3-(2-chloro-pyrid-3-yl)-2-[(3-pyrrolidin-1-ylmethyl-phenylamino)-methyl]-3H-thieno[3,2-d]pyrimidin-4-one | 221152-52-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并嘧啶酮衍生物
• 英文名称: 3-(2-chloro-pyrid-3-yl)-2-[(3-pyrrolidin-1-ylmethyl-phenylamino)-methyl]-3H-thieno[3,2-d]pyrimidin-4-one
• 英文别名: 3-(2-Chloropyridin-3-yl)-2-[[3-(pyrrolidin-1-ylmethyl)anilino]methyl]thieno[3,2-d]pyrimidin-4-one
• CAS: 221152-52-9
• 化学式: C₂₃H₂₂ClN₅OS
• 分子量: 451.98
• InChiKey: IWMZUNJNUVYNBQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  31
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  89.1
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Quinazolin-4-one ampa antagonists
  申请人：Pfizer Products Inc.

  公开号：EP0884310A1

  公开（公告）日：1998-12-16

  The present invention relates to novel quinazolin-4-one derivatives of the formula I, wherein A is a benzo or thieno fused aromatic ring; B is phenyl, pyridyl or pyrimidyl; X is N or CH; Y and Z, taken together, i.e., Y-Z, are either -CH2NH- or -NHCH2-; R1 is selected from hydrogen, (C1-C6)alkyl optionally substituted with from one to three fluorine atoms, cyano, halo, amino, nitro and (C1-C6)alkoxy optionally substituted with from one to three fluorine atoms; R2 is halo, cyano, (C1-C6)alkyl optionally substituted with from one to three fluorine atoms, nitro, amino, (C1-C6)alkylthio, (C1-C6)alkoxy optionally substituted with from one to three fluorine atoms, hydroxy, H-C(=O)-, (C1-C6)alkyl-O-C(=O)- or NH2-C(=O)-; R3 and R4 are selected, independently, from hydrogen, (C1-C6)alkyl optionally substituted with from one to three fluorine atoms, halo, cyano, hydroxy (C1-C6)alkoxy optionally substituted with from one to three fluorine atoms, -C(=O)H, -CH2OR5 and -CH2NR6R7; pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.

  本发明涉及式 I 的新型喹唑啉-4-酮衍生物、 其中 A 是苯并或噻吩并芳香环； B 是苯基、吡啶基或嘧啶基 X 是 N 或 CH； Y 和 Z 合在一起，即 Y-Z，是-CH2NH-或-NHCH2-； R1 选自氢、任选被 1 至 3 个氟原子取代的(C1-C6)烷基、氰基、卤素、氨基、硝基和任选被 1 至 3 个氟原子取代的(C1-C6)烷氧基； R2 是卤素、氰基、任选被一至三个氟原子取代的(C1-C6)烷基、硝基、氨基、(C1-C6)烷硫基、任选被一至三个氟原子取代的(C1-C6)烷氧基、羟基、H-C(=O)-、(C1-C6)烷基-O-C(=O)- 或 NH2-C(=O)-； R3 和 R4 独立选自氢、任选被一至三个氟原子取代的 (C1-C6)烷基、卤素、氰基、任选被一至三个氟原子取代的羟基 (C1-C6)烷氧基、-C(＝O)H、-CH2OR5 和 -CH2NR6R7； 含有此类化合物的药物组合物 使用此类化合物治疗神经退行性疾病、精神疾病以及药物和酒精诱发的中枢和周围神经系统疾病。
• AMPA antagonists for the treatment of dyskinesias associated with dopamine agonist therapy
  申请人：Pfizer Products Inc.

  公开号：EP0900568A2

  公开（公告）日：1999-03-10

  The invention relates to a method of treating dyskinesias associated with dopamine agonist therapy in a mammal which comprises administering to said mammal a compound, as defined herein, which is an antagonist of the AMPA receptor. Dopamine agonist therapy, as referred to in the present invention, is generally used in the treatment of a central nervous system disorder such as Parkinson's disease.

  本发明涉及一种治疗哺乳动物多巴胺激动剂治疗相关运动障碍的方法，该方法包括向所述哺乳动物施用本文所定义的化合物，该化合物是 AMPA 受体的拮抗剂。本发明所述的多巴胺激动剂疗法通常用于治疗帕金森病等中枢神经系统疾病。
• Modulation of AMPA/kainate Receptors for the Treatment of Hypoglycemia
  申请人：Vanderklish Peter

  公开号：US20200397751A1

  公开（公告）日：2020-12-24

  Methods for modulating the levels of glucagon and blood glucose of a mammal are provided. In the subject methods, a positive allosteric modulator of AMPA/kainate receptors is administered to a host. The subject methods find use in applications where it is desired to increase one or both of the glucagon and blood glucose levels in a mammalian host. The subject methods find use in applications where it is desired to decrease the size, or breadth, of the circadian range of blood glucose levels in a mammalian host. The subject methods also find use in applications where it is desired to decrease the frequency, severity, or occurrence of hypoglycemia in a mammalian host. Finally, the subject method finds use in applications where it is desired to decrease the frequency, severity, or occurrence of nocturnal hypoglycemia in a mammalian host, particularly that which occurs in diabetics as a result of therapy with insulins or insulin analogs or other glucose lowering agents, or combinations of such agents.
• US6136812A
  申请人：——

  公开号：US6136812A

  公开（公告）日：2000-10-24
• US6627755B1
  申请人：——

  公开号：US6627755B1

  公开（公告）日：2003-09-30