5-(3,5-Dimethylpiperidin-1-yl)-1,3,4-thiadiazol-2-amine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 5-(3,5-Dimethylpiperidin-1-yl)-1,3,4-thiadiazol-2-amine
• 化学式: C₉H₁₆N₄S
• 分子量: 212.32
• InChiKey: PZABURDJMZNJOA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  83.3
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] 5'-CARBAMOYL-1,1-BIPHENYL-4-CARBOXAMIDE DERIVATIVES AND THEIR USE AS P38 KINASE INHIBITORS<br/>[FR] DERIVES DE 5'-CARBAMOYL-1,1-BIPHENYL-4-CARBOXAMIDE ET LEUR UTILISATION COMME INHIBITEURS DE LA KINASE P38
  申请人：GLAXO GROUP LTD

  公开号：WO2003032972A1

  公开（公告）日：2003-04-24

  Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1-6alkyl, C3-7cycloalkyl, C2-6alkenyl, -SO2NR4R5, -CONR4R5 and -COOR4; and when m is 2 to 4 R1 is additionally selected from C1-6alkoxy, hydroxy, NR4R5, -NR4SO2R5, -NR4SOR5, -NR4COR5, and -NR4CONR4R5; R2 is selected from hydrogen, C1-6alkyl and -(CH2)n-C3-7cycloalkyl; R3 is the group -CO-NH-(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1-6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.

  化合物的式子(I)：其中当m为0到4时，R1从C1-6烷基、C3-7环烷基、C2-6烯基、-SO2NR4R5、-CONR4R5和-COOR4中选择；当m为2到4时，R1还从C1-6烷氧基、羟基、NR4R5、-NR4SO2R5、-NR4SOR5、-NR4COR5和-NR4CONR4R5中选择；R2从氢、C1-6烷基和-(CH2)n-C3-7环烷基中选择；R3是群- CO-NH-( )p-R6; U从甲基和卤素中选择；W从甲基和氯中选择；V和Y各自独立地从氢、甲基和卤素中选择；m从0、1、2、3和4中选择，其中所得碳链的每个碳原子可以选择性地用一个或两个独立选择的C1-6烷基基团取代；n从0、1、2和3中选择；p和r独立地从0、1和2中选择；s从0、1和2中选择；或其药学上可接受的盐或溶剂，以及它们作为药物的用途，特别是作为p38激酶抑制剂。
• 5'-Carbamoyl-1,1-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors
  申请人：——

  公开号：US20040267012A1

  公开（公告）日：2004-12-30

  Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1-6alkyl, C3-7cycloalkyl, C2-6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1-6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, —NR4COR5, and —NR4CONR4R5; R2 is selected from hydrogen, C1-6alkyl and —(CH2)n-C3-7cycloalkyl; R3 is the group —CO—NH—(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1-6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. 1

  化学式为(I)的化合物：其中当m为0至4时，R1从C1-6烷基，C3-7环烷基，C2-6烯基，—SO2NR4R5，—CONR4R5和—COOR4中选择；当m为2至4时，R1还可从C1-6烷氧基，羟基，NR4R5，—NR4SO2R5，—NR4SOR5，—NR4COR5和—NR4CONR4R5中选择；R2从氢，C1-6烷基和—（CH2）n-C3-7环烷基中选择；R3为—CO—NH—（ ）p-R6基团；U从甲基和卤素中选择；W从甲基和氯中选择；V和Y各自独立地从氢，甲基和卤素中选择；m从0、1、2、3和4中选择，其中所得碳链的每个碳原子可以选择性地被一个或两个从C1-6烷基中独立选择的基团取代；n从0、1、2和3中选择；p和r独立地从0、1和2中选择；s从0、1和2中选择；或其药学上可接受的盐或溶剂，以及它们作为药物的用途，特别是作为p38激酶抑制剂。
• 5'-CARBAMOYL-1,1-BIPHENYL-CARBOXAMIDE DERIVATIVES AND THEIR USE AS P38 KINASE INHIBITORS
  申请人：GLAXO GROUP LIMITED

  公开号：EP1435936A1

  公开（公告）日：2004-07-14
• US7208629B2
  申请人：——

  公开号：US7208629B2

  公开（公告）日：2007-04-24