2-amino-ethanesulfonic acid (1-cyclopropyl-piperidin-4-yl)-amide | 915373-90-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 2-amino-ethanesulfonic acid (1-cyclopropyl-piperidin-4-yl)-amide
• 英文别名: 2-amino-N-(1-cyclopropylpiperidin-4-yl)ethanesulfonamide
• CAS: 915373-90-9
• 化学式: C₁₀H₂₁N₃O₂S
• 分子量: 247.362
• InChiKey: WQEBWMQVVGVQQT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  16
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  83.8
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-氯噻吩-5-甲酸 、 2-amino-ethanesulfonic acid (1-cyclopropyl-piperidin-4-yl)-amide 在 5-Chloro-thiophene-2-carboxylic acid [2-(1-cyclopropyl-piperidin-4-ylsulfamoyl)-ethyl]-amide 、 acetonitrile-water 、 三氟乙酸 作用下， 以gave pure 5-chloro-thiophene-2-carboxylic acid [2-(1-cyclopropyl-piperidin-4-ylsulfamoyl)-ethyl]-amide的产率得到5-Chloro-thiophene-2-carboxylic acid [2-(1-cyclopropyl-piperidin-4-ylsulfamoyl)-ethyl]-amide
  参考文献：
  名称：

  Heteroaryl-carboxylic acid (sulfamoyl alkyl) amide-derivatives as factor Xa inhibitors

  摘要：

  本发明涉及公式I的化合物，其表现出强烈的抗血栓作用，例如适用于治疗和预防心血管疾病，如血栓栓塞性疾病或再狭窄。

  公开号：

  US08088925B2

文献信息

• Heteroaryl-carboxylic acid (sulfamoyl alkyl) amide - derivatives as factor Xa inhibitors
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：EP1724269A1

  公开（公告）日：2006-11-22

  The present invention relates to compounds of the formula I, in which R1; R2; R3; V; G1 and G2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa, and can in general be applied in conditions in which an undesired activity of factor Xa is present or for the cure or prevention of which an inhibition of factor Xa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

  本发明涉及具有以下式I的化合物，其中R1; R2; R3; V; G1和G2具有声明中指示的含义。式I的化合物是有价值的药理活性化合物。它们表现出强烈的抗血栓作用，例如，适用于治疗和预防心血管疾病，如血栓栓塞性疾病或再狭窄。它们是血凝酶因子Xa的可逆抑制剂，通常可应用于存在血凝酶因子Xa不良活性的情况或者预期抑制血凝酶因子Xa以治疗或预防的情况。此外，该发明还涉及制备具有式I的化合物的方法，它们的用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。
• HETEROARYL-CARBOXYLIC ACID (SULFAMOYL ALKYL) AMIDE - DERIVATIVES AS FACTOR XA INHIBITORS
  申请人：WAGNER Michael

  公开号：US20080167346A1

  公开（公告）日：2008-07-10

  The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.

  本发明涉及公式I的化合物，其表现出强烈的抗血栓作用，并适用于治疗和预防心血管疾病，如血栓栓塞性疾病或再狭窄。
• US8088925B2
  申请人：——

  公开号：US8088925B2

  公开（公告）日：2012-01-03
• [EN] HETEROARYL-CARBOXYLIC ACID (SULFAMOYL ALKYL) AMIDE - DERIVATIVES AS FACTOR XA INHIBITORS<br/>[FR] DERIVES D'AMIDE DE L'ACIDE HETEROARYLE CARBOXYLIQUE (ALKYLE DE SULFAMOYLE) EN TANT QU'INHIBITEURS DU FACTEUR XA
  申请人：SANOFI AVENTIS DEUTSCHLAND

  公开号：WO2006122661A1

  公开（公告）日：2006-11-23

  [EN] The present invention relates to compounds of the Formula (I), in which R1; R2; R3; V; G1 and G2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa, and can in general be applied in conditions in which an undesired activity of factor Xa is present or for the cure or prevention of which an inhibition of factor Xa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
  [FR] La présente invention concerne des composés de formule (I), dans laquelle R1; R2; R3; V; G1 et G2 ont les significations indiquées dans les revendications. Les composés de formule (I) sont des composés de valeur actifs sur le plan pharmacologique. Ils montrent un effet antithrombotique fort et sont adéquats, par exemple, pour la thérapie et la prophylaxie des troubles cardiovasculaires comme les maladies thromboemboliques ou la resténose. Ce sont des inhibiteurs réversibles du facteur Xa des enzymes de coagulation, et ils peuvent en général être appliqués dans des conditions dans lesquelles une activité non désirée du facteur Xa est présente ou pour le traitement ou la prévention desquelles une inhibition du facteur Xa est voulue. L'invention concerne de plus les procédés pour la préparation des composés de formule (I), leur utilisation, en particulier comme ingrédients actifs dans les produits pharmaceutiques, et les préparations pharmaceutiques les comprenant.