5-(4-hydroxy-phenyl)-5-oxo-valeric acid | 4648-94-6

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物
• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 5-(4-hydroxy-phenyl)-5-oxo-valeric acid
• 英文别名: 5-(4-Hydroxy-phenyl)-5-oxo-valeriansaeure；4-<4-Hydroxy-benzoyl>-buttersaeure；4-(p-Hydroxybenzoyl)-buttersaeure；5-(4-hydroxyphenyl)-5-oxopentanoic acid
• CAS: 4648-94-6
• 化学式: C₁₁H₁₂O₄
• 分子量: 208.214
• InChiKey: AGQBCNFDMDWFML-UHFFFAOYSA-N

物化性质

• 熔点：
  202-203 °C
• 沸点：
  461.7±25.0 °C(Predicted)
• 密度：
  1.273±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  74.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-(4-hydroxy-phenyl)-5-oxo-valeric acid 在 盐酸 、 amalgamated zinc 作用下， 生成 5-(4-羟基苯基)戊酸
  参考文献：
  名称：

  Treibs; Falk, Chemische Berichte, 1954, vol. 87, p. 345,348

  摘要：

  DOI：
• 作为产物：
  描述：

  5-(4-甲氧基苯基)-5-氧代戊酸 在 氢溴酸 、 溶剂黄146 作用下， 反应 20.0h， 生成 5-(4-hydroxy-phenyl)-5-oxo-valeric acid
  参考文献：
  名称：

  (Phenylmethoxy)phenyl derivatives of w-oxo- and w-tetrazolylalkanoic acids and related tetrazoles. Synthesis and evaluation as leukotriene D4 receptor antagonists

  摘要：

  Two series of (phenylmethoxy)phenyl compounds derived from the structure of LY163443 were synthesized and evaluated as leukotriene D4 receptor antagonists. In the OMEGA-[(phenylmethoxy)phenyl]-OMEGA-oxoalkanoic acid series, 5-[4-[(4-acetyl-2-ethyl-3-hydroxyphenyl)methoxy]phenyl]-3,3-dimethyl-5-oxopentanoic acid (8) was the most potent antagonist of LTD4-induced contractions of guinea pig ileum (pK(B) of 7.60) and LTD4 pressor response in pithed rats (ED50 of 1.4 mg/kg iv). Replacing the carboxylic acid function with 5-tetrazole gave slightly more potent compounds. In the OMEGA-[5-[[(phenylmethoxy)phenyl]alkyl]tetrazolyl]alkanoic acid series, replacing the carboxylic acid with 5-tetrazole gave compounds that were equally effective in the guinea pig ileum but more potent in vivo against the LTD4 pressor response in rat. The pK(B) value in the guinea pig ileum for 1-[2-hydroxy-3-propyl-4-[[4-[[2-[3-(1H-tetrazol-5-yl)propyl]-2H-tetrazol-5-yl]methyl]phenoxy]methyl]phenyl]ethanone (25) was 7.87 and the ED50 for antagonism of the LTD4 pressor response was 4.0 mg/kg iv. The sodium salts of 8 (9) and 25 (26) given by the iv route of administration antagonized LTD4-induced cardiovascular alterations in anesthetized rat and LTD4-induced bronchoconstriction in guinea pig in a dose-dependent manner. Oral activity was also demonstrated against the LTD4-induced bronchoconstriction in guinea pig.

  DOI：

  10.1021/jm00113a014

文献信息

• PEGylated recombinant human growth hormone compounds
  申请人：Ascendis Pharma Endocrinology Division A/S

  公开号：US10960053B2

  公开（公告）日：2021-03-30

  A chemically modified human Growth Hormone (rhGH) prepared by attaching a transient linker which comprises a polyethylene glycol. The chemically modified protein may have a much longer lasting rhGH activity than that of the unmodified rhGH, enabling reduced dose and scheduling opportunities and the modified rhGH may not cause lipoatrophy. Also includes methods of use for the treatment and/or prevention of diseases or disorders in which use of growth hormone is beneficial.

  一种化学修饰的人类生长激素（rhGH），通过连接由聚乙二醇组成的瞬时连接体制备而成。与未修饰的 rhGH 相比，经化学修饰的蛋白质可能具有更持久的 rhGH 活性，从而可以减少剂量和使用时间，而且经修饰的 rhGH 可能不会引起脂肪萎缩。还包括用于治疗和/或预防使用生长激素有益的疾病或失调的方法。
• Treibs; Falk, Chemische Berichte, 1954, vol. 87, p. 345,348
  作者：Treibs、Falk

  DOI：——

  日期：——
• AZOLE ACID DERIVATIVES, ALONE OR IN COMBINATION, FOR TREATING DIABETES AND DYSLIPIDEMIAS; AND FOR TREATING MALIGNANT DISEASES
  申请人：Bristol-Myers Squibb Company

  公开号：EP1401433B1

  公开（公告）日：2010-11-10
• PEGYLATED RECOMBINANT HUMAN GROWTH HORMONE COMPOUNDS
  申请人：Ascendis Pharma Growth Disorders Division A/S

  公开号：EP2279007B1

  公开（公告）日：2016-05-18
• Interferon Alpha Carrier Prodrugs
  申请人：Rau Harald

  公开号：US20120058084A1

  公开（公告）日：2012-03-08

  The present invention relates to a pharmaceutical composition comprising a water-soluble polymeric carrier linked prodrug of interferon alpha, wherein the prodrug is capable of releasing free interferon alpha, wherein the release half life under physiological conditions is at least 4 days. The invention further relates to prodrugs for said pharmaceutical composition and their use for treating, controlling, delaying or preventing a condition that can benefit from interferon alpha treatment, such as hepatitis C.