N-hydroxy-2-[(4-methoxyanilino)-sulfonyl]benzamide

• 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: N-hydroxy-2-[(4-methoxyanilino)-sulfonyl]benzamide
• 英文别名: N-Hydroxy-2-(4-methoxy-phenylsulfamoyl)-benzamide；N-hydroxy-2-[(4-methoxyphenyl)sulfamoyl]benzamide
• 化学式: C₁₄H₁₄N₂O₅S
• 分子量: 322.342
• InChiKey: UNYWJVNGOZMHAU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  113
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  乙基2-(氯磺酰基)苯甲酸酯 在 甲醇 、 氢氧化钾 、 1-羟基苯并三唑 、 1-(3-二甲基氨基丙基)-3-乙基碳二亚胺 、 三乙胺 、 乙酰氯 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 生成 N-hydroxy-2-[(4-methoxyanilino)-sulfonyl]benzamide
  参考文献：
  名称：

  Synthesis and activity of selective MMP inhibitors with an aryl backbone

  摘要：

  A series of novel, MMP-1 sparing arylhydroxamate sulfonamides with activity against MMP-2 and -13 is described.

  DOI：

  10.1016/s0960-894x(00)00584-9

文献信息

• Sulfonyl aryl or heteroaryl hydroxamic acid compounds
  申请人：G. D. Searle & Co.,

  公开号：US20030191317A1

  公开（公告）日：2003-10-09

  A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

  本发明涉及一种磺酰基芳香或杂芳环羟羧酸化合物，该化合物在抑制基质金属蛋白酶活性方面起作用，还涉及一种治疗方法，包括向与病理性基质金属蛋白酶活性相关病情的宿主投入考虑的磺酰基芳香或杂芳环羟羧酸化合物，其有效量抑制MMP酶活性。
• Use of sulfonyl aryl or heteroaryl hydroxamic acids and derivatives thereof as aggrecanase inhibitors
  申请人：——

  公开号：US20030171404A1

  公开（公告）日：2003-09-11

  This invention is directed to a process for inhibiting aggrecanase activity. The process comprises administering a therapeutically effective amount of a sulfonyl aromatic or heteroaromatic hydroxamic acid, a derivative thereof, or a pharmaceutically acceptable salt of the hydroxamic acid or derivative to a host animal. The compound generally corresponds in structure to the following formula: 1 wherein W and the R groups are described in more detail in Applicants' specification.

  这项发明涉及一种抑制聚集素酶活性的过程。该过程包括向宿主动物施用一定治疗有效量的磺酰芳香或杂芳羟肟酸、其衍生物或羟肟酸或其衍生物的药用盐。该化合物通常与以下结构对应：1其中W和R基的详细描述在申请人的说明书中。
• Sulfonyl aryl hydroxamates and their use as matrix metalloprotease inhibitors
  申请人：——

  公开号：US20030073845A1

  公开（公告）日：2003-04-17

  This invention is directed to sulfonyl aromatic hydroxamic acid compounds and salts thereof that, inter alia, inhibit matrix metalloprotease (MMP) activity and/or aggrecanase activity. In some particularly preferred embodiments, the compound corresponds in structure to one of the following formulas: 1 wherein W 2 , the R groups, and —A—R—E—Y are described in more detail in Applicants' specification. This invention also is directed to a process that comprises administering such a compound or pharmaceutically acceptable salt thereof to a host animal having a condition associated with MMP activity.

  本发明涉及磺酰基芳基羟肟酸化合物及其盐，这些化合物在抑制基质金属蛋白酶（MMP）活性和/或聚集素酶活性方面具有作用。在一些特别优选的实施方式中，该化合物的结构符合以下公式之一：其中W2、R基团和—A—R—E—Y在申请人的说明书中有更详细的描述。本发明还涉及一种过程，该过程包括向患有与MMP活性相关的病况的宿主动物施用这种化合物或其药用可接受盐。
• [EN] HYDROXAMIC ACID DERIVATIVES AS MATRIX METALLOPROTEASE INHIBITORS<br/>[FR] COMPOSES SULFONYLE ARYLE OU HETEROARYLE D'ACIDE HYDROXAMIQUE
  申请人：SEARLE & CO

  公开号：WO2000069819A1

  公开（公告）日：2000-11-23

  A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to formula (a) wherein W and the R groups are defined elsewhere.

  本发明涉及一种磺酰基芳香族或杂芳香族环羟肟酸化合物，该化合物在抑制基质金属蛋白酶活性方面具有作用，还涉及一种治疗过程，包括向患有与病理基质金属蛋白酶活性相关的病症的宿主中投与考虑到的磺酰基芳香族或杂芳香族环羟肟酸化合物，其剂量足以抑制MMP酶活性。 考虑到的化合物在结构上对应于公式（a），其中W和R基在其他地方定义。
• SULFONYL DIVALENT ARYL OR HETEROARYL HYDROXAMIC ACID COMPOUNDS
  申请人：——

  公开号：US20010020021A1

  公开（公告）日：2001-09-06

  A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

  本文披露了一种磺酰基双价芳香或杂芳香环羟肟酸化合物，其可以抑制基质金属蛋白酶活性，同时也揭示了一种治疗过程，包括向患有与病理基质金属蛋白酶活性相关的病情的宿主中投与考虑的磺酰基双价芳香或杂芳香环羟肟酸化合物，其剂量具有抑制MMP酶活性的有效作用量。