4-[[6-[(2-fluoro-4 methylsulfonylphenyl)amino]pyrimidin-4-yl]oxy]piperidine-1-carboxylic acid isopropyl ester

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-[[6-[(2-fluoro-4 methylsulfonylphenyl)amino]pyrimidin-4-yl]oxy]piperidine-1-carboxylic acid isopropyl ester
• 英文别名: 4-[6-(2-fluoro-4-methanesulfonyl-phenylamino)-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester；propan-2-yl 4-[6-(2-fluoro-4-methylsulfonylanilino)pyrimidin-4-yl]oxypiperidine-1-carboxylate
• 化学式: C₂₀H₂₅FN₄O₅S
• 分子量: 452.507
• InChiKey: PSTAUCWYFNORSZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  119
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  (2-fluoro-4-methanesulfonyl-phenyl)-[6-(piperidin-4-yloxy)-pyrimidin-4-yl]-amine 、 氯甲酸异丙酯 在 三乙胺 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 1.0h， 以81%的产率得到4-[[6-[(2-fluoro-4 methylsulfonylphenyl)amino]pyrimidin-4-yl]oxy]piperidine-1-carboxylic acid isopropyl ester
  参考文献：
  名称：

  [EN] SUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO
  [FR] DERIVES D'ARYLE ET D'HETEROARYLE SUBSTITUES TENANT LIEU DE MODULATEURS DU METABOLISME ET PREVENTION ET TRAITEMENT DE TROUBLES ASSOCIES

  摘要：

  公开号：

  WO2005121121A3

文献信息

• [EN] L- ( PIPERIDIN-4-YL) -PYRAZOLE DERIVATIVES AS GPR 119 MODULATORS<br/>[FR] DERIVES DE L-(PIPERIDIN-4-YL)-PYRAZOLE UTILISES EN TANT QUE MODULATEURS DU GPR 119
  申请人：PFIZER

  公开号：WO2010140092A1

  公开（公告）日：2010-12-09

  Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

  本文描述了化合物I的化合物，其调节G蛋白偶联受体GPR119的活性，并且它们在治疗与动物中G蛋白偶联受体GPR119调节相关的疾病中的用途。
• [EN] 4- (5-CYANO-PYRAZOL-1-YL) -PIPERIDINE DERIVATIVES AS GPR 119 MODULATORS<br/>[FR] DÉRIVÉS DE 4-(5-CYANOPYRAZOL-1-YL)PIPÉRIDINE EN TANT QUE MODULATEURS DU GPR119
  申请人：PFIZER

  公开号：WO2012069948A1

  公开（公告）日：2012-05-31

  Compounds that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein- coupled receptor GPR119 in animals are described herein.

  本文描述了调节G蛋白偶联受体GPR119活性的化合物及其在治疗与动物中G蛋白偶联受体GPR119调节相关疾病中的用途。
• [EN] IMIDAZO-PYRAZOLES AS GPR119 INHIBITORS<br/>[FR] IMIDAZO-PYRAZOLES COMME INHIBITEURS DU GPR119
  申请人：PFIZER

  公开号：WO2011061679A1

  公开（公告）日：2011-05-26

  Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is -C(O)-O-R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano, nitro, C1-C6 fluoroalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluoroalkoxy, or C3-C6 cycloalkyl; R6 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, -C(O)-NH2, or C1-C6 alkyl substituted with hydroxy or C1- C6 alkoxy; m is 1 or 2, wherein when m is 1 then R8 is hydrogen, C1-C6 alkyl, -CH2-(C1- C5)haloalkyl, C3-C6 cycloalkyl, or C1-C6 alkyl substituted with hydroxy; and when m is 2 then each R8 is independently C1-C3 alkyl or -CH2-(C1-C2)haloalkyl; modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G- protein-coupled receptor GPR119 in animals are described herein.

  式(I)的化合物中：X为(A)或(B)；Y为O或键；R1为-C(O)-O-R3或R2为氢、氰基、C1-C6烷基或C3-C6环烷基；R5为氢、氰基、硝基、C1-C6氟代烷基、C1-C6烷基、C1-C6烷氧基、C1-C6氟代烷氧基或C3-C6环烷基；R6为氢、C1-C6烷基、C3-C6环烷基、-C(O)-NH2或C1-C6烷基取代的羟基或C1-C6烷氧基；m为1或2，当m为1时，则R8为氢、C1-C6烷基、-CH2-(C1-C5)卤代烷基、C3-C6环烷基或C1-C6烷基取代的羟基；当m为2时，则每个R8独立地为C1-C3烷基或-CH2-(C1-C2)卤代烷基；调节G蛋白偶联受体GPR119的活性及其在治疗与动物体内G蛋白偶联受体GPR119调节相关疾病中的用途。
• [EN] GPR 119 MODULATORS<br/>[FR] MODULATEURS DE GPR 119
  申请人：PFIZER

  公开号：WO2011036576A1

  公开（公告）日：2011-03-31

  Compounds of formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.

  本文描述了式(I)的化合物，该化合物可以调节G蛋白偶联受体GPR119的活性，并用于治疗与动物中G蛋白偶联受体GPR119调节相关的疾病。
• Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
  申请人：Jones Robert M.

  公开号：US20090036434A1

  公开（公告）日：2009-02-05

  The present invention relates to certain substituted aryl and heteroaryl derivative of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及公式（I）的某些取代芳基和杂环芳基衍生物，它们是代谢调节剂。因此，本发明的化合物在代谢相关疾病和并发症的治疗中是有用的，如糖尿病和肥胖症。