7-(2-dimethylamino-ethoxy)-3H-quinazolin-4-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 7-(2-dimethylamino-ethoxy)-3H-quinazolin-4-one
• 英文别名: 7-(2-Dimethylaminoethoxy)-3H-quinazolin-4-one；7-[2-(dimethylamino)ethoxy]-3H-quinazolin-4-one
• 化学式: C₁₂H₁₅N₃O₂
• 分子量: 233.27
• InChiKey: BCYQCEIXJALECV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  53.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  N,N-二甲基乙醇胺 、 7-氟-4-喹唑啉酮 以affording 0.52 g (75% yield) of the title compound as a solid的产率得到7-(2-dimethylamino-ethoxy)-3H-quinazolin-4-one
  参考文献：
  名称：

  Use of Oxindole Derivatives in the Treatment of Dementia Related Diseases, Alzheimer's Disease and Conditions Associated with Glycogen Synthase Kinase-3

  摘要：

  本发明涉及一种新的使用氧吲哚衍生物的公式I，作为其自由碱基或药学上可接受的盐，[化学式应在此处插入。请参阅纸质副本。]其中R1、R2、R3、m和n的定义如权利要求1所述，以及新的化合物、其制备过程和用于制备中的新中间体，含有这些治疗活性化合物的药物组合物以及在疗法中使用这些活性化合物，特别是在预防和/或治疗与糖原合成酶激酶-3相关的痴呆症、阿尔茨海默病和条件方面的应用。

  公开号：

  US20090312322A1

文献信息

• Use of oxindole derivatives in the treatment of dementia related diseases, alzheimer's disease and conditions associated with glycogen synthase kinase-3
  申请人：Berg Stefan

  公开号：US20050070559A1

  公开（公告）日：2005-03-31

  The present invention relates to a new use of oxindole derivatives of formula I, as a free base or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , m and n arm as defined as in claim 1, as well as to new compounds, a process for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy, especially in the prevention and/or treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3.

  本发明涉及一种公式I的氧化吲哚衍生物的新用途，作为其自由碱基或药学上可接受的盐，其中R1、R2、R3、m和n的定义如权利要求书1所述。同时涉及新化合物、其制备方法以及用于制备新化合物的新中间体，含有所述治疗活性化合物的药物组合物以及所述活性化合物在治疗中的应用，特别是在预防和/或治疗与糖原合成酶激酶-3相关的痴呆症、阿尔茨海默病和条件方面的应用。
• Compounds for Treating Protein-Kinase Mediated Disorders
  申请人：Berdini Valerio

  公开号：US20080275029A1

  公开（公告）日：2008-11-06

  The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B; wherein the ring Q is a benzene ring; J 2 -J 1 is N═CR 7 or R 1a N—CO; G is OH or NR 5 R 6 ; E is CONR 7 , NR 7 CO, C(R 8 )═C(R 8 ) or (X) m (CR 8 R 8a ) n where X is O, S or NR 7 ; provided that when J 2 -J 1 is R 1a N—CO, E is other than NR 7 CO; m and n are each 0 or 1, where m+n=1 or 2; A is a bond and R 4 and R 4a are absent or A is a saturated optionally substituted C 1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N; R 1 , R 1a , R 2 , and R 3 are each H; halogen; C 1-6 hydrocarbyl optionally substituted by halogen, OH or C 1-2 alkoxy; CN; CONHR 8 ; NH 2 ; NHCOR 10 or NHCONHR 10 ; R 4 is H or C 1-4 alkyl; R 4a is H, C 1-4 alkyl or a group R 9 ; R 5 and R 6 are each selected from H, R 9 and C 1-4 hydrocarbyl optionally substituted by halogen, C 1-2 alkoxy or R 9 ; or NR 5 R 6 forms a saturated 4-7 membered monocyclic heterocyclic group; R 7 is H or C 1-4 alkyl; R 8 and R 8a each H or saturated C 1-4 hydrocarbyl optionally substituted by fluorine; R 9 is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R 4 , R 4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR 5 R 6 , R 4 and A form a saturated 4-7 membered monocyclic heterocycle; or R 4 , together with R 7 or R 8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR 5 R 6 and R 7 or R 8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R 10 is optionally substituted phenyl or benzyl.

  该发明提供了一种式(I)的化合物或其盐、溶剂化物、互变异构体或N-氧化物，用于治疗或预防由蛋白激酶A和/或蛋白激酶B介导的疾病状态或病情；其中，环Q是苯环；J2-J1是N═CR7或R1aN—CO；G是OH或NR5R6；E是CONR7、NR7CO、C(R8)═C(R8)或(X)m(CR8R8a)n，其中X为O、S或NR7；但当J2-J1是R1aN—CO时，E为除NR7CO之外的其他化合物；m和n各为0或1，其中m+n=1或2；A是键，R4和R4a不存在或A是饱和的可选取代的C1-7烃链连接基，在E和G之间具有最大链长为5个原子，链连接基中的一个碳原子可被O或N取代；R1、R1a、R2和R3各为H、卤素、C1-6烃基，可选取代卤素、OH或C1-2烷氧基、CN、CONHR8、NH2、NHCOR10或NHCONHR10；R4为H或C1-4烷基；R4a为H、C1-4烷基或基团R9；R5和R6各为H、R9和C1-4烃基，可选取代卤素、C1-2烷氧基或R9；或NR5R6形成饱和的4-7成员的单环杂环基；R7为H或C1-4烷基；R8和R8a各为H或饱和的C1-4烃基，可选取代氟；R9为含有最多3个环杂原子（选自N、O和S）的单环或双环碳环或杂环基；或R4、R4a和A一起形成饱和的单环4-7成员杂环；或NR5R6、R4和A形成饱和的4-7成员单环杂环；或R4与R7或R8和A、E一起形成4-7成员饱和的单环杂环；或NR5R6与R7或R8一起与A和E形成4-7成员饱和的单环杂环；R10为可选取代苯基或苄基。
• WO2006/51290
  申请人：——

  公开号：——

  公开（公告）日：——
• USE OF OXINDOLE DERIVATIVES IN THE TREATMENT OF DEMENTIA RELATED DISEASES, ALZHEIMER S DISEASE AND CONDITIONS ASSOCIATED WITH GLYCOGEN SYNTHASE KINASE-3
  申请人：AstraZeneca AB

  公开号：EP1458394A1

  公开（公告）日：2004-09-22
• COMPOUNDS FOR TREATING PROTEIN-KINASE MEDIATED DISORDERS
  申请人：Astex Therapeutics Limited

  公开号：EP1814552A2

  公开（公告）日：2007-08-08