4-(thiazol-2-ylsulfamoyl)-benzenesulfonyl chloride

• 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: 4-(thiazol-2-ylsulfamoyl)-benzenesulfonyl chloride
• 英文别名: 4-chlorosulfonyl-N-(2-thiazolyl)benzenesulfonamide；4-(1,3-thiazol-2-ylsulfamoyl)benzenesulfonyl chloride
• 化学式: C₉H₇ClN₂O₄S₃
• 分子量: 338.817
• InChiKey: TZBPLEKRKKVKHT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  138
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  4-(thiazol-2-ylsulfamoyl)-benzenesulfonyl chloride 、 2,2-二苯基乙胺 在 吡啶 作用下， 生成 benzene-1,4-disulfonic acid 1-[(2,2-diphenyl-ethyl)-amide] 4-thiazol-2-ylamide
  参考文献：
  名称：

  WO2007/56099

  摘要：

  公开号：
• 作为产物：
  描述：

  磺胺噻唑 在 盐酸 、 溶剂黄146 、 sodium nitrite 、 二氧化硫 、 copper dichloride 作用下， 以 水 、 乙腈 、 溶剂黄146 为溶剂， 反应 2.33h， 生成 4-(thiazol-2-ylsulfamoyl)-benzenesulfonyl chloride
  参考文献：
  名称：

  WO2007/56099

  摘要：

  公开号：

文献信息

• Integrin expression inhibitors
  申请人：——

  公开号：US20040018192A1

  公开（公告）日：2004-01-29

  The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them. 1 In the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, —CH═CH— or —(CR 4b R 5b ) m b — (wherein R 4b and R 5b are the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and m b means an integer of 1 or 2); R 1 means hydrogen atom or a C1-C6 alkyl group; Z means a single bond or —CO—NH—; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.

  本发明提供了一种整合素表达抑制剂，以及基于整合素抑制作用的用于治疗动脉硬化、银屑病、癌症、视网膜血管生成、糖尿病视网膜病变或炎症性疾病的药剂、抗凝剂或癌症转移抑制剂。即提供了一种包含以下式(I)所表示的磺胺化合物、其药理学上可接受的盐或其水合物作为活性成分的整合素表达抑制剂。 在该式中，B表示一个C6-C10芳基环或6-至10成员杂芳基环，可能具有取代基，并且环的一部分可能是饱和的；K表示一个单键，-CH═CH-或-(CR 4b R 5b ) m b -（其中R 4b 和R 5b 相同或不同，各自表示氢原子或C1-C4烷基；m b 表示1或2的整数）；R 1 表示氢原子或C1-C6烷基；Z表示一个单键或-CO-NH-；R表示一个C6-C10芳基环或6-至10成员杂芳基环，可能具有取代基，并且环的一部分可能是饱和的，分别。
• Integrin expression inhibitor
  申请人：Wakabayashi Toshiaki

  公开号：US20050176712A1

  公开（公告）日：2005-08-11

  The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them, wherein in the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, —CH═CH— or —(CR 4b R 5b ) m b — (wherein R 4b and R 5b are the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and m b means an integer of 1 or 2); R 1 means hydrogen atom or a C1-C6 alkyl group; Z means a single bond or —CO—NH—; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.

  本发明提供了一种整合素表达抑制剂，并提供了一种基于整合素抑制作用的用于治疗动脉硬化、银屑病、癌症、视网膜血管生成、糖尿病视网膜病变或炎症性疾病的药剂、抗凝剂或癌症转移抑制剂。换句话说，本发明提供了一种整合素表达抑制剂，其包括以下式（I）所表示的磺酰胺化合物作为活性成分、其药学上可接受的盐或其水合物： 其中，在上述式中，B表示C6-C10芳基环或6-至10元杂环芳基环，其中可能有取代基，并且环的一部分可能是饱和的；K表示单键，-CH═CH-或-(CR4bR5b)mb-（其中R4b和R5b相同或不同，每个表示氢原子或C1-C4烷基；mb表示1或2的整数）；R1表示氢原子或C1-C6烷基；Z表示单键或-CO-NH-；R分别表示C6-C10芳基环或6-至10元杂环芳基环，其中可能有取代基，并且环的一部分可能是饱和的。
• INHIBITORS OF ION CHANNELS
  申请人：Wang Xiaodong

  公开号：US20070135493A1

  公开（公告）日：2007-06-14

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

  本发明提供了在治疗疾病中有用的化合物、组合物和方法，通过抑制电压门控钠通道中的钠离子通量。更具体地，本发明提供了取代芳基磺酰胺、包含这些化合物的组合物以及使用这些化合物或组合物治疗中枢或外周神经系统疾病，尤其是疼痛和慢性疼痛的方法，通过阻断与所示条件的发生或复发相关的钠通道。本发明的化合物、组合物和方法特别适用于通过抑制电压门控钠通道中的离子通量来治疗神经病理性或炎性疼痛。
• INTEGRIN EXPRESSION INHIBITOR
  申请人：WAKABAYASHI Toshiaki

  公开号：US20100267754A1

  公开（公告）日：2010-10-21

  The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them, wherein in the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, —CH═CH— or —(CR 4b R 5b ) m b — (wherein R 4b and R 5b are the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and m b means an integer of 1 or 2); R 1 means hydrogen atom or a C1-C6 alkyl group; Z means a single bond or —CO—NH—; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.

  本发明提供了一种整合素表达抑制剂，以及一种用于治疗动脉硬化、银屑病、癌症、视网膜血管生成、糖尿病视网膜病变或炎症性疾病、抗凝剂或癌症转移抑制剂的药剂，其基于整合素抑制作用。即，提供一种整合素表达抑制剂，其包括以下式（I）所表示的磺酰胺化合物作为活性成分，其药理学上可接受的盐或水合物，其中在该式中，B表示一个C6-C10芳基环或6-到10成员杂环环，可以有取代基，在环中的一部分可能是饱和的；K表示单键，—CH═CH—或—（CR4bR5b）mb—（其中R4b和R5b相同或不同，每个表示氢原子或C1-C4烷基；mb表示1或2的整数）；R1表示氢原子或C1-C6烷基；Z表示单键或—CO—NH—；R分别表示C6-C10芳基环或6-到10成员杂环环，可以有取代基，在环中的一部分可能是饱和的。
• SODIUM CHANNEL INHIBITORS
  申请人：Beaudoin Serge

  公开号：US20100267782A1

  公开（公告）日：2010-10-21

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

  本发明提供了一种在通过抑制电压门控钠通道的钠离子通量治疗疾病方面有用的化合物、组合物和方法。更具体地，本发明提供了取代芳基磺酰胺、包含这些化合物的组合物以及使用这些化合物或组合物治疗中枢或外周神经系统疾病，特别是疼痛和慢性疼痛的方法，通过阻断与所述疾病的发生或复发有关的钠通道。本发明的化合物、组合物和方法特别适用于通过抑制电压门控钠通道的离子通量治疗神经病理性或炎症性疼痛。