N-[4-(4-甲基苯氧基)苯基]甲烷磺酰胺 | 1017800-01-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-[4-(4-甲基苯氧基)苯基]甲烷磺酰胺
• 英文名称: N-(4-p-tolyloxy-phenyl)-methanesulfonamide
• 英文别名: N-[4-(4-methylphenoxy)phenyl]methane sulfonamide；N-[4-(4-methylphenoxy)phenyl]methanesulfonamide
• CAS: 1017800-01-9
• 化学式: C₁₄H₁₅NO₃S
• 分子量: 277.344
• InChiKey: HFCHRQNIUUVLOT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  63.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-(2,3-环氧丙烷)吗啉 、 N-[4-(4-甲基苯氧基)苯基]甲烷磺酰胺 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.5h， 以88%的产率得到N-(2-hydroxy-3-morpholin-4-ylpropyl)-N-[4-(4-methylphenoxy)phenyl]methanesulfonamide
  参考文献：
  名称：

  Microwave assisted ring-opening of epoxides with N-biaryl sulfonamides in the synthesis of matrix metalloproteinase-9 inhibitors

  摘要：

  A microwave accelerated epoxide ring-opening process with N-biaryl sulfonamides is described. Under this mild, highly efficient condition, an alpha-hydroxy-beta-N-biaryl sulfonamide skeleton is rapidly assembled leading ultimately to a novel series of matrix metalloproteinase-9 inhibitors with single digit nanomolar activities. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2007.11.184
• 作为产物：
  描述：

  甲基磺酰氯 、 4-氨基-4-甲基二苯醚 在 吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 生成 N-[4-(4-甲基苯氧基)苯基]甲烷磺酰胺
  参考文献：
  名称：

  HETEROCYCLIC DERIVED METALLOPROTEASE INHIBITORS

  摘要：

  这项发明提供了一种新颖的杂环衍生物基质金属蛋白酶抑制剂的化学式，以及包含同样化合物的药物组合物，用于治疗通过拮抗基质金属蛋白酶而改善的疾病。该发明还提供了使用即时药物组合物的治疗和预防方法。

  公开号：

  US20080103129A1

文献信息

• [EN] MATRIX METALLOPROTEINASE INHIBITORS<br/>[FR] INHIBITEURS DE MÉTALLOPROTÉINASE MATRICIELLE
  申请人：RANBAXY LAB LTD

  公开号：WO2012038944A1

  公开（公告）日：2012-03-29

  The present invention relates to methyl sulfonamides and N-formamides derivatives of formula (I) and to processes for their syntheses. The invention also relates to pharmacological compositions containing these derivatives and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatie arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, dry eye, neointimal proliferation which leads to restenosis and ischemic heart failure, stroke, renal disease, tumor metastasis, and other inflammatory disorders characterized by over expression and over activation of an matrix metalloproteinase using the compounds.

  本发明涉及公式（I）的甲基磺酰胺和N-甲酰胺衍生物，以及它们的合成方法。该发明还涉及含有这些衍生物的药物组合物，以及治疗哮喘、类风湿关节炎、慢性阻塞性肺病、鼻炎、骨关节炎、银屑病性关节炎、牛皮癣、肺纤维化、肺部炎症、急性呼吸窘迫综合征、牙周炎、多发性硬化症、牙龈炎、动脉粥样硬化、干眼症、新生内膜增生导致再狭窄和缺血性心力衰竭、中风、肾脏疾病、肿瘤转移以及其他以基质金属蛋白酶过度表达和过度活化为特征的炎症性疾病的方法，使用这些化合物。
• HETEROCYCLIC DERIVED METALLOPROTEASE INHIBITORS
  申请人：Zhang Yue-Mei

  公开号：US20080103129A1

  公开（公告）日：2008-05-01

  This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.

  这项发明提供了一种新颖的杂环衍生物基质金属蛋白酶抑制剂的化学式，以及包含同样化合物的药物组合物，用于治疗通过拮抗基质金属蛋白酶而改善的疾病。该发明还提供了使用即时药物组合物的治疗和预防方法。
• MATRIX METALLOPROTEASE INHIBITORS
  申请人：YANG Shyh-Ming

  公开号：US20080085893A1

  公开（公告）日：2008-04-10

  The present invention relates to compounds of Formula I, wherein R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. In addition, the present invention relates to methods treating disorders related to matrix metalloproteases. More particularly, the compounds of the present invention are useful for treating stroke.

  本发明涉及式I的化合物，其中R1、R2、R3、R4、R5、R6和R7在规范中定义。此外，本发明涉及治疗与基质金属蛋白酶相关疾病的方法。更具体地，本发明的化合物对治疗中风具有用处。
• SPIROHETEROCYCLIC DERIVATIVE COMPOUNDS AND DRUGS COMPRISING THE COMPOUNDS AS THE ACTIVE INGREDIENT
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1553098A1

  公开（公告）日：2005-07-13

  Spiroheterocyclic ring derivatives of the formula (I) (wherein R1 is H, alkyl, alkenyl, etc.; R2 is keto, thioketo, alkyl, etc.; R3 is alkyl, alkenyl, etc.; AB ring is fused bi-cyclic ring or spiro ring), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as an active ingredient. The compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, allergic diseases, immunosuppression, cancer metastasis and acquired immune deficiency syndrome etc.

  公式（I）的Spiroheterocyclic环衍生物（其中R1是H，烷基，烯基等；R2是酮，硫酮，烷基等；R3是烷基，烯基等；AB环是融合的双环或螺环），其季铵盐，N-氧化物，非毒性盐或包含它们的药物组成物，作为活性成分。公式（I）的化合物调节趋化因子/趋化因子受体的作用，它们用于预防和治疗各种炎症性疾病，过敏性疾病，免疫抑制，癌症转移和获得性免疫缺陷综合症等。
• Drugs containing triazaspiro[5.5]undecane derivatives as the active ingredient
  申请人：——

  公开号：US20040106619A1

  公开（公告）日：2004-06-03

  A pharmaceutical composition for prevention and/or treatment for HIV infection or AIDS induced by the infection which comprises, as an active ingredient, a triazaspiro[5.5]undecane derivative, a quaternary ammonium salt thereof, an N-oxide thereof, or a non-toxic salt thereof, and if necessary, it may be combined with at least one member of other agents for prevention and/or treatment for HIV infection (wherein all symbols are as defined in the specification.). 1 The triazaspiro[5.5]undecane derivatives, the quaternary ammonium salts thereof or the N-oxides thereof, or the non-toxic salts thereof are useful in preventing and/or treating HIV infection and AIDS induced by the infection.

  一种用于预防和/或治疗由HIV感染引起的艾滋病的药物组合物，其作为活性成分包括三氮杂螺[5.5]十一烷衍生物、其季铵盐、其N-氧化物或其非毒性盐，如有必要，还可以与其他预防和/或治疗HIV感染的药物组合使用（其中所有符号均如规范中定义） 。1三氮杂螺[5.5]十一烷衍生物、其季铵盐或其N-氧化物，或其非毒性盐在预防和/或治疗HIV感染和由该感染引起的艾滋病中有用。