2-Amino-5-hydroxyhexanoic acid

• 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-Amino-5-hydroxyhexanoic acid
• 化学式: C₆H₁₃NO₃
• mdl: MFCD19203864
• 分子量: 147.17
• InChiKey: CQUIPUAMBATVOP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.9
• 重原子数：
  10
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.833
• 拓扑面积：
  83.6
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• FAP-activated anti-tumor compounds
  申请人：——

  公开号：US20030232742A1

  公开（公告）日：2003-12-18

  The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug is chemically stable under physiological conditions and can be used for the manufacture of physically stable aqueous formulations. It has a cleavage site which is recognised by FAP&agr;, and the drug released by the enzymatic activity of FAP&agr; is cytotoxic or cytostatic under physiological conditions.

  该发明涉及一种前药，它能够通过人类成纤维细胞活化蛋白（FAPα）的催化作用转化为药物，所述前药在生理条件下化学稳定，并可用于制备物理稳定的水性配方。它具有一个被FAPα识别的裂解位点，由FAPα的酶活性释放的药物在生理条件下具有细胞毒性或细胞静止作用。
• FAP-activated anti-tumor prodrugs
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：US20040033957A1

  公开（公告）日：2004-02-19

  The present invention relates to prodrugs which are capable of being converted into prodrug intermediates of a cytotoxic or cytostatic drug, by the catalytic action of FAP&agr;, said prodrugs exhibit an oligomeric part comprising up to 9 amino carboxylic acid residues, the amide bond between the C-terminal amino carboxylic acid and the preceding amino acid thereof is recognized and cleaved by FAP&agr; in the immediate environment of a target cell, and a cytotoxic or cytostatic part, wherein the N-terminal amino function of the oligomeric part is attached to a capping group (Cg).

  本发明涉及能够在 FAP&agr 催化作用下转化为细胞毒性或细胞抑制药物的原药中间体的原药，所述原药表现为 由最多 9 个氨基羧酸残基组成的低聚物部分，在靶细胞的直接环境中，C 端氨基羧酸与前一个氨基之间的酰胺键被 FAP&agr 识别并裂解，以及 细胞毒性或细胞抑制部分，其中低聚物部分的 N 端氨基功能连接到一个封顶基团（Cg）上。
• Methods for treating diabetes
  申请人：Jesson I. Michael

  公开号：US20060063719A1

  公开（公告）日：2006-03-23

  The invention relates to compositions of Glu-boroPro and methods of use thereof in the prevention or management of type 2 diabetes.

  本发明涉及 Glu-boroPro 组合物及其用于预防或治疗 2 型糖尿病的方法。
• Methods and compositions for treating glucose-associated conditions, metabolic syndrome, dyslipidemias and other conditions
  申请人：Aziz Nazneen

  公开号：US20060094693A1

  公开（公告）日：2006-05-04

  The invention relates, in part, to of Glu-boroPro containing compounds and methods of use thereof in the prevention or management of conditions that are associated with impaired glucose tolerance such as diabetes. The invention also relates to compositions of Glu-boroPro containing compounds and methods of use thereof in the prevention or management of conditions such as metabolic syndrome, dyslipidemias, inflammation, cardiovascular disorders such as hypertension and atherosclerosis, and to reduce body weight or prevent weight gain. The compounds of the invention are also useful in lowering levels of triglycerides, free fatty acids, C-reactive protein (CRP), HbA 1 C, total glycosylated hemoglobin (TGHb), in increasing insulin sensitivity index and in stimulating insulin release.

  本发明部分涉及含 Glu-boroPro 的化合物及其在预防或治疗糖尿病等葡萄糖耐量受损相关疾病中的使用方法。本发明还涉及含 Glu-boroPro 化合物的组合物及其在预防或治疗代谢综合征、血脂异常、炎症、高血压和动脉粥样硬化等心血管疾病以及减轻体重或防止体重增加中的使用方法。本发明的化合物还能降低甘油三酯、游离脂肪酸、C 反应蛋白 (CRP)、HbA 1 C、总糖化血红蛋白 (TGHb)、增加胰岛素敏感性指数和刺激胰岛素释放等方面也有作用。
• FAP-ACTIVATED ANTI-TUMOR COMPOUNDS
  申请人：Boehringer Ingelheim Pharma KG

  公开号：EP1180116A2

  公开（公告）日：2002-02-20