(E)-N-hydroxy-3-[3-[(4-methoxyphenyl)sulfonyl-propan-2-ylamino]phenyl]-3-pyridin-3-ylprop-2-enamide

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: (E)-N-hydroxy-3-[3-[(4-methoxyphenyl)sulfonyl-propan-2-ylamino]phenyl]-3-pyridin-3-ylprop-2-enamide
• 化学式: C₂₄H₂₅N₃O₅S
• 分子量: 467.5
• InChiKey: RJUMZISZZHYKDC-HZHRSRAPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  33
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  117
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• NOVEL PROPENOHYDROXAMIC ACID DERIVATIVES
  申请人：WAKUNAGA PHARMACEUTICAL CO., LTD.

  公开号：EP1314721A1

  公开（公告）日：2003-05-28

  Provided are a propenohydroxamic acid derivative represented by the following formula (1): [wherein, R1 represents a hydrogen atom, an alkyl group or a halogen atom, R2 represents a cycloalkyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group, R3 represents a hydrogen atom or a halogen atom, R4 represents a hydrogen atom, a substituted or unsubstituted alkyl group or a substituted or unsubstituted alkenyl group, R5 represents R6CO-, R6SO2-, R6NRCO- or R6NHCS- (in which, R6 represents a substituted or unsubstituted alkyl or cycloalkyl group, a cyclic amino group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group), R7 represents a hydrogen atom or a protecting group and A represents CH, a nitrogen atom or an oxidized nitrogen atom], or salt thereof; and a medicament containing the propenohydroxamic acid derivative or salt thereof. The compound (1) or salt thereof has excellent TACE inhibitory activity and is therefore useful as a medicament for preventing and/or treating diseases such as septicemia, rheumatoid arthritis, osteoarthritis, infectious diseases, autoimmune diseases, malignant neoplasm, collagenosis, chronic ulcerative colitis, MOF and insulin-independent diabetes.

  提供的是以下式（1）所表示的丙烯羟羟肟酸衍生物：[其中，R1代表氢原子、烷基或卤素原子，R2代表环烷基、取代或未取代芳基或取代或未取代杂环芳基，R3代表氢原子或卤素原子，R4代表氢原子、取代或未取代烷基或取代或未取代烯基，R5代表R6CO-、R6SO2-、R6NRCO-或R6NHCS-（其中，R6代表取代或未取代烷基或环烷基、环氨基、取代或未取代芳基或取代或未取代杂环芳基），R7代表氢原子或保护基，A代表CH、氮原子或氧化氮原子]，或其盐；以及含有该丙烯羟羟肟酸衍生物或其盐的药物。该化合物（1）或其盐具有优异的TACE抑制活性，因此可用作预防和/或治疗败血症、类风湿关节炎、骨关节炎、传染病、自身免疫疾病、恶性肿瘤、结缔组织病、慢性溃疡性结肠炎、多器官功能障碍综合征和胰岛素非依赖性糖尿病等疾病的药物。
• UTILIZATION OF TACE INHIBITORS FOR THE TREATMENT OF ACNE
  申请人：AUBERT JÉRÔME

  公开号：US20100168089A1

  公开（公告）日：2010-07-01

  An in vitro method of screening for candidate compounds for the preventive or curative treatment of acne entails determination of the ability of a compound to inhibit the expression or the activity of TACE, and also to the administration of inhibitors of the expression or of the activity of this enzyme, in the treatment of acne.

  一种体外筛选预防或治疗痤疮候选化合物的方法，需要确定化合物抑制TACE（酶）表达或活性的能力，并且使用这种酶表达或活性的抑制剂进行痤疮治疗。
• Novel propenohydroxamic acid derivatives
  申请人：——

  公开号：US20040029928A1

  公开（公告）日：2004-02-12

  Provided are a propenohydroxamic acid derivative represented by the following formula (1): 1 [wherein, R 1 represents a hydrogen atom, an alkyl group or a halogen atom, R 2 represents a cycloalkyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group, R 3 represents a hydrogen atom or a halogen atom, R 4 represents a hydrogen atom, a substituted or unsubstituted alkyl group or a substituted or unsubstituted alkenyl group, R 5 represents R 6 CO—, R 6 SO 2 —, R 6 NHCO— or R 6 NHCS— (in which, R 6 represents a substituted or unsubstituted alkyl or cycloalkyl group, a cyclic amino group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group), R 7 represents a hydrogen atom or a protecting group and A represents CH, a nitrogen atom or an oxidized nitrogen atom], or salt thereof; and a medicament containing the propenohydroxamic acid derivative or salt thereof. The compound (1) or salt thereof has excellent TACE inhibitory activity and is therefore useful as a medicament for preventing and/or treating diseases such as septicemia, rheumatoid arthritis, osteoarthritis, infectious diseases, autoimmune diseases, malignant neoplasm, collagenosis, chronic ulcerative colitis, MOF and insulin-independent diabetes.

  提供了一种由以下式（1）表示的丙烯羟肟酸衍生物：1 [其中，R1表示氢原子，烷基或卤素原子，R2表示环烷基，取代或未取代芳基或取代或未取代杂芳基，R3表示氢原子或卤素原子，R4表示氢原子，取代或未取代烷基或取代或未取代烯基，R5表示R6CO—，R6SO2—，R6NHCO—或R6NHCS—（其中，R6表示取代或未取代的烷基或环烷基，环氨基，取代或未取代的芳基或取代或未取代的杂芳基），R7表示氢原子或保护基，A表示CH，氮原子或氧化氮原子]，或其盐；以及含有丙烯羟肟酸衍生物或其盐的药物。化合物（1）或其盐具有优异的TACE抑制活性，因此可用作预防和/或治疗败血症、类风湿性关节炎、骨关节炎、感染性疾病、自身免疫性疾病、恶性肿瘤、结缔组织病、慢性溃疡性结肠炎、MOF和非胰岛素依赖性糖尿病等疾病的药物。
• Method of using a COX-2 inhibitor and a TACE inhibitors as a combination therapy
  申请人：Pharmacia Corporation

  公开号：US20040122011A1

  公开（公告）日：2004-06-24

  The present invention provides compositions and methods to treat, prevent or inhibit a neoplasia, a neoplasia-related disorder, pain, inflammation, an inflammatory-related disorder, a vaso-occlusive event or a vaso-occlusive-related disorder in a mammal using a combination of a COX-2 inhibitor and a TACE inhibitor.

  本发明提供了一种使用COX-2抑制剂和TACE抑制剂的组合物和方法，以治疗、预防或抑制哺乳动物中的肿瘤、肿瘤相关疾病、疼痛、炎症、炎症相关疾病、血管闭塞性事件或血管闭塞性相关疾病。
• UTILISATION DE L'ACIDE E-3-[3-[N-(4-METHOXYBENZENESULFONYL)-N-ISOPROPYLAMINO]PHENYL]-3-(3-PYRIDYL)PROPENOHYDROXAMIQUE POUR LA PREPARATION D'UN MEDICAMENT DESTINE A PREVENIR ET/OU A TRAITER LES PATHOLOGIES INFLAMMATOIRES CUTANEES
  申请人：GALDERMA RESEARCH & DEVELOPMENT

  公开号：EP1998772A2

  公开（公告）日：2008-12-10