2-[2-Amino-2-[1-(1-fluoroethenyl)cyclopentyl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile

• 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: 2-[2-Amino-2-[1-(1-fluoroethenyl)cyclopentyl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
• 化学式: C₁₅H₂₀FN₃O
• 分子量: 277.34
• InChiKey: MIJLRCUAILZBET-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.73
• 拓扑面积：
  70.1
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• N-Protected amino hydroxy adamantane carboxylic acid and process for its preparation
  申请人：Bristol-Myers Squibb Company

  公开号：EP2272825A2

  公开（公告）日：2011-01-12

  Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula (I) where x is 0 or 1 and y is 0 or 1 (provided that x = 1 when y = 0 and x = 0 when y = 1); n is 0 or 1; X is H; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity and/or other therapeutic agent.

  提供了具有式（I）的二肽基肽酶 IV（DP 4）抑制化合物 其中 x 为 0 或 1，y 为 0 或 1（条件是当 y = 0 时 x = 1，当 y = 1 时 x = 0）；n 为 0 或 1；X 为 H；其中 R1、R2、R3 和 R4 如本文所述。还提供了一种治疗糖尿病和相关疾病，特别是II型糖尿病，以及本文所述的其他疾病的方法，该方法采用了这种DP 4抑制剂或这种DP 4抑制剂与另一种或多种抗糖尿病剂如二甲双胍、甘氟脲、曲格列酮、吡格列酮、罗格列酮和/或胰岛素和/或一种或多种降血脂剂和/或抗肥胖和/或其他治疗剂的组合。
• Coated tablet formulation and method
  申请人：Bristol-Myers Squibb Company

  公开号：EP2298288A1

  公开（公告）日：2011-03-23

  A coated tablet formulation is provided which includes a medicament such as the DPP4-inhibitor, saxaglipitin, formula (I), or its HCl salt, which is subject to intra-molecular cyclization, which formulation includes a tablet core containing one or more fillers, and other conventional excipients, which tablet core includes a coating thereon which may include two or more layers, at least one layer of which is an inner seal coat layer which is formed of one or more coating polymers, a second layer of which is formed of medicament which is the DPP4-inhibitor and one or more coating polymers, and an optional, but preferable third outer protective layer which is formed of one or more coating polymers. A method for forming the coated tablet is also provided.

  本发明提供了一种包衣片剂，其中包括可发生分子内环化的药物，如 DPP4 抑制剂、沙格雷利定、式（I）或其盐酸盐，该制剂包括含有一种或多种填料和其他常规赋形剂的片芯，片芯上有一层包衣，包衣可包括两层或多层、其中至少一层是由一种或多种包衣聚合物形成的内密封包衣层，第二层是由作为 DPP4 抑制剂的药物和一种或多种包衣聚合物形成的包衣层，第三层是由一种或多种包衣聚合物形成的可选但优选的外保护层。此外，还提供了一种形成包衣片剂的方法。
• CYCLOPROPYL-FUSED PYRROLIDINE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV, PROCESSES FOR THEIR PREPARATION, AND THEIR USE
  申请人：Bristol-Myers Squibb Company

  公开号：EP1261586B1

  公开（公告）日：2008-05-21