4-(difluoromethyl)cyclohexan-1-amine | 1314939-44-0

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 4-(difluoromethyl)cyclohexan-1-amine
• CAS: 1314939-44-0
• 化学式: C₇H₁₃F₂N
• 分子量: 149.184
• InChiKey: FHINUUZVNPBBSO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  26
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  tert-butyl 4-(((4-nitrophenoxy)carbonyl)amino)piperidine-1-carboxylate 、 4-(difluoromethyl)cyclohexan-1-amine 以 四氢呋喃 为溶剂， 反应 12.0h， 生成 C₁₈H₃₁F₂N₃O₃
  参考文献：
  名称：

  1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia

  摘要：

  1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea 14a (AR9281), a potent and selective soluble epoxide hydrolase inhibitor, was recently tested in a phase 2a clinical setting for its effectiveness in reducing blood pressure and improving insulin resistance in pre-diabetic patients. In a mouse model of diet induced obesity, AR9281 attenuated the enhanced glucose excursion following an intraperitoneal glucose tolerance test. AR9281 also attenuated the increase in blood pressure in angiotensin-II-induced hypertension in rats. These effects were dose-dependent and well correlated with inhibition of the sEH activity in whole blood, consistent with a role of sEH in the observed pharmacology in rodents. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.12.042

文献信息

• [EN] ΡΡΑRγ MODULATORS AND METHODS OF USE<br/>[FR] MODULATEURS DE ΡΡΑRγ ET MÉTHODES D'UTILISATION
  申请人：EISAI R&D MANGEMENT CO LTD

  公开号：WO2022099144A1

  公开（公告）日：2022-05-12

  Disclosed herein are novel PPARy modulators of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the same, and methods of using the same, in particular for the treatment of cancers.

  本文公开了一种新型的PPARy调节剂，其化学式为（I），以及其药学上可接受的盐，包含它们的制药组合物，以及使用它们的方法，特别是用于治疗癌症的方法。
• QUINOLINE-3-CARBOXAMIDES AS H-PGDS INHIBITORS
  申请人：Astex Therapeutics Limited

  公开号：EP3390384B1

  公开（公告）日：2021-09-15
• PROLINE AMIDE COMPOUNDS AND THEIR AZETIDINE ANALOGUES CARRYING A SPECIFICALLY SUBSTITUTED BENZYL RADICAL
  申请人：AbbVie Deutschland GmbH & Co. KG

  公开号：US20200039930A1

  公开（公告）日：2020-02-06

  The present invention relates to proline amide compounds and their azetidine derivatives of formula I wherein the variables are as defined in the claims and the description. The invention further relates to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT 2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT 2C receptor, to a method for preventing or treating conditions and disorders which respond to the modulation of the 5-HT 2C receptor, and processes for preparing such compounds and compositions.
• [EN] QUINOLINE-3-CARBOXAMIDES AS H-PGDS INHIBITORS<br/>[FR] QUINOLÉINE-3-CARBOXAMIDES UTILISÉS COMME INHIBITEURS DE H-PGDS
  申请人：ASTEX THERAPEUTICS LTD

  公开号：WO2017103851A1

  公开（公告）日：2017-06-22

  The present invention relates to compounds of Formula (XI) wherein R1a, R2a, R3a, R4a, R5a, R6a, and Aa are as defined herein, and pharmaceutically acceptable salts thereof. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) inhibitors and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
• 1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia
  作者：Sampath-Kumar Anandan、Heather Kay Webb、Dawn Chen、Yi-Xin (Jim) Wang、Basker R. Aavula、Sylvaine Cases、Ying Cheng、Zung N. Do、Upasana Mehra、Vinh Tran、Jon Vincelette、Joanna Waszczuk、Kathy White、Kenneth R. Wong、Le-Ning Zhang、Paul D. Jones、Bruce D. Hammock、Dinesh V. Patel、Randall Whitcomb、D. Euan MacIntyre、James Sabry、Richard Gless

  DOI：10.1016/j.bmcl.2010.12.042

  日期：2011.2

  1-(1-Acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea 14a (AR9281), a potent and selective soluble epoxide hydrolase inhibitor, was recently tested in a phase 2a clinical setting for its effectiveness in reducing blood pressure and improving insulin resistance in pre-diabetic patients. In a mouse model of diet induced obesity, AR9281 attenuated the enhanced glucose excursion following an intraperitoneal glucose tolerance test. AR9281 also attenuated the increase in blood pressure in angiotensin-II-induced hypertension in rats. These effects were dose-dependent and well correlated with inhibition of the sEH activity in whole blood, consistent with a role of sEH in the observed pharmacology in rodents. (C) 2010 Elsevier Ltd. All rights reserved.