5-(2-aminoethyl)-2-methoxybenzenesulfonamide | 308336-31-4

• 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: 5-(2-aminoethyl)-2-methoxybenzenesulfonamide
• 英文别名: 2-[3-(aminosulfonyl)-4-methoxyphenyl]ethylamine；5-(2-aminoethyl)-2-(methyloxy)benzenesulfonamide；5-(2-Aminoethyl)-2-methoxybenzene-sulphonamide
• CAS: 308336-31-4
• 化学式: C₉H₁₄N₂O₃S
• mdl: MFCD27920007
• 分子量: 230.288
• InChiKey: PZRHMFALYBNXGC-UHFFFAOYSA-N

物化性质

• 沸点：
  446.6±55.0 °C(Predicted)
• 密度：
  1.287±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  104
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-(2-aminoethyl)-2-methoxybenzenesulfonamide 在 三溴化硼 、 甲醇 作用下， 以 二氯甲烷 为溶剂， 反应 5.0h， 以40%的产率得到5-(2-aminoethyl)-2-hydroxybenzenesulfonamide hydrobromide
  参考文献：
  名称：

  [EN] PYRIMIDINE DERIVATIVES USED AS ITK INHIBITORS
  [FR] DÉRIVÉS DE PYRIMIDINE UTILISÉS COMME INHIBITEURS DE LTK

  摘要：

  本发明涉及某些新颖化合物。具体而言，本发明涉及以下公式（I）的化合物及其盐类。发明的化合物是激酶活性的抑制剂，特别是ltk活性的抑制剂。

  公开号：

  WO2010106016A1
• 作为产物：
  描述：

  5-<2-(tifluoroacetylamino)ethyl>-2-methoxybenzenesulfonamide 在 sodium hydroxide 作用下， 以 甲醇 为溶剂， 反应 0.5h， 生成 5-(2-aminoethyl)-2-methoxybenzenesulfonamide
  参考文献：
  名称：

  Novel Phenoxyalkylamine Derivatives. VII. Synthesis and Pharmacological Activities of 2-Alkoxy-5-((phenoxyalkylamino)alkyl)benzenesulfonamide Derivatives.

  摘要：

  为了找到一种对多巴胺D2受体亲和力具有高选择性的新的α-拮抗剂，我们对2-烷氧基-5-[(苯氧烷基氨基)烷基]苯磺酰胺衍生物的烷基链及两个苯环上的取代基进行了结构改造。发现位于分子中心的氨基部分与苯环（环A）之间的烷基链的改造是最显著的。具备1-甲基乙基作为烷基链的5-[2-[[2-(5-氟-2-甲氧基苯氧基)乙基]氨基]丙基]-2-甲氧基苯磺酰胺（II-4）表现出高α-拮抗选择性以及强效的α-拮抗活性。

  DOI：

  10.1248/cpb.40.1443

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。
• Cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives, processes for their preparation, their use, and pharmaceutical preparations comprising them
  申请人：Aventis Pharma Deutschland GmbH

  公开号：US06350778B1

  公开（公告）日：2002-02-26

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

  本发明涉及公式I的肉桂酰氨基烷基取代的苯磺酰胺衍生物 其中A(1)，A(2)，A(3)，R(1)，R(2)，R(3)，R(4)，X，Y和Z的含义如权利要求所述。公式I的化合物是有价值的药物活性化合物，例如，对心脏肌肉和/或心脏神经中的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，心功能不全或心肌病，或预防心脏猝死，或改善心脏收缩功能降低。本发明还涉及制备公式I化合物的方法，其用途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。
• 2'-Methyl-5-(1,3,4-oxadiazol-2-yl)1,1'-biphenyl-4-carboxaide derivatives and their use as p38 kinase inhibitors
  申请人：——

  公开号：US20040266839A1

  公开（公告）日：2004-12-30

  Compounds of formula (I), wherein R 1 is a phenyl group which may be optionally substituted; R 2 is selected from hydrogen, C 1-6 alkyl and (CH 2 ) p —C 3-7 cycloalkyl; R 3 is the group: (Formula II), R 4 is selected from hydrogen and C 1-4 alkyl; U is selected from methyl and halogen; X and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4, and may be optionally substituted with up to two groups selected independently from C 1-6 alkyl; n is selected from 0, 1 and 2; p is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. 1

  公式（I）的化合物，其中R1是苯基，可以选择性地被取代；R2选自氢、C1-6烷基和(CH2)p-C3-7环烷基；R3是基团：（公式II），R4选自氢和C1-4烷基；U选自甲基和卤素；X和Y各自独立地选自氢、甲基和卤素；m选自0、1、2、3和4，并且可以选择性地被最多两个独立选择自C1-6烷基的基团取代；n选自0、1和2；p选自0、1和2；或其药学上可接受的盐或溶剂，以及它们作为药物的用途，特别是作为p38激酶抑制剂。
• Preventives/remedies for urinary disturbance
  申请人：Ishihara Yuji

  公开号：US20050197362A1

  公开（公告）日：2005-09-08

  Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.

  具有乙酰胆碱酯酶抑制作用和α1拮抗作用的化合物的预防/治疗措施，可以显著改善膀胱的尿液功能（即改善尿流率和排尿效率的效果），而不影响尿压或血压。