6-(4'-(2-amino-2-oxoethyl)-2'-chlorobiphenyl-4-yl)-3,5-dimethylpyrazine-2-carboxamide | 1259022-40-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 6-(4'-(2-amino-2-oxoethyl)-2'-chlorobiphenyl-4-yl)-3,5-dimethylpyrazine-2-carboxamide
• 英文别名: 6-[4-[4-(2-amino-2-oxoethyl)-2-chlorophenyl]phenyl]-3,5-dimethylpyrazine-2-carboxamide
• CAS: 1259022-40-6
• 化学式: C₂₁H₁₉ClN₄O₂
• 分子量: 394.86
• InChiKey: YWUOTPDYRAOWML-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  methyl 2-(4'-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)-2-chlorobiphenyl-4-yl)acetate 在 氨 作用下， 以 甲醇 为溶剂， 反应 1.0h， 以28%的产率得到6-(4'-(2-amino-2-oxoethyl)-2'-chlorobiphenyl-4-yl)-3,5-dimethylpyrazine-2-carboxamide
  参考文献：
  名称：

  CHEMICAL COMPOUNDS 785

  摘要：

  DGAT-1抑制剂化合物公式(I)，药物可接受的盐和前药，以及药物组合物、制造过程和使用方法，例如用于治疗肥胖 其中，例如，r为0或1，X 1 为线性（1-3C）烷基； q为0或1，X 2 为氟、氯或（1-3C）烷基； Y 1 选自氟、氯、溴、氰、（1-3C）烷基和（1-2C）烷氧基； n为0、1或2，Y 2 为氟、氯或（1-3C）烷基； p为0、1或2，Y 3 为（1-3C）烷基或形成（3-5C）环烷基环； Z为羧基或—CONHSO 2 Me或—CONRbRc，其中Rb和Rc独立选自例如氢和（1-4C）烷基，或Rb和Rc相连以形成吗啉环或（4-6C）杂环，当Z为—CONRbRc时，Rb和Rc基团可以可选地被羧基取代。

  公开号：

  US20100324068A1

文献信息

• Substituted pyrazines as DGAT-1 inhibitors
  申请人：AstraZeneca AB

  公开号：US08188092B2

  公开（公告）日：2012-05-29

  DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X2 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or —CONHSO2Me or —CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is —CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.

  本文介绍了公式（I）的DGAT-1抑制剂化合物、药学上可接受的盐和前药，以及制备它们的药物组合物、制备过程及其在治疗肥胖症等方面的用途，其中，例如，r为0或1，X1为线性（1-3C）烷基；q为0或1，X2为氟、氯或（1-3C）烷基；Y1从氟、氯、溴、氰、（1-3C）烷基和（1-2C）烷氧中选择；n为0、1或2，Y2为氟、氯或（1-3C）烷基；p为0、1或2，Y3为（1-3C）烷基或形成（3-5C）环烷基；Z为羧基或—CONHSO2Me或—CONRbRc，其中Rb和Rc独立选择，例如，氢和（1-4C）烷基或Rb和Rc连接以形成吗啡环或（4-6C）杂环，当Z为—CONRbRc时，Rb和Rc基团可以选择性地被羧基取代。
• PYRAZINE CARBOXAMIDES AS INHIBITORS OF DGAT1
  申请人：AstraZeneca AB

  公开号：EP2443096A1

  公开（公告）日：2012-04-25
• US8188092B2
  申请人：——

  公开号：US8188092B2

  公开（公告）日：2012-05-29
• [EN] PYRAZINE CARBOXAMIDES AS INHIBITORS OF DGAT1<br/>[FR] CARBOXAMIDES DE PYRAZINE UTILES COMME INHIBITEURS DE LA DGAT1
  申请人：ASTRAZENECA AB

  公开号：WO2010146395A1

  公开（公告）日：2010-12-23

  DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X1 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or - CONHSO2 Me or –CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is –CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.
• CHEMICAL COMPOUNDS 785
  申请人：Birch Alan Martin

  公开号：US20100324068A1

  公开（公告）日：2010-12-23

  DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X 1 is linear (1-3C)alkyl; q is 0 or 1 and X 2 is fluoro, chloro or (1-3C)alkyl; Y 1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y 2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y 3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or —CONHSO 2 Me or —CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is —CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.

  DGAT-1抑制剂化合物公式(I)，药物可接受的盐和前药，以及药物组合物、制造过程和使用方法，例如用于治疗肥胖 其中，例如，r为0或1，X 1 为线性（1-3C）烷基； q为0或1，X 2 为氟、氯或（1-3C）烷基； Y 1 选自氟、氯、溴、氰、（1-3C）烷基和（1-2C）烷氧基； n为0、1或2，Y 2 为氟、氯或（1-3C）烷基； p为0、1或2，Y 3 为（1-3C）烷基或形成（3-5C）环烷基环； Z为羧基或—CONHSO 2 Me或—CONRbRc，其中Rb和Rc独立选自例如氢和（1-4C）烷基，或Rb和Rc相连以形成吗啉环或（4-6C）杂环，当Z为—CONRbRc时，Rb和Rc基团可以可选地被羧基取代。