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1. 发明申请

WO2005049600A1 BETA-LACTAMS FOR TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS疾病的BETA-LACTAMS
公开(公告)号：WO2005049600A1
公开(公告)日：2005-06-02
申请号：PCT/EP2004/012772
申请日：2004-11-10
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , DI FABIO, Romano , GIOVANNINI, Riccardo , PAIO, Alfredo , TRANQUILLINI, Maria, Elvira , MATTIOLI, Lucia
发明人： ALVARO, Giuseppe , DI FABIO, Romano , GIOVANNINI, Riccardo , PAIO, Alfredo , TRANQUILLINI, Maria, Elvira , MATTIOLI, Lucia
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present invention relates to novel compounds of formula (I) wherein ---- represents a single or a double bond; R represents a radical selected from formulae i), ii), iii) and iv) in which R 1 is halogen, cyano, C 1-4 alkyl, C 1-4 alkoxy, trifluoromethyl or trifluoromethoxy and p is zero or an integer from 1 to 3; R 2 represents hydrogen or C 1-4 alkyl; R 3 represents hydrogen, hydroxy or C 1-4 alkyl; R 4 represents hydrogen or R 4 together with R 3 represents =0 or =CH 2 ; R 5 represents phenyl, naphthyl, a 9 to 10 membered fused bicyclic heterocyclic group or a 5 or 6 membered heteroaryl group, wherein said groups are optionally substituted by 1 to 3 groups independently selected from trifluoromethyl, C 1-4 alkyl, hydroxy, cyano, C 1-4 alkoxy, trifluoromethoxy, halogen or S(O)qC 1-4 alkyl; R 6 and R 7 independently represent hydrogen, cyano, C 1-4 alkyl; R 8 is (CH 2 )rR 10 ; R 9 represents hydrogen, halogen, C 3-7 cycloalkyl, hydroxy, nitro, cyano or C 1-4 alkyl optionally substituted by one or two groups selected from halogen, cyano, hydroxy or C 1-4 alkoxy; R 10 represents hydrogen or C 3-7 cycloalkyl; n represents 1 or 2; q is 0, 1 or 2; r is 0 or an integer from 1 to 4; or a pharmaceutically acceptable salt or a solvate thereof, process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of the serotonin reuptake transporter protein.
摘要翻译：本发明涉及式（I）的新化合物，其中----表示单键或双键; R表示选自式i），ii），iii）和iv）中的基团，其中R 1为卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基或三氟甲氧基，p为0或1至3的整数 ; R2代表氢或C1-4烷基; R3表示氢，羟基或C1-4烷基; R4表示氢或R4，R3表示= 0或= CH2; R5表示苯基，萘基，9至10元稠合双环杂环基或5或6元杂芳基，其中所述基团任选被1至3个独立地选自三氟甲基，C 1-4烷基，羟基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）qC 1-4烷基; R6和R7独立地表示氢，氰基，C1-4烷基; R8为（CH2）rR10; R9代表氢，卤素，C3-7环烷基，羟基，硝基，氰基或任选被一个或两个选自卤素，氰基，羟基或C 1-4烷氧基的基团取代的C 1-4烷基; R 10表示氢或C 3-7环烷基; n表示1或2; q是0,1或2; r为0或1至4的整数; 或其药学上可接受的盐或溶剂合物，其制备方法及其用于治疗由粘蛋白介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白。

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