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    • 4. 发明申请
      WO2008033757A2 2-(1-OXO-1H-ISOQUINOLIN-2-YL) ACETAMIDE DERIVATIVES 审中-公开
    • 2-(1-OXO-1H-ISOQUINOLIN-2-YL) ACETAMIDE DERIVATIVES
    • 2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物
    • WO2008033757A2
    • 2008-03-20
    • PCT/US2007/077999
    • 2007-09-10
    • N.V. ORGANON , LETOURNEAU, Jeffrey , CHAN, Jui, Hsiang , JOKIEL, Patrick , OHLMEYER, Michael , NEAGU, Irina , RIVIELLO, Christopher, Mark , MORPHY, John, Richard , NAPIER, Susan, Elizabeth , HO, Koc-kan
    • LETOURNEAU, Jeffrey , CHAN, Jui, Hsiang , JOKIEL, Patrick , OHLMEYER, Michael , NEAGU, Irina , RIVIELLO, Christopher, Mark , MORPHY, John, Richard , NAPIER, Susan, Elizabeth , HO, Koc-kan
    • A61K31/397 , A61K31/472 , A61P25/00 , C07D217/24
    • C07D217/24 , C07D401/12
    • The present invention relates to a 2-(1 -oxo-1 /-/-isoquinolin-2-yl)acetamide derivative of formula (I), wherein R1 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-2alkyl, C2-6alkenyl or C2-6alkynyl, said C1- 6alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-2alkyl being optionally substituted with one or more halogens; R2 is C6-10aryl optionally substituted with one to three substituents selected from halogen, hydroxy, cyano, C1-6alkyl, C3.6cycloalkyl, C1-6alkyloxy and C3.6cycloalkyloxy, said C1-6alkyl, C3-6 cycloalkyl, C1 -6 alkyloxy and C3-6cycloalkyloxy being optionally substituted with one or more halogens or R2 is a 5-10 membered heteroaryl ring system comprising a heteroatom selected from N, O, S and optionally substituted with a substituent selected from methyl, C1-6alkyloxy and halogen; R3 is an optional substituent selected from C1-6alkyl, C1-6alkyloxy and halogen, said C1-6alky and C1-6alkyloxy being optionally substituted with one or more halogens; R4 is a group located at the 6- or 7- position of the oxoisoquinoline ring and is selected from formulas (II, III, IV, V, VI, VII,) each R5 is independently H or C1-6alkyl or one of R5 when joined together with one of R6 or R7 forms a 4-7 membered heterocyclic ring; R6 and R7 are independently H, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-2alkyl, C6-10 aryl or C6-10arylC1-2alkyl; or R6 and R7 together with the nitrogen to which they are bonded form a 4 to 8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR10, said heterocyclic ring being optionally substituted with one or two substituents selected from halogen, hydroxyl, C1-6alkyl, C1-6alkyloxy, cyano and COOR11 and said heterocyclic ring being optionally fused at two adjacent carbon atoms to a phenyl ring; or one of R6 and R7 when joined together with one of R5 forms a 4-7 membered heterocyclic ring; or one of R6 and R7 when joined together with one of R8 forms a 5-6 membered heterocyclic ring; R8 is one or two substituents selected from H, C1-6alkyl, C1-6alkyloxy and halogen or one of R8 when joined together with one of R6 and R7 forms a 5-6 membered heterocyclic ring; or one of R8 when joined together with R9 forms a 5-6 membered ring R9 is H or C1-6alkyl or R9 when joined together with one of R8 forms a 5-6 membered ring; R10 is H, C1-6alkyl or C1-6acyl; R11 is H or C1-6alkyl; m is 2-4; n is 1-3; X is CH2, O, S, SO2 Or NR12; R12 is H, C1-6alkyl, C1 -6acyl or C6-10arylC1-2alkyl group, said C6-10arylC1-2alkyl group being optionally substituted with methyl or methoxy; Y is CH2, (CH2)2 or (CH2)3; Q, T, V and W are C or N with the proviso that one of Q, T, V and W is N and the others are C; Q', T and V are selected from C, O, N and S with the proviso that one of Q', T and V is O, N, or S and the others are C; or a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to a pharmaceutical composition comprising a 2-(1 -oxo-7/-/-isoquinolin-2- yl)acetamide derivative according to the present invention and its use in therapy.
    • 本发明涉及式（I）的2-（1-氧代-1-异喹啉-2-基）乙酰胺衍生物，其中R 1是C 1-6烷基，C 3-6环烷基，C 3-6环烷基C 1-2烷基，C 2 C 1-6烷基，C 3-6环烷基和任选被一个或多个卤素取代的C 3-6环烷基C 1-2烷基; R2是任选被1至3个选自卤素，羟基，氰基，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基和C 3-6环烷氧基的取代基取代的C 6-10芳基，所述C 1-6烷基，C 3-6环烷基，C 1-6烷氧基 任选被一个或多个卤素取代的C 3-6环烷氧基或R 2是包含选自N，O，S的杂原子并任选被选自甲基，C 1-6烷氧基和卤素的取代基取代的5-10元杂芳基环系统; R3是选自C 1-6烷基，C 1-6烷氧基和卤素的任选取代基，所述C 1-6烷基和C 1-6烷氧基任选被一个或多个卤素取代; R4是位于氧代异喹啉环的6-或7-位的基团，并且选自式（II，III，IV，V，VI，VII），每个R 5独立地为H或C 1-6烷基或R5中的一个 与R6或R7中的一个连接在一起形成4-7元杂环; R6和R7独立地为H，C1-6烷基，C3-6环烷基，C3-6环烷基C1-2烷基，C6-10芳基或C6-10芳基C1-2烷基; 或R6和R7与它们所键合的氮一起形成任选地包含另外的选自O，S和NR 10的杂原子部分的4至8元饱和或不饱和杂环，所述杂环任选被一个或两个选自以下的取代基取代： 卤素，羟基，C 1-6烷基，C 1-6烷氧基，氰基和COOR 11，并且所述杂环任选地在两个相邻碳原子处稠合成苯环; 当R 1和R 5中的一个与R 5中的一个连接在一起形成4-7元杂环时; 或者R 6和R 7中的一个与R8中的一个连接在一起形成5-6元杂环; R8是一个或两个选自H，C 1-6烷基，C 1-6烷氧基和卤素的取代基，或者当R 6和R 7中的一个连接在一起时，R 8中的一个形成5-6元杂环; 当R 8与R 9一起形成5-6元环时，R 8为H或C 1-6烷基或R 9，当与R 8中的一个连接在一起形成5-6元环时; R 10是H，C 1-6烷基或C 1-6酰基; R11为H或C1-6烷基; m为2-4; n为1-3; X是CH 2，O，S，SO 2或NR 12; R 12为H，C 1-6烷基，C 1-6酰基或C 6-10芳基C 1-2烷基，所述C 6-10芳基C 1-2烷基任选被甲基或甲氧基取代; Y是CH 2，（CH 2）2或（CH 2）3; Q，T，V和W为C或N，条件是Q，T，V和W之一为N，其余为C; Q'，T和V选自C，O，N和S，条件是Q'，T和V之一为O，N或S，其余为C; 或其药学上可接受的盐或溶剂合物。 本发明还涉及包含根据本发明的2-（1-氧代-7-异喹啉-2-基）乙酰胺衍生物及其在治疗中的用途的药物组合物。
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