4-benzylpiperidin-1-yl-(2-methoxy-4-hydroxy)benzene Carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-benzylpiperidin-1-yl-(2-methoxy-4-hydroxy)benzene Carboxamide
• 英文别名: 3-(4-Benzylpiperidin-1-yl)-4-hydroxy-2-methoxybenzamide
• 化学式: C₂₀H₂₄N₂O₃
• 分子量: 340.422
• InChiKey: DBJCGYAHDFYFJD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  75.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-benzylpiperidin-1-yl-(2-methoxy-4-benzyloxy)benzene carboxamide 在 钯 H2 作用下， 以 甲醇 为溶剂， 以11.24 g (95.7%)的产率得到4-benzylpiperidin-1-yl-(2-methoxy-4-hydroxy)benzene Carboxamide
  参考文献：
  名称：

  Inhibitors of p38-&agr;kinase

  摘要：

  本发明涉及使用式子及其药学上可接受的盐或制药组合物的化合物治疗由p38-α激酶介导的疾病的方法，其中Z为N或CR1，R1为非干扰取代基，X1和X2均为连接基，Ar1和Ar2相同或不同，且表示可选择取代的C1-C20烃基残基，其中Ar1和Ar2中至少一个是可选择取代的芳基基团，但是当X2为CH2或同分异构体时，X1为CO或同分异构体，且Ar2为可选择取代的苯基，Ar1不是可选择取代的吲哚基、苯并咪唑基或苯并三唑基取代基，其中所述可选择取代的苯基不是可选择取代的吲哚基、苯并咪唑基或苯并三唑基，Y为非干扰取代基，其中n为0-4的整数，m为0-4的整数，1为0-3的整数。

  公开号：

  US06410540B1

文献信息

• Inhibitors of p38-&agr;kinase
  申请人：Scios, Inc.

  公开号：US06410540B1

  公开（公告）日：2002-06-25

  The invention is directed to methods to treat conditions mediated by p38-&agr;kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein Z is N or CR1, R1 is a noninterfering substituent, each of X1 and X2 is a linker, Ar1 and Ar2 are identical or different, and represent optionally substituted C1-C20 hydrocarbyl residues wherein at least one of Ar1 and Ar2 is an optionally substituted aryl group, with the proviso that when X2 is CH2 or an isostere thereof, X1 is CO or an isostere thereof, and Ar2 is optionally substituted phenyl, Ar1 is other than an optionally substituted indolyl, benzimidazolyl or benzotriazolyl substituent, and wherein said optionally substituted phenyl is not an optionally substituted indolyl, benzimidazolyl, or benzotriazolyl, Y is a noninterfering substituent, wherein n is an integer from 0-4, and wherein m is an integer from 0-4 and 1 is an integer from 0-3.

  本发明涉及使用式子及其药学上可接受的盐或制药组合物的化合物治疗由p38-α激酶介导的疾病的方法，其中Z为N或CR1，R1为非干扰取代基，X1和X2均为连接基，Ar1和Ar2相同或不同，且表示可选择取代的C1-C20烃基残基，其中Ar1和Ar2中至少一个是可选择取代的芳基基团，但是当X2为CH2或同分异构体时，X1为CO或同分异构体，且Ar2为可选择取代的苯基，Ar1不是可选择取代的吲哚基、苯并咪唑基或苯并三唑基取代基，其中所述可选择取代的苯基不是可选择取代的吲哚基、苯并咪唑基或苯并三唑基，Y为非干扰取代基，其中n为0-4的整数，m为0-4的整数，1为0-3的整数。
• USE OF PIPERIDINES AND/OR PIPERAZINES AS INHIBITORS OF P38-ALPHA KINASE
  申请人：SCIOS INC.

  公开号：EP1107758A2

  公开（公告）日：2001-06-20
• US6410540B1
  申请人：——

  公开号：US6410540B1

  公开（公告）日：2002-06-25
• [EN] INHIBITORS OF p38- alpha KINASE<br/>[FR] INHIBITEURS DE p38- alpha KINASE
  申请人：SCIOS INC

  公开号：WO2000012074A2

  公开（公告）日：2000-03-09

  The invention is directed to methods to treat conditions mediated by kinase using compounds of formula (1) and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein Z is N or CR1, R1 is a noninterfering substituent, each of X?1 and X2¿ is a linker, Ar?1 and Ar2¿ are identical or different, and represent optionally substituted C1-C20 hydrocarbyl residues wherein at least one of Ar?1 and Ar2¿ is an optionally substituted aryl group, with the proviso that when X2 is CH¿2? or an isostere thereof, X?1¿ is CO or an isostere thereof, and Ar2 is optionally substituted phenyl, Ar1 is other than an optionally substituted indolyl, benzimidazolyl or benzotriazolyl substituent, and wherein said optionally substituted phenyl is not an optionally substituted indolyl, benzimidazolyl, or benzotriazolyl, Y is a noninterfering substituent, wherein n is an integer from 0-4, and wherein m is an integer from 0-4 and 1 is an integer from 0-3.
• [EN] INHIBITORS OF p38- alpha KINASE<br/>[FR] INHIBITEURS DE LA P38- alpha KINASE
  申请人：SCIOS INC

  公开号：WO2001064676A2

  公开（公告）日：2001-09-07

  The invention is directed to prepare medicaments for treatment of and to methods to treat conditions mediated by kinase using compounds of the formula (3) wherein Ar1 and Ph are limited to specific embodiments or wherein the compound of formula (3) is a compound set forth in Figures 1A-1I.