发明授权
EP1708713B1 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-BENZO(D)(1,3)OXAZIN-2-ONE DERIVATIVES AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR (5-HT) FOR THE TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM 有权
1-苄基-5-哌嗪-1-基-3,4-二氢-1H-喹唑啉-2-酮衍生物及其各自-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)恶嗪-2-酮衍生物作为5-羟色胺受体(5-HT)对于中枢神经系统疾病治疗的调节剂

  • 专利标题: 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-BENZO(D)(1,3)OXAZIN-2-ONE DERIVATIVES AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR (5-HT) FOR THE TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM
  • 专利标题(中): 1-苄基-5-哌嗪-1-基-3,4-二氢-1H-喹唑啉-2-酮衍生物及其各自-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)恶嗪-2-酮衍生物作为5-羟色胺受体(5-HT)对于中枢神经系统疾病治疗的调节剂
  • 申请号: EP05700747.8
    申请日: 2005-01-07
  • 公开(公告)号: EP1708713B1
    公开(公告)日: 2008-03-12
  • 发明人: SUI, MengZHAO, Shu-Hai
  • 申请人: F. Hoffmann-la Roche AG
  • 申请人地址: 124 Grenzacherstrasse 4070 Basel CH
  • 专利权人: F. Hoffmann-la Roche AG
  • 当前专利权人: F. Hoffmann-la Roche AG
  • 当前专利权人地址: 124 Grenzacherstrasse 4070 Basel CH
  • 代理机构: Wasner, Marita
  • 优先权: US537080P 20040116
  • 国际公布: WO2005067933 20050728
  • 主分类号: A61K31/517
  • IPC分类号: A61K31/517 A61K31/5415 A61K31/536 C07D239/80 C07D285/16 C07D265/18 C07D405/06 A61P25/18
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-BENZO(D)(1,3)OXAZIN-2-ONE DERIVATIVES AS MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR (5-HT) FOR THE TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM
摘要:
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 -(CRaRb)r- or -SO2-, wherein r is from 0 to 2 and each of Ra and Rb is independently hydrogen or alkyl; X is CH or N; R2 is optionally substituted aryl or optionally substituted heteroaryl; preferably R2 is aryl, and more preferably phenyl optionally substituted by one or more trifluoromethyl, halo, cyano, C1-C6 alkyl or C1-C6 alkoxy; A is -NR3- or -O- wherein R3 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.
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