苯磺酰胺,N-(氨基硫代甲基)- | 13068-68-3

• 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: 苯磺酰胺,N-(氨基硫代甲基)-
• 英文名称: benzenesulfonyl-thiourea
• 英文别名: Benzolsulfonyl-thioharnstoff；benzenesulfonylthiourea；N-Benzolsulfonyl-thioharnstoff；N-Carbamothioylbenzenesulfonamide
• CAS: 13068-68-3
• 化学式: C₇H₈N₂O₂S₂
• 分子量: 216.285
• InChiKey: PVMBGVAQRSHDBB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  113
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  苯磺酰胺,N-(氨基硫代甲基)- 、 三氯硫氯甲烷 生成 (benzenesulfonyl-carbamimidoyl)-trichloromethyl-disulfane
  参考文献：
  名称：

  US2813902

  摘要：

  公开号：
• 作为产物：
  描述：

  N-cyano-benzenesulfonamide 在 tetraphosphorus decasulfide 、 溶剂黄146 作用下， 生成 苯磺酰胺,N-(氨基硫代甲基)-
  参考文献：
  名称：

  Production of arylsulfonyl thioureas

  摘要：

  公开号：

  US02738355A1

文献信息

• Acylaminoalkyl-substituted benzenesulfonamide derivatives, their preparation, their use and pharmaceutical preparations comprising them
  申请人：——

  公开号：US20020123494A1

  公开（公告）日：2002-09-05

  One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), 1 in which A, R(1), R(2), X, Y, and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.

  本发明的一个实施例涉及公式(I)的酰氨基烷基取代的苯磺酰胺衍生物， 1 其中A，R(1)，R(2)，X，Y和Z具有说明书中指出的含义，以及药用可接受的盐。发明的化合物是有价值的药用活性化合物，例如，对心脏肌肉和/或迷走神经心脏的ATP敏感钾通道具有抑制作用，例如，适用于治疗心血管系统疾病，如冠心病、心律失常、心功能不全、心肌病、心脏收缩力下降或心脏迷走神经功能障碍，或用于预防心脏猝死。本发明还涉及制备公式(I)的化合物和药用可接受的盐的过程，它们的使用，以及包含它们的药物制剂。
• Heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives, their preparation, their use and pharmaceutical preparations comprising them
  申请人：——

  公开号：US20020123495A1

  公开（公告）日：2002-09-05

  One embodiment of the present invention relates to heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), 1 in which R(1), R(2), R(3), R(4), Het, X, Y and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart, or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.

  本发明的一个实施例涉及式(I)的杂芳基丙烯酰氨基烷基取代的苯磺酰胺衍生物， 1 其中R(1)、R(2)、R(3)、R(4)、Het、X、Y和Z的含义如说明书中所指出的，以及涉及药用可接受的盐。本发明的化合物是有价值的药物活性化合物，例如，对心肌和/或迷走神经心脏的ATP敏感钾通道具有抑制作用，例如，适用于治疗心血管系统疾病，如冠心病、心律失常、心力衰竭、心肌病、心脏收缩力下降或心脏迷走神经功能障碍，或用于预防心脏猝死。本发明还涉及制备式(I)化合物及药用可接受的盐的方法，它们的使用，以及包含它们的药物制剂。
• THERAPEUTIC COMBINATIONS
  申请人：SUPERSALUS, INC.

  公开号：US20200253926A1

  公开（公告）日：2020-08-13

  Methods of treatment include administering effective amounts of a nitrogen oxide (NO) donor (such as nicorandil) and a hydrogen sulfide (H 2 S) releasing agent (such as zofenopril) to a subject in need thereof. In various embodiments, the H 2 S releasing agent is administered in an amount that is effective to enhance the therapeutic efficacy of the NO donor. Coformulations of the H 2 S releasing agent and the NO donor are provided that are suitable for treating a number of conditions. In various embodiments, treatments for conditions such as chronic kidney disease, Duchenne Muscular Dystrophy, Becker Muscular Dystrophy, familial dilated cardiomyopathy and/or idiopathic dilated cardiomyopathy are provided.

  治疗方法包括向需要的对象施用有效量的一氧化氮（NO）供体（如尼可拉地尔）和硫化氢（H2S）释放剂（如左非诺普利）。在各种实施方式中，以有效量施用H2S释放剂以增强NO供体的治疗功效。提供了H2S释放剂和NO供体的联合制剂，适用于治疗多种疾病。在各种实施方式中，提供了治疗慢性肾病、杜兴氏肌肉萎缩症、贝克氏肌肉萎缩症、家族性扩张型心肌病和/或特发性扩张型心肌病等疾病的方法。
• Use of benzenesulfonyl (thioureas or ure as) for treating of septic shock or gene ralized inflammatory syndrome
  申请人：——

  公开号：US20030083385A1

  公开（公告）日：2003-05-01

  The present invention is directed to the use of a benzenesulfonyl(thiourea or urea) of formula I 1 wherein R 1 is hydrogen, (C 1 -C 8 )-alkyl-, (C 3 -C 8 )-cycloalkyl-, (C 3 -C 8 )-cycloalkyl-(C 1 -C 4 )-alkyl- or fluoro-(C 1 -C 8 )-alkyl-; R 2 is (C 1 -C 6 )-alkoxy-, (C 3 -C 8 )-cycloalkyloxy-, (C 3 -C 8 )-cycloalkyl-(C 1 -C 4 )-alkoxy-, (C 1 -C 6 )-alkoxy-(C 1 -C 4 )-alkoxy- or (C 1 -C 6 )-alkoxy-(C 1 -C 4 )-alkoxy-(C 1 -C 4 )-alkoxy-; E is oxygen or sulfur; Y is a hydrocarbon residue of formula —(CR 3 2 ) n —, wherein the residues R 3 , all independently of each other, are hydrogen or (C 1 -C 2 )-alkyl, and n is 1, 2, 3 or 4; X is hydrogen, halogen or (C 1 -C 6 )-alkyl; and Z is halogen, (C 1 -C 4 )-alkyl-, fluoro-(C 1 -C 4 )-alkyl-, (C 1 -C 4 )-alkoxy- or fluoro-(C 1 -C 4 )-alkoxy-, or a physiologically tolerable salt thereof or solvate thereof, for treating a patient suffering from septic shock or the generalized inflammatory syndrome (SIRS) comprising administering to the patient a pharmaceutically effective amount of the compound of formula I, or a physiologically tolerable salt thereof or solvate thereof. The invention is also directed to the use of benzenesulfonyl(thioureas or ureas) of formula I, or a physiologically tolerable salt thereof or solvate thereof, for treating a patient suffering from pathological changes in blood pressure due to a septic shock or generalized inflammatory syndrome (SIRS) state, comprising administering to the patient a pharmaceutically effective amount of the compounds of formula I, or a physiologically tolerable salt thereof or solvate thereof.

  本发明涉及使用式I1的苯磺酰基（硫脲或脲）的方法，其中R1是氢、（C1-C8）-烷基、（C3-C8）-环烷基、（C3-C8）-环烷基-(C1-C4)-烷基或氟代（C1-C8）-烷基；R2是（C1-C6）-烷氧基、（C3-C8）-环烷氧基、（C3-C8）-环烷基-(C1-C4)-烷氧基、（C1-C6）-烷氧基-(C1-C4)-烷氧基或（C1-C6）-烷氧基-(C1-C4)-烷氧基-(C1-C4)-烷氧基；E是氧或硫；Y是式—（CR32）n—的烃基残基，其中残基R3都是独立的氢或（C1-C2）-烷基，n为1、2、3或4；X是氢、卤素或（C1-C6）-烷基；Z是卤素、（C1-C4）-烷基、氟代（C1-C4）-烷基、（C1-C4）-烷氧基或氟代（C1-C4）-烷氧基，或其生理上可耐受的盐或溶剂，用于治疗患有感染性休克或全身性炎症综合征（SIRS）的患者，包括向患者投予式I的化合物的药物有效量，或其生理上可耐受的盐或溶剂。本发明还涉及使用式I的苯磺酰基（硫脲或脲）或其生理上可耐受的盐或溶剂，用于治疗由感染性休克或全身性炎症综合征（SIRS）状态引起的血压病理变化的患者，包括向患者投予式I的化合物的药物有效量，或其生理上可耐受的盐或溶剂。
• USE OF BENZENESULFONYL(THIO)UREAS FOR THE TREATMENT AND PROPHYLAXIS OF DYSFUNCTIONS OF THE AUTONOMOUS NERVOUS SYSTEM AND USE OF BENZENESULFONYL(THIO)UREAS IN COMBINATION WITH BETA-RECEPTOR BLOCKERS
  申请人：——

  公开号：US20020082300A1

  公开（公告）日：2002-06-27

  Substituted benzenesulfonylureas and -thioureas of the formula I 1 in which R 1 , R 2 , E, X, Y and Z have the meanings described herein, show effects on the autonomous nervous system. The invention relates to the use of the compounds of the formula I in the treatment and prophylaxis of dysfunctions of the autonomous nervous system, in particular of vagal dysfunctions, for example in the case of cardiovascular diseases. The invention also relates to the use of compounds of the formula I in combination with beta-receptor blockers and to products and pharmaceutical preparations which comprise at least one compound of the formula I and at least one beta-receptor blocker, and to novel compounds.

  公式I1中的取代苯磺酰脲和-硫脲化合物，其中R1、R2、E、X、Y和Z的含义如下所述，对自主神经系统产生影响。本发明涉及将公式I中的化合物用于治疗和预防自主神经系统功能障碍，特别是迷走神经功能障碍，例如在心血管疾病的情况下。本发明还涉及将公式I中的化合物与β-受体阻滞剂结合使用，以及至少包括公式I中至少一种化合物和至少一种β-受体阻滞剂的产品和制药制剂，以及新化合物。