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    1-amino-7-isoquinoline derivatives as serine protease inhibitors
    1.
    发明授权
    1-amino-7-isoquinoline derivatives as serine protease inhibitors 失效
    1-氨基-7-异喹啉衍生物作为丝氨酸蛋白酶抑制剂

    公开(公告)号：US06420438B1

    公开(公告)日：2002-07-16

    申请号：US09865418

    申请日：2001-05-29

    申请人： John Walter Liebeschuetz ,  William Alexander Wylie ,  Bohdan Waszkowycz ,  Christopher William Murray ,  Andrew David Rimmer ,  Pauline Mary Welsh ,  Stuart Donald Jones ,  Jonathan Michael Ernest Roscoe ,  Stephen Clinton Young ,  Phillip John Morgan ,  Nicholas Paul Camp ,  Andrew Philip Austin Crew

    发明人： John Walter Liebeschuetz ,  William Alexander Wylie ,  Bohdan Waszkowycz ,  Christopher William Murray ,  Andrew David Rimmer ,  Pauline Mary Welsh ,  Stuart Donald Jones ,  Jonathan Michael Ernest Roscoe ,  Stephen Clinton Young ,  Phillip John Morgan ,  Nicholas Paul Camp ,  Andrew Philip Austin Crew

    IPC分类号： A61K4360

    CPC分类号： C07D401/12 ,  A61K38/00 ,  C07D217/22 ,  C07D217/24 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07K5/0207

    摘要： The invention relates to serine protease inhibitor compounds of formula (I) where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl, alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycarbonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl; R2 is hydrogen, halo, methyl, amino, hydroxy, or oxo; and R is X—X—Y(R7)—L—Lp(D)n; wherein each X independently is C, N, O or S atom or a CO, CR1, C(R1)2 or NR1 group, at least one X being C, CO, CR1 or a C(R1)2 group; Y (the &agr;-atom) is a nitrogen atom or a CR1 group or Y and L taken together form a cyclic group; R7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylalkenyl, aralkyl, heteroaryl-alkyl, arylalkenyl, heteroarylalkenyl all optionally substituted by a group R1; L is an organic linker group containing 1 to 5 backbone atoms selected from C, N, O and S, or a branched alkyl or cyclic group; Lp is a lipophilic organic group selected from alkyl, heterocyclic, alkenyl, alkaryl, cycloalkyl, polycycloalkyl, cycloalkenyl, aryl, aralkyl or haloalkyl group or a combination of two or more such groups optionally substituted by one or more of oxa, thia, aza or R1 groups; D is a hydrogen bond donor group; and n is 0, 1 or 2 and salts thereof.

    摘要翻译： 本发明涉及式（I）的丝氨酸蛋白酶抑制剂化合物，其中R1是氢，卤素，氰基，硝基或羟基，氨基，烷氧基，烷基，氨基烷基，羟基烷基，硫醇，烷硫基，氨基磺酰基，烷氧基烷基，烷氧基羰基，酰氧基甲氧基羰基或烷基氨基 被羟基，烷基氨基，烷氧基，氧代，芳基，环烷基，氨基，卤素，氰基，硝基，硫醇，烷硫基，烷基磺酰基，烷基亚磺酰基，烷基磺酰氨基，烷基氨基磺酰基，卤代烷氧基和卤代烷基取代。 R2是氢，卤素，甲基，氨基，羟基或氧代; R为X-X-Y（R7）-L-Lp（D）n; 其中每个X独立地为C，N，O或S原子或CO，CR1，C（R1）2或NR1基团，至少一个X为C，CO，CR1或C（R1）2基团; Y（α原子）是氮原子或CR 1基，Y或L一起形成环状基团; R 7是选自烷基，烯基，单 - 或双 - 环烷基，芳基，杂芳基，单 - 或双环烷基烷基，单或双环烷基烯基，芳烷基，杂芳基 - 烷基，芳基烯基，杂芳基烯基的亲油基团，全部任选被基团R 1取代; L是含有1至5个选自C，N，O和S的骨架原子或支链烷基或环状基团的有机连接基团; Lp是选自烷基，杂环，烯基，烷芳基，环烷基，多环烷基，环烯基，芳基，芳烷基或卤代烷基中的亲脂性有机基团或两个或更多个这样的基团的组合，其任选被一个或多个氧杂，硫杂，氮杂或 R1组; D是氢键供体基团; 和n为0,1或2及其盐。