3-(5-Chloro-thiophene-2-sulfonylamino)-N-[4-(3-oxo-morpholin-4-yl)-phenyl]-propionamide | 863015-65-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 3-(5-Chloro-thiophene-2-sulfonylamino)-N-[4-(3-oxo-morpholin-4-yl)-phenyl]-propionamide
• 英文别名: 3-[(5-chlorothiophen-2-yl)sulfonylamino]-N-[4-(3-oxomorpholin-4-yl)phenyl]propanamide
• CAS: 863015-65-0
• 化学式: C₁₇H₁₈ClN₃O₅S₂
• 分子量: 443.932
• InChiKey: PDLVJUFYJWJKIV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  28
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  141
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  3-(5-Chloro-thiophene-2-sulfonylamino)-propionic acid 、 propylphosphonic anhydride, O-((cyano-(ethoxycarbonyl)-methylene)amino)-N,N,N',N'-tetramethyluronium tetrafluoroborate 、 4-(4-氨基苯基)吗啡啉-3-酮 在 三乙胺 、 三氟乙酸 作用下， 以 水 、 N,N-二甲基甲酰胺 为溶剂， 生成 3-(5-Chloro-thiophene-2-sulfonylamino)-N-[4-(3-oxo-morpholin-4-yl)-phenyl]-propionamide
  参考文献：
  名称：

  Beta-aminoacid-derivatives as factor Xa inhibitors

  摘要：

  本发明涉及式I的化合物，其中R0; R1; R2; R3; R4; R5，R6，Q; V，G和M具有索赔中指示的含义。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，如血栓栓塞疾病或再狭窄。它们是血凝酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，通常可应用于存在因子Xa和/或因子VIIa的不良活性或对其进行抑制的治疗或预防的情况。此外，本发明涉及式I化合物的制备方法，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。

  公开号：

  EP1571154A1

文献信息

• Beta-Aminoacid-Derivatives As Factor Xa Inhibitors
  申请人：Urmann Matthias

  公开号：US20070179122A1

  公开（公告）日：2007-08-02

  The present invention relates to compounds of the formula I, in which R 0 ; R 1 ; R 2 ; R 3 ; R 4 ; R 5 , R, Q; V, G and M 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 thromboemboic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa 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.

  本发明涉及公式I的化合物，其中R0；R1；R2；R3；R4；R5，R，Q；V，G和M具有所述权利要求中指示的含义。公式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，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。它们是血凝酶酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，通常可应用于存在因子Xa和/或因子VIIa的不良活性或预防其抑制因子Xa和/或因子VIIa的治疗或预防。此外，本发明还涉及制备公式I化合物的过程，它们的用途，特别是作为药物中的活性成分，以及包含它们的制药制剂。
• BETA-AMINOACID-DERIVATIVES AS FACTOR Xa INHIBITORS
  申请人：Sanofi-Aventis Deutschland GmbH

  公开号：EP1723164A1

  公开（公告）日：2006-11-22
• [EN] BETA-AMINOACID-DERIVATIVES AS FACTOR Xa INHIBITORS<br/>[FR] DERIVES BETA-AMINOACIDE EN TANT QU'INHIBITEURS DU FACTEUR XA
  申请人：AVENTIS PHARMA GMBH

  公开号：WO2005095440A1

  公开（公告）日：2005-10-13

  The present invention relates to compounds of the Formula (I), in which R°; R1; R2; R3; R4; R5; R6; Q; V; G and M 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 (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa 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.