(1R,3R,5S)-8-(methylsulfonyl)-8-azabicyclo[3.2.1]octan-3-ol | 1361392-00-8

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 托烷生物碱
• 英文名称: (1R,3R,5S)-8-(methylsulfonyl)-8-azabicyclo[3.2.1]octan-3-ol
• 英文别名: (1R,3s,5S)-8-(methylsulfonyl)-8-azabicyclo[3.2.1]octan-3-ol
• CAS: 1361392-00-8
• 化学式: C₈H₁₅NO₃S
• 分子量: 205.278
• InChiKey: PFNINWFAYARTTF-RNLVFQAGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.07
• 重原子数：
  13.0
• 可旋转键数：
  1.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  57.61
• 氢给体数：
  1.0
• 氢受体数：
  3.0

文献信息

• CYCLOHEXANE ANALOGUES AS GPR119 AGONISTS
  申请人：Kang Sang Uk

  公开号：US20120053180A1

  公开（公告）日：2012-03-01

  This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.

  这项发明涉及一系列含有替代基的环己烷类似物，这些类似物是 GPR119 激动剂，旨在治疗由 GPR119 介导的代谢性疾病，包括I型和II型糖尿病。糖尿病是对人类健康构成日益增加的威胁，导致各种并发症（失明、肾衰竭、神经病变、心脏病发作、中风等）。最近发现，激活在胰岛素β细胞中高表达的 GPR119 会导致葡萄糖依赖性胰岛素分泌和 GLP-1 释放。许多制药公司目前正在开发 GPR119 激动剂，我们在此披露了替代的 GPR119 激动剂。我们的发明描述了具有结构式（I）的 GPR119 激动剂，结构式（I）的药学上可接受的盐或溶剂，结构式（I）的异构体或前药，以及结构式（I）与其他抗糖尿病药物（如 DPP-IV 抑制剂和/或胰岛素增敏剂）的联合治疗。
• [EN] PYRIDONE-SULFONE MORPHINAN ANALOGS AS OPIOID RECEPTOR LIGANDS<br/>[FR] ANALOGUES DE MORPHINANE PYRIDONE-SULFONES UTILISÉS COMME LIGANDS DE RÉCEPTEURS OPIOÏDES
  申请人：PURDUE PHARMA LP

  公开号：WO2015102682A1

  公开（公告）日：2015-07-09

  The application is directed to Pyridone-sulfone morphinan analogs compounds of Formula I: or pharmaceutically acceptable salts and solvates thereof, wherein ==, R1, R2, R3, R4 and Z are as defined as set forth in the specification. The invention is also directed to use of the compounds of Formula I or the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the odulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

  该应用程序针对Formula I的吡啶酮-砜吗啡类似物化合物，或其药学上可接受的盐和溶剂，其中==，R1，R2，R3，R4和Z的定义如规范所述。该发明还涉及使用Formula I的化合物或其药学上可接受的盐和溶剂来治疗对一种或多种阿片受体调节敏感的紊乱，或作为合成中间体。本发明的某些化合物特别适用于治疗疼痛。
• PYRIDONE-SULFONE MORPHINAN ANALOGS AS OPIOID RECEPTOR LIGANDS
  申请人：PURDUE PHARMA L.P.

  公开号：US20160318932A1

  公开（公告）日：2016-11-03

  The application is directed to Pyridone-sulfone morphinan analogs compounds of Formula I: or pharmaceutically acceptable salts and solvates thereof, wherein ==, R1, R2, R3, R4 and Z are as defined as set forth in the specification. The invention is also directed to use of the compounds of Formula I or the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the odulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.