(2R,3S)-2-bromo-3-methylpentanoic acid | 32653-36-4

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: (2R,3S)-2-bromo-3-methylpentanoic acid
• 英文别名: (+)(2R:3S)-2-bromo-3-methyl-valeric acid；(+)(2R:3S)-2-Brom-3-methyl-valeriansaeure
• CAS: 32653-36-4
• 化学式: C₆H₁₁BrO₂
• 分子量: 195.056
• InChiKey: GQZXYZIKUQUVKE-CRCLSJGQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  9
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2R,3S)-2-bromo-3-methylpentanoic acid 在 氯化亚砜 作用下， 生成 chloride of/the/ (+)(2R:3S)-2-bromo-3-methyl-valeric acid
  参考文献：
  名称：

  Abderhalden; Zeisset, Hoppe-Seyler's Zeitschrift fur Physiologische Chemie, 1931, vol. 200, p. 186

  摘要：

  DOI：
• 作为产物：
  描述：

  D-别异亮氨酸 在 氢溴酸 、 sodium nitrite 作用下， 以 水 为溶剂， 反应 16.0h， 生成 (2R,3S)-2-bromo-3-methylpentanoic acid
  参考文献：
  名称：

  ANTAGONISTS OF HUMAN INTEGRIN (ALPHA4)(BETA7)

  摘要：

  揭示了α4β7整合素的小分子拮抗剂，以及使用它们治疗多种特定疾病或病况的方法。

  公开号：

  US20190315692A1

文献信息

• ANTAGONISTS OF HUMAN INTEGRIN (ALPHA4)(BETA7)
  申请人：Morphic Therapeutic, Inc.

  公开号：US20190315692A1

  公开（公告）日：2019-10-17

  Disclosed are small molecule antagonists of α4β7 integrin, and methods of using them to treat a number of specific diseases or conditions.

  揭示了α4β7整合素的小分子拮抗剂，以及使用它们治疗多种特定疾病或病况的方法。
• Thio-containing inhibitors of aminopeptidase P, compositions thereof and method of use
  申请人：Simmons H. William

  公开号：US20070060525A1

  公开（公告）日：2007-03-15

  The present invention is directed to an α thio-containing compound that is capable of inhibiting the enzyme, membrane aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The compound is useful as a pharmaceutical agent because by inhibiting bradykinin degradation, the compound allows bradykinin to exert its beneficial effects on the cardiovascular system, to improve renal function, and to improve glucose tolerance and insulin-sensitivity. The present invention is also directed to a pharmaceutical composition comprising the mAPP inhibitor of the present invention and a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, preferably human, in need of treatment comprising administering to the patient a therapeutically effective amount of an α thio-containing compound of the present invention. The method of the present invention also contemplates the further step of administering to the mammalian patient in need of treatment a therapeutically effective amount of an inhibitor of angiotensin converting enzyme (ACE).

  本发明涉及一种含α硫基的化合物，能够抑制酶、膜氨肽酶P（mAPP或APP），其天然底物为激肽。该化合物可用作药物代理，因为通过抑制激肽降解，使激肽能够在心血管系统上发挥其有益作用，改善肾功能，并改善葡萄糖耐量和胰岛素敏感性。本发明还涉及一种含有本发明mAPP抑制剂和药用可接受载体的药物组合物。另一方面，本发明涉及一种在需要治疗的哺乳动物患者，优选为人类，中抑制激肽降解的方法，包括向患者投予本发明的α硫基化合物的治疗有效量。本发明的方法还包括向需要治疗的哺乳动物患者投予抑制肾素转化酶（ACE）的治疗有效量的进一步步骤。
• Amino acid derivative
  申请人：Eisai Co., Ltd.

  公开号：US05679671A1

  公开（公告）日：1997-10-21

  The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity. This amino acid derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent; m and n represent each independently an integer of 0, 1 or 2 and J represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.

  本发明涉及一种具有血管紧张素转化酶抑制活性、抗利尿激素和心房利钠肽水解酶抑制活性的氨基酸衍生物。该氨基酸衍生物由下列通式(I)表示：##STR1##其中，R1代表氢原子或酰基；R2代表氢原子、较低的烷基、环烷基、可能具有取代基的芳基、可能具有取代基的杂芳基、可能具有取代基的芳基烷基、或可能具有取代基的杂芳基烷基；m和n分别独立地表示0、1或2的整数，J表示具有血管紧张素转化酶抑制活性的环状基团。
• Thio-containing inhibitors of aminopeptidase P, and compositions thereof
  申请人：——

  公开号：US07390789B2

  公开（公告）日：2008-06-24

  The present invention is directed to an α thio-containing compound that is capable of inhibiting the enzyme, membrane aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The compound is useful as a pharmaceutical agent because by inhibiting bradykinin degradation, the compound allows bradykinin to exert its beneficial effects on the cardiovascular system, to improve renal function, and to improve glucose tolerance and insulin-sensitivity. The present invention is also directed to a pharmaceutical composition comprising the mAPP inhibitor of the present invention and a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, preferably human, in need of treatment comprising administering to the patient a therapeutically effective amount of an α thio-containing compound of the present invention. The method of the present invention also contemplates the further step of administering to the mammalian patient in need of treatment a therapeutically effective amount of an inhibitor of angiotensin converting enzyme (ACE).

  本发明涉及一种含有α硫基的化合物，能够抑制酶、膜氨肽酶P（mAPP或APP），其天然底物为缓激肽。该化合物作为一种药物剂，具有用途，因为通过抑制缓激肽的降解，该化合物使缓激肽能够在心血管系统中发挥其有益作用，改善肾功能，改善葡萄糖耐受性和胰岛素敏感性。本发明还涉及一种含有本发明的mAPP抑制剂和药用载体的药物组合物。在另一个方面，本发明涉及一种方法，在需要治疗的哺乳动物患者中，特别是人类，抑制缓激肽的降解，包括向患者施用本发明的α硫基化合物的治疗有效量。本发明的方法还考虑了向需要治疗的哺乳动物患者施用血管紧张素转换酶（ACE）抑制剂的治疗有效量的进一步步骤。
• AMINO ACID DERIVATIVE
  申请人：Eisai Co., Ltd.

  公开号：EP0671172A1

  公开（公告）日：1995-09-13

  An amino acid derivative having an angiotensin I-converting enzyme inhibitor activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibitor activity, and represented by general formula (I) wherein R¹ represents hydrogen or acyl; R² represents hydrogen, lower alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; m and n represent each independently an integer of 0.1 or 2; and J represents a cyclic group having an angiotensin I-converting enzyme inhibitor activity.

  一种具有血管紧张素Ⅰ转换酶抑制剂活性、血管加压素拮抗剂活性和心房钠尿肽水解酶抑制剂活性的氨基酸衍生物，由通式(I)表示 其中R¹代表氢或酰基；R²代表氢、低级烷基、环烷基、任选取代的芳基、任选取代的杂芳基、任选取代的芳烷基或任选取代的杂芳基烷基；m和n各自独立地代表0.1或2的整数；J代表具有血管紧张素I-转化酶抑制剂活性的环状基团。