L-Lysinamide, L-valyl-L-leucyl-N-(4-nitrophenyl)- | 64816-15-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: L-Lysinamide, L-valyl-L-leucyl-N-(4-nitrophenyl)-
• 英文别名: (2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-N-(4-nitrophenyl)hexanamide
• CAS: 64816-15-5
• 化学式: C23H38N6O5
• 分子量: 478.6
• InChiKey: CAJXYXPLLJDEOB-UFYCRDLUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  34
• 可旋转键数：
  13
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  185
• 氢给体数：
  5
• 氢受体数：
  7

文献信息

• Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them
  申请人：Aventis Pharma Deutschland GmbH

  公开号：EP1022268A1

  公开（公告）日：2000-07-26

  The present invention relates to new compounds for the inhibition of blood clotting proteins, and more particularly, to arylalkanoyl derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), R(6a) and R(6b) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula I, to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, to and the use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

  本发明涉及用于抑制血液凝固蛋白的新化合物，更具体地，是指式I的芳烷酰衍生物， 其中R(1)、R(2)、R(3)、R(4)、R(5)、R(6a)和R(6b)的含义如权利要求中所示。式I的化合物是血液凝固酶因子Xa的抑制剂。本发明还涉及制备式I化合物的方法，抑制因子Xa活性和血液凝固的方法，使用式I化合物治疗和预防可以通过抑制因子Xa活性来治疗或预防的疾病，如血栓栓塞性疾病，以及使用式I化合物制备用于治疗上述疾病的药物。本发明还涉及包含式I化合物的组合物，与惰性载体混合或以其他方式相关联，尤其是包含式I化合物的药物组合物，以及药用可接受的载体物质和辅助物质。
• Novel malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them
  申请人：——

  公开号：US20020022596A1

  公开（公告）日：2002-02-21

  The present invention relates to new malonic acid derivatives of the formula 1, 1 wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula 1, to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

  本发明涉及公式1,1的新马隆酸衍生物，其中R(1)、R(2)、R(3)、R(4)、R(5)和R(6)具有声明中指示的含义。公式I的化合物是血凝酶因子Xa的抑制剂。本发明还涉及制备公式1化合物的方法，抑制因子Xa活性和抑制血凝的方法，以及使用公式I化合物在治疗和预防可以通过抑制因子Xa活性治疗或预防的疾病中的应用，例如血栓栓塞性疾病，以及使用公式I化合物制备在这些疾病中应用的药物。本发明还涉及含有公式I化合物的组合物与惰性载体混合或以其他方式结合，特别是含有公式I化合物与药用载体物质和辅助物质的制药组合物。
• Triprenyl phenol compound, process for production of triprenyl phenol compound, and thrombolysis enhancer
  申请人：Hasumi Keiji

  公开号：US20090216028A1

  公开（公告）日：2009-08-27

  The present invention provides a triprenyl phenol compound represented by the following formula (II) and (III) and having a thrombolysis-enhancing activity, and an efficient method for producing the triprenyl phenol compound. In formula (II) and (III), R 1 represents an aromatic group having as a substituent or as a part of a substituent at least one member selected from the group consisting of a carboxyl group, a hydroxyl group, a sulfonic acid group and a secondary amino group, or an aromatic group which comprises a secondary amino group and may comprise nitrogen; R 4 in the general formula (III) represents an aromatic amino acid residue represented by the general formula (III-1) below; X represents —CHY—(CH 3 ) 2 Z; and Y and Z are respectively —H or —OH or together form a single bond: (III-1) wherein R 5 represents a hydroxyl group which may be present or absent; and n represents an integer of 0 or 1.

  本发明提供了一种由以下化学式（II）和（III）所代表的三倍萜酚化合物，具有增强溶栓活性，以及一种高效制备该三倍萜酚化合物的方法。在化学式（II）和（III）中，R1代表芳香基团，其作为取代基或取代基的一部分至少包括羧基、羟基、磺酸基和二级氨基组成的群中的一种，或者是包含二级氨基并可能包含氮的芳香基团；在通式（III）中，R4代表由通式（III-1）所表示的芳香氨基酸残基；X代表—CHY—（CH3）2Z；Y和Z分别为—H或—OH或形成单键：（III-1）其中，R5代表可能存在或不存在的羟基；n代表0或1的整数。
• TRIPRENYL PHENOL COMPOUND, PROCESS FOR PRODUCTION OF TRIPRENYL PHENOL COMPOUND, AND THROMBOLYSIS ENHANCER
  申请人：HASUMI Keiji

  公开号：US20120100579A1

  公开（公告）日：2012-04-26

  A triprenyl phenol compound represented by the following formula (II) and (III) and having a thrombolysis-enhancing activity, and an efficient method for producing the triprenyl phenol compound. In formula (II) and (III), R 1 represents an aromatic group having as a substituent or as a part of a substituent at least one member selected from the group consisting of a carboxyl group, a hydroxyl group, a sulfonic acid group and a secondary amino group, or an aromatic group which comprises a secondary amino group and may comprise nitrogen; R 4 in the general formula (III) represents an aromatic amino acid residue represented by the general formula (III-1) below; X represents —CHY—(CH 3 ) 2 Z; and Y and Z are respectively —H or —OH or together form a single bond: (III-1) wherein R 5 represents a hydroxyl group which may be present or absent; and n represents an integer of 0 or 1.

  以下为一种由式子（II）和（III）所代表的三倍半萜酚类化合物，具有促进溶血性的活性，以及一种高效的制备该三倍半萜酚类化合物的方法。在式子（II）和（III）中，R1代表一种芳香基团，其作为一个取代基或部分取代基，至少包含羧基、羟基、磺酸基和次级氨基中的一种，或者是包含次级氨基且可能包含氮的芳香基团；在一般式（III）中，R4代表由一般式（III-1）所表示的芳香氨基酸残基；X代表—CHY—（CH3）2Z；Y和Z分别代表—H或—OH，或者一起形成一个单键：（III-1）其中R5代表可能存在或不存在的羟基；n代表0或1的整数。
• Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity)
  申请人：Aventis Pharma Deutschland GmbH

  公开号：EP1016663A1

  公开（公告）日：2000-07-05

  The present invention relates to new compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula I, to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

  本发明涉及用于抑制凝血蛋白的新化合物，尤其涉及式 I 的丙二酸衍生物、 其中R(1)、R(2)、R(3)、R(4)、R(5)和R(6)具有权利要求中所述的含义。式 I 的化合物是血液凝固酶 Xa 因子的抑制剂。本发明还涉及制备式 I 化合物的工艺，涉及抑制因子 Xa 活性和抑制血液凝固的方法，涉及式 I 化合物在治疗和预防疾病中的用途，这些疾病可通过抑制因子 Xa 活性来治疗或预防，如血栓栓塞性疾病，还涉及式 I 化合物在制备用于此类疾病的药物中的用途。本发明还涉及含有与惰性载体混合或以其他方式结合的式 I 化合物的组合物，特别是含有式 I 化合物与药学上可接受的载体物质和辅助物质的药物组合物。