Org 24598

• 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: Org 24598
• 英文别名: N-methyl-N-[(3R)-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propyl]glycine；2-[methyl-[(3R)-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propyl]amino]acetic acid
• 化学式: C₁₉H₂₀F₃NO₃
• 分子量: 367.368
• InChiKey: KZWQAWBTWNPFPW-QGZVFWFLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  49.8
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  Org 24598 在 N-溴代丁二酰亚胺(NBS) 、 溶剂黄146 、 三氟乙酸 作用下， 以93 %的产率得到(R)-N-(3-(2-bromo-4-(trifluoromethyl)phenoxy)-3-phenylpropyl)-N-methylglycine
  参考文献：
  名称：

  Synthesis of [³H]Org24598 using in‐house prepared [³H]MeI

  摘要：

  报告了氚标记的甘氨酸转运体 1 抑制剂 Org24598 的合成过程。由于 Org24598 骨架在氢化条件下不稳定，因此采用了一种使用内部制备的氚标记烷基化剂（[3H]MeI，SA = 26.2 Ci/mmol）的合成方法。本文还讨论了其他标记方法。

  DOI：

  10.1002/jlcr.4084

文献信息

• METHOD OF TREATING SCHIZOPHRENIA PRODROME
  申请人：Yale University

  公开号：EP1871165B1

  公开（公告）日：2017-06-21
• PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING DRUG ADDICTION AND PREVENTING A DRUG RELAPSE
  申请人：Arizona Board of Regents, for and on behalf of, Arizona State University

  公开号：US20150141462A1

  公开（公告）日：2015-05-21

  The present invention relates to pharmaceutical compositions comprising (a) a pharmaceutically effective amount of an mGluR5 positive allosteric modulator, derivative, prodrug or a pharmaceutically acceptable salt thereof; (b) a pharmaceutically effective amount of an agent selected from an NMDA partial agonist or a GlyT1 inhibitor, derivative, prodrug or a pharmaceutically acceptable salt thereof; and (c) a pharmaceutically acceptable carrier. The present invention also relates to methods for treating drug addiction and preventing a drug relapse in a patient. The methods comprise (a) administering to the patient a pharmaceutically effective amount of an mGluR5 positive allosteric modulator, derivative, prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof; (b) administering to the patient a pharmaceutically effective amount of an agent selected from an NMDA partial agonist or a GlyT1 inhibitor, derivative, prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof.
• METHODS OF TREATING ERYTHROPOIETIC PROTOPORPHYRIA, X-LINKED PROTOPORPHYRIA, OR CONGENITAL ERYTHROPOIETIC PORPHYRIA WITH GLYCINE TRANSPORT INHIBITORS
  申请人：Disc Medicine, Inc.

  公开号：US20210283129A1

  公开（公告）日：2021-09-16

  The present embodiments are directed to methods of using glycine transporter inhibitors, such as GlyT1 inhibitors, or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions thereof, for preventing or treating erythropoietic protoporphyria (EPP), X-linked protoporphyria (XLPP), and/or congenital erythropoietic porphyria (CEP), and related syndromes thereof.
• US8492418B2
  申请人：——

  公开号：US8492418B2

  公开（公告）日：2013-07-23
• [EN] PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING DRUG ADDICTION AND PREVENTING A DRUG RELAPSE<br/>[FR] COMPOSITIONS PHARMACEUTIQUES ET MÉTHODES DE TRAITEMENT D'UNE PHARMACODÉPENDANCE ET DE PRÉVENTION À UNE RECHUTE MÉDICAMENTEUSE
  申请人：UNIV ARIZONA

  公开号：WO2013188465A2

  公开（公告）日：2013-12-19

  The present invention relates to pharmaceutical compositions comprising (a) a pharmaceutically effective amount of an mGluR5 positive allosteric modulator, derivative, prodrug or a pharmaceutically acceptable salt thereof; (b) a pharmaceutically effective amount of an agent selected from an NMDA partial agonist or a GlyT1 inhibitor, derivative, prodrug or a pharmaceutically acceptable salt thereof; and (c) a pharmaceutically acceptable carrier. The present invention also relates to methods for treating drug addiction and preventing a drug relapse in a patient. The methods comprise (a) administering to the patient a pharmaceutically effective amount of an mGluR5 positive allosteric modulator, derivative, prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof; (b) administering to the patient a pharmaceutically effective amount of an agent selected from an NMDA partial agonist or a GlyT1 inhibitor, derivative, prodrug or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof.