作为5-羟色胺受体(5-ht)调节剂用于治疗中枢神经系统疾病的1-苄基-5-哌嗪-1-基-3,4二氢-1h-喹唑啉-2-酮衍生物和各个1h-苯并(1,2,6)噻二嗪-2,2-二氧化物和1,4-二氢-苯并(d)(1,3)*嗪-2-酮衍生物

1-benzyl-5-piperazin-1-yl-3,4-dihydro-1H- quinazolin-2-one derivatives and the respective 1H-benzo(1,2,6)thiadiazine-2,2-dioxide and 1,4-dihydro-benzene as modulators of the 5-hydroxytryptamine recept

Abstract

The invention relates to substituted quinazolinone compunds of formula (I) or a pharmaceutically acceptable salt thereof, wherein Y is C or S; m is 1 when Y is C and m is 2 when Y is S; n is 1 or 2; p is from 0 to 3; q is from 1 to 3; Z is -(CR<a>R)r- or -SO2-, wherein r is from 0 to 2 and each of R<a> and R is independently hydrogen or alkyl; X is CH or N; R<2> is optionally substituted aryl or optionally substituted heteroaryl; preferably R<2> is aryl, and more preferably phenyl optionally substituted by one or more trifluoromethyl, halo, cyano, C1-C6 alkyl or C1-C6 alkoxy; A is -NR<3>- or -O- wherein R<3> is: hydrogen; alkyl, acyl, amidoalkyl, hydroxyalkyl or alkoxyalkyl; the other substituents are defined in the claims. The compounds are modulators of the 5-hydroxytryptamine receptor and are useful for the treatment of diseases of the central nervous system such as psychoses, schizophrenia, manic depressions, neurological disorders, memory disorders, attention deficit disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, food uptake disorders, and Huntington's disease.
本发明涉及式(I)的被取代的喹唑啉酮化合物或其可药用的盐,其中Y是C或S;当Y是C时m是1,当Y是S时m是2;n是1或2;p是0至3;q是1至3;Z是-(CRaRb)r-或-SO2-,其中r是0至2且Ra和Rb各自独立地是氢或烷基;X是CH或N;R2是任选地被取代的芳基或任选地被取代的杂芳基;R2优选地是芳基,并且更优选地是任选地被一个或多个三氟甲基、卤素、氰基、C1-C6烷基或C1-C6烷氧基取代的苯基;A是-NR3-或-O-,其中R3是:氢、烷基、酰基、酰氨基烷基、羟基烷基或烷氧基烷基;其它取代基如权利要求书中所定义。该化合物是5-羟色胺受体的调节剂,可用于治疗中枢神经系统疾病如精神病、精神分裂症、躁狂抑郁症、神经障碍、记忆障碍、注意力缺陷障碍、帕金森病、肌萎缩性侧索硬化、阿尔茨海默病、进食障碍和亨廷顿舞蹈病。

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