3-Dimethylamino-1-(2,4-dimethyl-thiazol-5-yl)-propenone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-Dimethylamino-1-(2,4-dimethyl-thiazol-5-yl)-propenone
• 英文别名: (E)-3-(2,4-dimethyl-1,3-thiazol-5-yl)-N,N-dimethylprop-2-enamide
• 化学式: C₁₀H₁₄N₂OS
• 分子量: 210.3
• InChiKey: TWLWKASOYJPJJM-AATRIKPKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  61.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-Dimethylamino-1-(2,4-dimethyl-thiazol-5-yl)-propenone 、 胍 生成 4-(2,4-二甲基-1,3-噻唑)-2-氨基嘧啶
  参考文献：
  名称：

  Anti-cancer compounds

  摘要：

  本发明涉及2-取代的4-杂环芳基嘧啶，其制备方法，含有它们的制药组合物以及它们作为细胞周期蛋白依赖性激酶（CDKs）抑制剂的用途，因此用于治疗增殖性疾病，如癌症、白血病、牛皮癣等。

  公开号：

  US20020019404A1
• 作为产物：
  描述：

  2,4-二甲基-5-乙酰基噻唑 、 N,N-二甲基甲酰胺二甲基缩醛 在 氮气 、 dichloromethane diisopropyl ether 作用下， 反应 18.0h， 以to afford 9.94 g 3-dimethylamino-1-(2,4-dimethyl-thiazol-5-yl)-propenone as a brown powder (79%)的产率得到3-Dimethylamino-1-(2,4-dimethyl-thiazol-5-yl)-propenone
  参考文献：
  名称：

  N-(4-(4-methylthiazol-5-yl) pyrimidin-2-yl)-N-phenylamines as antiproliferative compounds

  摘要：

  本发明涉及2-取代的4-杂环芳基嘧啶，它们的制备，含有它们的药物组合物以及它们作为细胞周期蛋白依赖性激酶（CDKs）抑制剂的用途，因此可用于治疗增殖性疾病，如癌症、白血病、银屑病等。

  公开号：

  US20060199830A1

文献信息

• N-(4-(4-methylthiazol-5-yl)pyrimidin-2-yl)-N-phenylamines as antiproliferative compounds
  申请人：——

  公开号：US20040259894A1

  公开（公告）日：2004-12-23

  The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukemia, psoriasis and the like.

  本发明涉及2-取代的4-杂环芳基嘧啶、它们的制备、含有它们的药物组合物以及它们作为细胞周期蛋白依赖性激酶（CDKs）的抑制剂的用途，因此可用于治疗增殖性疾病，如癌症、白血病、牛皮癣等。
• Anti-viral compounds
  申请人：Wang Shudong

  公开号：US20050288307A1

  公开（公告）日：2005-12-29

  The present invention relates to the use of 2-substituted 4-heteroaryl-pyrimidines and related compounds in the treatment of viral disorders.

  本发明涉及使用2-取代的4-杂环基嘧啶和相关化合物治疗病毒性疾病。
• Pyrimidine compounds
  申请人：Wang Shudong

  公开号：US20050192300A1

  公开（公告）日：2005-09-01

  The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders.

  本发明涉及式I的取代嘧啶、其制备、含有它们的药物组合物以及它们作为细胞周期蛋白依赖性激酶（CDKs）抑制剂的应用，因此可用于治疗增殖性疾病和/或病毒性疾病。
• Pyridinylamino-pyrimidine derivatives as protein kinase inhibitors
  申请人：Wang Shudong

  公开号：US20060241297A1

  公开（公告）日：2006-10-26

  The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein: (A) “a” is a single bond and “b” is a double bond; R 1 and R 2 are each independently as defined below; R 10 is absent; or (B) “a” is a double bond and “b” is a single bond; R 1 is oxygen; R 2 is as defined below; and R 10 is H or alkyl; X is S, O, NH, or NR 7 ; Y is N or CR 8 ; one of Z 1 , Z 2 , and Z 3 is N or N + R a and the remainder are each independently CR 7 ; R 1 , R 2 , R 5 and R 6 are each independently R 7 ; R 3 and R 4 are each independently R 8 ; each R 7 is independently H, halogen, NR b R c , OR d or a hydrocarbyl group optionally substituted by one or more R 9 groups; each R 8 is independently H or (CH 2 ) n R 9 , where n is 0 or 1; each R 9 is independently selected from H, halogen, NO 2 , CN, R e , NHCOR f , CF 3 , COR g , NR h R i , CONR j R k , SO 2 NR l R m , SO 2 R n , OR p , OCH 2 CH 2 OR q , morpholine, piperidine and piperazine; and R a-q are each independently H or alkyl, wherein said alkyl group is optionally substituted by one or more R 9 groups; where the compound is other than [4-(2,4-dimethyl-thiazol-5-yl)-pyrimidin-2-yl]-pyridin-2-yl-amine and 4-[4-fluorophenyl)-1-(1-methyl-4-piperidinyl)-1H-imidazol-5-yl]-N-4-pyridinyl-2-pyrimidinamine. Further aspects of the invention relate to the use of compounds of formula I in the treatment of proliferative disorders, viral disorders, CNS disorders, strokes, alopecia and/or diabetes.

  本发明涉及式I的化合物或其药学上可接受的盐，其中：（A）“a”为单键，“b”为双键；R1和R2分别如下所定义；R10不存在；或（B）“a”为双键，“b”为单键；R1为氧原子；R2如下所定义；R10为H或烷基；X为S、O、NH或NR7；Y为N或CR8；Z1、Z2和Z3中的一个为N或N+Ra，其余分别独立为CR7；R1、R2、R5和R6分别独立为R7；R3和R4分别独立为R8；每个R7独立地为H、卤素、NRbRc、ORd或一个或多个R9基团选择性取代的烃基；每个R8独立地为H或（CH2）nR9，其中n为0或1；每个R9独立地选择自H、卤素、NO2、CN、Re、NHCORf、CF3、CORg、NRhRi、CONRjRk、SO2NRlRm、SO2Rn、ORp、OCH2CH2ORq、吗啡啶、哌啶和哌嗪；而Ra-q独立地为H或烷基，其中所述的烷基可以选择性地被一个或多个R9基团取代；其中该化合物不是[4-(2,4-二甲基噻唑-5-基)嘧啶-2-基]-吡啶-2-基胺和4-[4-氟苯基)-1-(1-甲基-4-哌啶基)-1H-咪唑-5-基]-N-4-吡啶基-2-嘧啶胺。本发明的另一方面涉及将式I的化合物用于治疗增殖性疾病、病毒性疾病、中枢神经系统疾病、中风、脱发和/或糖尿病。
• 2-substituted-4-heteroaryl-pyrimidines useful for the treatment of proliferative disorders
  申请人：Wang Shudong

  公开号：US20090137572A1

  公开（公告）日：2009-05-28

  The present invention relates to selected substituted pyrimidines their preparation, pharmaceutical compositions containing them and their use as inhibitors of one or more protein kinases, and hence their use in the treatment of proliferative disorders, viral disorders and/or other disorders.

  本发明涉及选定的取代嘧啶及其制备方法，含有它们的制药组合物以及它们作为一种或多种蛋白激酶抑制剂的用途，因此可用于治疗增殖性疾病、病毒性疾病和/或其他疾病。