2-[[phenylhydroxyphosphinyl]methyl]pentanedioic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-[[phenylhydroxyphosphinyl]methyl]pentanedioic acid
• 英文别名: 2-{[hydroxy(phenyl)phosphoryl]methyl}pentanedioic acid；[(phenylhydroxyphosphinyl)-methyl]pentanedioic acid；2-[(phenylhydroxyphosphinyl)methyl]pentanedioic acid；2-(Hydroxy-phenyl-phosphinoylmethyl)-pentanedioic acid；2-[[hydroxy(phenyl)phosphoryl]methyl]pentanedioic acid
• 化学式: C₁₂H₁₅O₆P
• 分子量: 286.221
• InChiKey: UIVPEQQNMNDWDC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  19
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  112
• 氢给体数：
  3
• 氢受体数：
  6

上下游信息

• 上游原料

  中文名称	英文名称	CAS号	化学式	分子量
  ——	Dibenzyl 2-[[phenyl(phenylmethoxy)phosphoryl]methyl]pentanedioate	1027325-04-7	C33H33O6P	556.595

反应信息

• 作为产物：
  描述：

  苯膦酸 在 5percent Pd/C 氢气 、 sodium hydride 、 N,N'-二环己基碳二亚胺 作用下， 以 四氢呋喃 、 乙醇 、 二氯甲烷 为溶剂， 20.0 ℃ 、344.75 kPa 条件下， 反应 36.0h， 生成 2-[[phenylhydroxyphosphinyl]methyl]pentanedioic acid
  参考文献：
  名称：

  Design and Pharmacological Activity of Phosphinic Acid Based NAALADase Inhibitors

  摘要：

  A novel series of phosphinic acid based inhibitors of the neuropeptidase NAALADase are described in this work. This series of compounds is the most potent series of inhibitors of the enzyme described to date. In addition, we have shown that these compounds are protective in animal models of neurodegeneration. Compound 34 significantly prevented neurodegeneration in a middle cerebral artery occlusion model of cerebral ischemia. In addition, in the chronic constrictive mc del of neuropathic pain, compound 34 significantly attenuated the hypersensitivity observed with saline-treated animals. These data suggest that NAALADase inhibition may provide a new approach for the treatment of both neurodegenerative disorders and peripheral neuropathies.

  DOI：

  10.1021/jm0001774

文献信息

• PSMA BINDING LIGAND-LINKER CONJUGATES AND METHODS FOR USING
  申请人：Purdue Research Foundation

  公开号：US20160067341A1

  公开（公告）日：2016-03-10

  Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

  本文描述了用于传递治疗、诊断和成像剂的前列腺特异性膜抗原（PSMA）结合共轭物。本文还描述了含有它们的药物组合物以及使用这些共轭物和组合物的方法。还描述了用于制造这些共轭物和含有它们的组合物的过程。
• Naaladase inhibitors for treating retinal disorders and glaucoma
  申请人：——

  公开号：US20030036534A1

  公开（公告）日：2003-02-20

  The present invention relates to pharmaceutical compositions and methods for treating a retinal disorder or glaucoma using NAALADase inhibitors.

  本发明涉及使用NAALADase抑制剂治疗视网膜疾病或青光眼的药物组合物和方法。
• Naaladase inhibitors for treating amyotrophic lateral sclerosis
  申请人：——

  公开号：US20020013295A1

  公开（公告）日：2002-01-31

  The present invention relates to pharmaceutical compositions and methods for treating amyotrophic lateral sclerosis using NAALADase inhibitors.

  该发明涉及使用NAALADase抑制剂治疗肌萎缩侧索硬化症的药物组合物和方法。
• [EN] CANCER IMAGING AGENT<br/>[FR] AGENT D'IMAGERIE DU CANCER
  申请人：ENDOCYTE INC

  公开号：WO2016112293A1

  公开（公告）日：2016-07-14

  The present disclosure relates to imaging agent formulations, methods for preparing imaging agent formulations and methods for using the same. The present disclosure also relates to kits for imaging agent formulations.

  本公开涉及成像剂配方、制备成像剂配方的方法以及使用它们的方法。本公开还涉及成像剂配方的套件。
• [EN] PSMA BINDING LIGAND-LINKER CONJUGATES AND METHODS FOR USING<br/>[FR] CONJUGUÉS LIGAND-LIEUR DE LIAISON AU PSMA ET PROCÉDÉS POUR UTILISER CEUX-CI
  申请人：PURDUE RESEARCH FOUNDATION

  公开号：WO2009026177A1

  公开（公告）日：2009-02-26

  Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

  本文描述了前列腺特异性膜抗原（PSMA）结合的联合物，可以用于输送治疗、诊断和成像剂。还描述了包含它们的制药组合物以及使用这些联合物和组合物的方法。还描述了制造这些联合物和包含它们的组合物的过程。