(2S)-N-[[4-[(E)-N'-methoxycarbamimidoyl]phenyl]methyl]azetidine-2-carboxamide

• 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: (2S)-N-[[4-[(E)-N'-methoxycarbamimidoyl]phenyl]methyl]azetidine-2-carboxamide
• 化学式: C₁₃H₁₈N₄O₂
• 分子量: 262.31
• InChiKey: UBYQUTKTYAAORW-NSHDSACASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  88.7
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• New Salts
  申请人：Ahlqvist Matti

  公开号：US20080269176A1

  公开（公告）日：2008-10-30

  There is provided pharmaceutically-acceptable acid addition salts of compounds of formula (I), wherein R 1 represents C 1-2 alkyl substituted by one or more fluoro substituents; R 2 represents C 1-2 alkyl; and n represents 0, 1 or 2, which salts are useful as prodrugs of competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required.

  提供了一种公式(I)化合物的药用酸加成盐，其中R1代表一种或多种氟代取代的C1-2烷基；R2代表C1-2烷基；n代表0、1或2。这些盐可用作竞争性蛋白酶抑制剂的前药，如凝血酶，因此特别适用于治疗需要抑制凝血酶的情况。
• Acid addition salts of mandelic acid derivatives
  申请人：AstraZeneca AB

  公开号：EP2055696A1

  公开（公告）日：2009-05-06

  There are provided pharmaceutically-acceptable acid addition salts of compounds of formula I, wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents; R2 represents G1-2 alkyl; n represents 0, 1 or 2; and wherein the acid addition salt is an inorganic acid addition salt, an organic acid addition salt, a carboxylic acid addition salt, a hydroxy acid addition salt or an amino acid addition salt; which salts are useful as prodrugs of competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

  提供了式 I 化合物的药学上可接受的酸加成盐、 其中 R1 代表被一个或多个氟取代基取代的 C1-2 烷基； R2代表G1-2烷基；n代表0、1或2；其中的酸加成盐是无机酸加成盐、有机酸加成盐、羧酸加成盐、羟基酸加成盐或氨基酸加成盐；这些盐可作为胰蛋白酶样蛋白酶（如凝血酶）的竞争性抑制剂的原药，因此特别适用于治疗需要抑制凝血酶的病症（如血栓形成）或作为抗凝剂。
• NEW CRYSTALLINE FORMS
  申请人：Aslund Bengt Leonard

  公开号：US20080287413A1

  公开（公告）日：2008-11-20

  There are provided crystalline forms of the compounds Ph(3-Cl)(5-OCHF 2 )—(R)CH(OH)C(O)-Aze-Pab(OMe) and Ph(3-Cl)(5-OCHF 2 )—(R)CH(OH)C(O)-Aze-Pab(OH), pharmaceutical compositions containing them, processes for obtaining them and their use in medical treatment.
• US7273858B2
  申请人：——

  公开号：US7273858B2

  公开（公告）日：2007-09-25
• US7763597B2
  申请人：——

  公开号：US7763597B2

  公开（公告）日：2010-07-27