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    6-substituted isoquinoline derivatives
    3.
    发明授权
    6-substituted isoquinoline derivatives 有权
    6-取代的异喹啉衍生物

    公开(公告)号：US07893088B2

    公开(公告)日：2011-02-22

    申请号：US11839703

    申请日：2007-08-16

    申请人： Peter Christopher Ray ,  Steven Laats ,  John Richard Morphy ,  Brad Sherborne

    发明人： Peter Christopher Ray ,  Steven Laats ,  John Richard Morphy ,  Brad Sherborne

    IPC分类号： C07D217/00 ,  A61K31/47

    CPC分类号： C07D217/22 ,  C07D217/24

    摘要： The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R4 is H or (C1-6)alkyl, optionally substituted with halogen, (C3-7)cycloalkyl, (C6-10)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C6-10)aryl and heterocyclic ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy or halogen; R5 is H or (C1-4)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.

    摘要翻译： 本发明涉及具有通式I的6-取代的异喹啉衍生物，其中X是O，S或NH; Y是OH或NH 2; m为0,1或2; n为0或1; o为0或1; 当Y为NH 2时，R 1为H; 或者当Y为OH时，R 1为H，（C 1-4）烷基或卤素; R2和R3独立地是H，（C1-4）烷基或卤素; R4是H或（C 1-6）烷基，任选地被卤素，（C 3-7）环烷基，（C 6-10）芳基或饱和的5-或6-元杂环包含1-3个独立地选自O， S和N，（C 6-10）芳基和杂环任选被（C 1-4）烷基，（C 1-4）烷氧基或卤素取代; R5是H或（C1-4）烷基; 或其药学上可接受的盐，条件是其中X为O，Y为OH，n为0且m + o = 2的式I化合物排除于包含该化合物的药物组合物中，以及使用 的所述6-取代的异喹啉衍生物用于制备用于治疗ROCK-1相关疾病如青光眼，高血压和动脉粥样硬化的药物。

    6-SUBSTITUTED ISOQUINOLINE DERIVATIVES
    4.
    发明申请
    6-SUBSTITUTED ISOQUINOLINE DERIVATIVES 有权
    6取代的异喹啉衍生物

    公开(公告)号：US20080045566A1

    公开(公告)日：2008-02-21

    申请号：US11839703

    申请日：2007-08-16

    申请人： Peter Christopher Ray ,  Steven Laats ,  John Richard Morphy ,  Brad Sherborne

    发明人： Peter Christopher Ray ,  Steven Laats ,  John Richard Morphy ,  Brad Sherborne

    IPC分类号： A61K31/472 ,  A61P27/06 ,  C07D217/00

    CPC分类号： C07D217/22 ,  C07D217/24

    摘要： The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R4 is H or (C1-6)alkyl, optionally substituted with halogen, (C3-7)cycloalkyl, (C6-10)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C6-10)aryl and heterocyclic ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy or halogen; R5 is H or (C1-4)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.

    摘要翻译： 本发明涉及具有通式I的6-取代的异喹啉衍生物，其中X是O，S或NH; Y是OH或NH 2; m为0,1或2; n为0或1; o为0或1; R 1是H，当Y是NH 2时; 或R 1为H，（C 1-4烷基）烷基或卤素，当Y为OH时; R 2和R 3独立地是H，（C 1-4烷基）烷基或卤素; R 4是H或（C 1-6 - ）烷基，任选被卤素，（C 3-7）环烷基取代，（C 1 -C 6） （C 6-10）芳基或饱和的5-或6-元杂环，其包含1-3个独立地选自O，S和N的杂原子， 芳基和杂环任选被（C 1-4烷基）烷基，（C 1-4-4烷基）烷氧基或卤素取代; R 5是H或（C 1-4烷基）烷基; 或其药学上可接受的盐，条件是其中X为O，Y为OH，n为0且m + o = 2的式I化合物排除于包含该化合物的药物组合物中，以及使用 的所述6-取代的异喹啉衍生物用于制备用于治疗ROCK-1相关疾病如青光眼，高血压和动脉粥样硬化的药物。