首页> 外国专利> Derivatives of substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido 1,2-a pyrimidine-4-one and 7-pyrimidinyl-2,3-dihydroimidazo 1,2-a pyrimidine-5 (1H) It is for neurodegenerative disorders

Derivatives of substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido 1,2-a pyrimidine-4-one and 7-pyrimidinyl-2,3-dihydroimidazo 1,2-a pyrimidine-5 (1H) It is for neurodegenerative disorders

机译:取代的2-嘧啶基-6,7,8,9-四氢嘧啶基[1,2-a]嘧啶-4-酮和7-嘧啶基-2,3-二氢咪唑基[1,2-a]嘧啶-5(1H )用于神经退行性疾病

摘要

This invention relates to a pyrimidone derivative represented by formula (I), or a salt thereof, where X is two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-6 alkyl group and a hydrogen atom; Y represents a bond, ethenylene group, ethynylene group, oxygen atom, sulfur atom, sulfonyl group, sulfoxide group, carbonyl group, possibly substituted nitrogen atom; or a possibly substituted methylene group; R1 is a possibly substituted pyrimidine group; R2 may be a C1-6 alkyl group optionally substituted by Saryloxy or Sarylamino; Stsikloalkilnuyu group Salkiltiogruppu, Salkoksigruppu, Spergalogenirovannuyu alkyl group Cgalogenirovannuyu alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indane ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or imidazole ring; R3 and R4 each independently represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a Salkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom. This invention also relates to a drug containing said derivative or a salt thereof as an active ingredient, which is used for prophylactic and / or therapeutic treatment of a neurodegenerative disease caused by the abnormal activity of GSK3β3 or GSK3β3 and cdk5 / p25, such as Alzheimer's disease.
机译:本发明涉及由式(I)表示的嘧啶酮衍生物或其盐,其中X是两个氢原子,一个硫原子,一个氧原子或一个C1-6烷基和一个氢原子; Y表示键,亚乙烯基,亚乙炔基,氧原子,硫原子,磺酰基,亚砜基,羰基,可能被取代的氮原子;或可能取代的亚甲基; R1是可能取代的嘧啶基; R2可以是任选地被芳基氧基或芳基氨基取代的C1-6烷基; Stsikloalkilnuyu基团Salkiltiogruppu,Salkoksigruppu,Spergalogenirovannuyu烷基Cgalogenirovannuyu烷基,苯硫基,苄基,苯环,茚满环,5,6,7,8-四氢萘环,萘环,吡啶环,吡咯环,噻吩环,呋喃环或咪唑环; R 3和R 4各自独立地表示氢原子,C 1-6烷基,羟基,烷氧基或卤原子; R 5代表氢原子,C 1-6烷基或卤素原子。本发明还涉及含有所述衍生物或其盐作为有效成分的药物,用于预防和/或治疗由GSK3β3或GSK3β3和cdk5 / p25的异常活性引起的神经退行性疾病,例如阿尔茨海默氏病。疾病。

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号