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    NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF
    8.
    发明公开
    NOVEL DIBENZO[B,F]OXEPINE-10-CARBOXAMIDES AND PHARMACEUTICAL USES THEREOF 有权
    NEER DIBENZO [B，F] OXEPIN-10-CARBONSÄUREAMIDEUND DEREN PHARMAZEUTISCHE ANWENDUNGEN

    公开(公告)号：EP1651592A2

    公开(公告)日：2006-05-03

    申请号：EP04763454.8

    申请日：2004-07-23

    申请人： Novartis AG ,  Novartis Pharma GmbH

    发明人： AUBERSON, Yves ,  BETSCHART, Claudia ,  FLOHR, Stefanie ,  GLATTHAR, Ralf ,  SIMIC, Oliver ,  TINTELNOT-BLOMLEY, Marina ,  TROXLER, Thomas, J. ,  VANGREVELINGHE, Eric ,  VEENSTRA, Siem, Jacob

    IPC分类号： C07C235/40 ,  C07D313/14 ,  C07D267/20 ,  A61K31/335 ,  A61K31/395 ,  A61K31/165 ,  A61P25/28

    CPC分类号： C07D405/12 ,  C07C235/82 ,  C07C2603/32 ,  C07D313/14 ,  C07D407/12 ,  C07D413/12 ,  C07D453/02 ,  C07D491/04

    摘要： The present invention pertains to compounds of formula (I) wherein X is O, NH, N(C1-4)alkyl, CO or CHOH, Y is CH or N, A and B are each hydrogen or together form a second bond between the carbon atoms to which they are attached, R1 is hydrogen or (C1-4)alkyl, R2 is optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, aryl or heteroaryl, R3 is CH(Re)CONRaRb or (CH2)nNRc,Rd, n is 0, 1 or 2, Ra, Rb, Rc and Rd, independently, are hydrogen or optionally substituted (C1-8)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-4)alkyl, (C7-9)bicycloalkyl, 1-aza-(C7-9)bicycloalkyl, aryl, aryl(C1-4)alkyl, heteroaryl, heteroaryl(C1-4)alkyl or heterocyclyl, or Ra, Rb, Rc and Rd, together with the nitrogen to which they are attached, form an optionally substituted pyrrolidinyl, piperidino, morpholino or piperazinyl group, Re is (C1-8)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-7)cycloalkyl or (C3-7)cycloalkyl(C1-4)alkyl, and R4, R5, R6, R7, R8 and R9, independently, are hydrogen, (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkyl-SO2, cyano, nitro or halogen; to a process for the preparation of such compounds of formula (I), their use as a pharmaceuticals, especially in the treatment of neurological and vascular disorders related to beta-­amyloid generation and/or aggregation, and to pharmaceutical compositions and combinations comprising such compounds of formula (I).

    摘要翻译： 本发明涉及新型的二苯并[b，f]氧杂七环素-10-甲酰胺化合物，其用于制备式I化合物的方法，它们作为药物的用途，特别是用于治疗与β受体相关的神经和血管疾病， 淀粉样蛋白生成和/或聚集，以及包含式I化合物的药物组合物和组合。