首页> 外国专利> (Pyrido / thieno) - f -oxazepin-5-one derivative, pharmaceutical composition, use of a (pyrido / thieno) - f -oxazepin-5-one derivative, and method of treating a disease neurological disorder or a psychiatric disorder

(Pyrido / thieno) - f -oxazepin-5-one derivative, pharmaceutical composition, use of a (pyrido / thieno) - f -oxazepin-5-one derivative, and method of treating a disease neurological disorder or a psychiatric disorder

机译:(吡啶并/噻吩)-[f]-氧杂嗪-5-酮衍生物,药物组合物,(吡啶并/噻吩并)-[f]-氧杂嗪-5-酮衍生物的用途以及治疗疾病的神经系统疾病或方法精神病

摘要

"(FIRY / TIENO) DERIVATIVE - [F] -OXAZEPIN-5-ONA, PHARMACEUTICAL COMPOSITION, USE OF A (FIRY / TIENO) - [F] -OXAZEPIN-5-ONA, AND, TREATMENT METHOD OF A NEUROLOGICAL DISEASE OR PSYCHIATRIC DISORDER ". The present invention relates to (pyrido / thieno) [f] -oxazepin-5-one derivatives having General Formula I wherein R 1, R 2 and R 3 are independently H or C (C) alkyl. ~ 1-4 ~); Ar represents a fused thiophene or pyridine ring optionally substituted by one or more substituents selected from C1-4 alkyl, C1-4 alkyloxy, C1-4 alkyloxy and C1-4 alkyl ~ 1-4 ~), CF ~ 3 ~, halogen, nitro, cyano, NR ^ 4 ^ R ^ 5 ^, NR ^ 4 ^ COR ^ 6 ^ and CONR ^ 4 ^ R ^ 5 ^, R ^ 4 ^ e R 5 are independently H or C 1-4 alkyl; or R 4 and R 5 form together with the nitrogen atom to which they are attached a 5 or 6 membered saturated heterocyclic ring, optionally containing another heteroatom selected from O, S or NR 6 6; R6 is C (1-4) alkyl; A represents the residue of a 4- to 7-membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted by 1 to 3 substituents selected from (1-4C) alkyl, (1-4C) alkyloxy ), hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and the use of these (pyrido / thieno) [f] -oxazepin-5-one derivatives in the treatment of neurological disorders and psychiatric disorders that are responsive to the intensification of mediated synaptic responses. AMPA receptors in the central nervous system.
机译:“(FIRY / TIENO)衍生物-[F]-OXAZEPIN-5-ONA,药物成分,(FIRY / TIENO)-[F]-OXAZEPIN-5-ONA的使用,以及神经疾病或精神病的治疗方法DISORDER”。本发明涉及通式(I)的R 1,R 2和R 3独立地为H或C(C)烷基的(吡啶基/噻吩并)[f]-氧杂庚酮-5-酮衍生物。 〜1-4〜); Ar表示稠合的噻吩或吡啶环,其任选地被一个或多个选自以下的取代基取代:C1-4烷基,C1-4烷氧基,C1-4烷氧基和C1-4烷基〜1-4〜,CF〜3〜,卤素,硝基,氰基,NR ^ 4 ^ R ^ 5 ^,NR ^ 4 ^ COR ^ 6 ^和CONR ^ 4 ^ R ^ 5 ^,R ^ 4 ^ e R 5独立地为H或C 1-4烷基; R 4和R 5与它们所连接的氮原子一起形成5或6元饱和杂环,任选地含有选自O,S或NR 6 6的另一个杂原子;或R6为C(1-4)烷基; A表示4至7元饱和杂环的残基,其任选地含有氧原子,该环任选地被选自(1-4C)烷基,(1-4C)烷氧基),羟基的1-3个取代基取代。 ,卤素和氧代;或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物,以及这些(吡啶并/噻吩)[f]-氧杂庚酮-5-酮衍生物在治疗对介导的突触反应的增强有反应的神经系统疾病和精神疾病中的用途。 。中枢神经系统中的AMPA受体。

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