N-{4-[2-(hydroxyamino)-2-oxoethyl]-4-piperidinyl}-4-[(2-methyl-4-quinolinyl)methoxy]benzamide | 362697-55-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-{4-[2-(hydroxyamino)-2-oxoethyl]-4-piperidinyl}-4-[(2-methyl-4-quinolinyl)methoxy]benzamide
• 英文别名: N-(4-(2-(hydroxyamino)-2-oxoethyl)piperidin-4-yl)-4-((2-methylquinolin-4-yl)methoxy)benzamide；N-[4-[2-(hydroxyamino)-2-oxoethyl]piperidin-4-yl]-4-[(2-methylquinolin-4-yl)methoxy]benzamide
• CAS: 362697-55-0
• 化学式: C₂₅H₂₈N₄O₄
• 分子量: 448.522
• InChiKey: BODLESUVCQEUII-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  33
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  113
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• Beta-Amino-Acid derivatives as inhibitors of matrix metalloproteases and TNF-Alpha
  申请人：——

  公开号：US20020013341A1

  公开（公告）日：2002-01-31

  The present application describes novel &bgr;-amino acid derivatives of formula I: 1 or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, U a , X a , Y a , Z a , R 1 , R 2 , R 3 , R 4 , and R 4a are defined in the present specification, which are useful as metalloprotease and/or as TNF-&agr; inhibitors.

  本申请描述了式I的新型β-氨基酸衍生物： 1 或其药用可接受的盐或前药形式，其中A、X、Z、U a 、X a 、Y a 、Z a 、R 1 、R 2 、R 3 、R 4 和R 4a 在本规范中有定义，这些衍生物可用作金属蛋白酶和/或TNF-α抑制剂。
• Beta-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-alpha
  申请人：——

  公开号：US20040072802A1

  公开（公告）日：2004-04-15

  The present application describes novel &bgr;-amino acid derivatives of formula I: 1 or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, X, Z, U a , X a , Y a , Z a , R 1 , R 2 , R 3 , R 4 , and R 4a are defined in the present specification, which are useful as metalloprotease and/or as TNF-&agr; inhibitors.

  本申请描述了式I的新颖β-氨基酸衍生物：1或其药用可接受的盐或前药形式，其中A、X、Z、Ua、Xa、Ya、Za、R1、R2、R3、R4和R4a在本规范中有定义，这些衍生物可用作金属蛋白酶和/或TNF-α抑制剂。
• Combined use of tace inhibitors and COX2 inhibitors as anti-inflammatory agents
  申请人：——

  公开号：US20030225054A1

  公开（公告）日：2003-12-04

  This invention relates to a method of treating inflammatory diseases in a mammal comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one TACE inhibitor of Formula (I), (II), (III), or (IV) of the present invention or a stereoisomer or pharmaceutically acceptable salt form thereof, (ii) one or more anti-inflammatory agents selected from the group consisting of: selective COX-2 inhibitors, interleukin-1 antagonists, dihydroorotate synthase inhibitors, p38 MAP kinase inhibitors, TNF-&agr; inhibitors, TNF-&agr; sequestration agents, and methotrexate. The invention also relates to compositions and kits containing the same.

  本发明涉及一种治疗哺乳动物炎症性疾病的方法，该方法包括向哺乳动物施用治疗有效量的以下物质的组合：(i)至少一种本发明式(I)、(II)、(III)或(IV)的TACE抑制剂或其立体异构体或药学上可接受的盐形式，(ii)一种或多种选自由以下组成的组的抗炎剂：选择性 COX-2 抑制剂、白细胞介素-1 拮抗剂、二氢烟酸合成酶抑制剂、p38 MAP 激酶抑制剂、TNF-&agr; 抑制剂、TNF-&agr; 封闭剂和甲氨蝶呤。本发明还涉及含有上述成分的组合物和试剂盒。
• Anti-inflammatory coatings for implantable medical devices and devices containing said coatings
  申请人：——

  公开号：US20040120977A1

  公开（公告）日：2004-06-24

  The present invention relates to implantable surgical medical devices having coatings comprising one or more compounds that inhibit TNF-&agr; converting enzyme (TACE), more particularly, stents having coatings comprising TACE inhibitors.

  本发明涉及具有包含一种或多种抑制 TNF-&agr; 转换酶（TACE）的化合物涂层的可植入外科医疗器械，特别是具有包含 TACE 抑制剂涂层的支架。
• BETA-AMINO ACID DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEASES AND TNF-ALPHA
  申请人：Bristol-Myers Squibb Pharma Company

  公开号：EP1263756A2

  公开（公告）日：2002-12-11