2, X3, X4 and X5 each independently represents a hydrogen atom, a halogen atom, an amino group, a carboxy group, a carbamoyl group, a cyano group, a nitro group, a C1-C6 alkyl group, a halogeno C1-C6 alkyl group, a C1-C6 alkoxy group, or a halogeno C1-C6 alkoxy group; and n represents an integer of 0 to 2].

    摘要翻译： 具有通式（I）的化合物，其药学上可接受的盐或其前药：其中R1表示氢原子，可被取代的C1-C6烷基，可被取代的C3-C6环烷基，C1 可被取代的-C6烷氧基或可被取代的C6-C10芳基; R2表示氢原子，卤素原子，羧基，C2-C7烷氧基羰基，氨基甲酰基，氰基，C1-C6烷基，卤代C1-C6烷基，C1-C6烷基 被杂芳基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基，羟基C 1 -C 6烷基，C 2 -C 12烷氧基烷基，甲酰基，C 2 -C 7烷酰基， C7环烷基羰基，C2-C7烷基氨基甲酰基，二（C1-C6烷基）氨基甲酰基，式R4-CO-CR5R6-（CH2）m-的基团，式R7-CO-（CH2） （R8） - 或氨磺酰基C1-C6烷基; R 3表示取代的C 1 -C 6烷基，杂环基或被1至5个取代基取代的杂环基; X1，X2，X3，X4和X5各自独立地表示氢原子，卤素原子，氨基，羧基，氨基甲酰基，氰基，硝基，C1-C6烷基，卤代C1 C 1-6烷基，C 1 -C 6烷氧基或卤代C 1 -C 6烷氧基; n表示0〜2的整数]。