N-(4-hydroxyphenyl)eicosa-5,8,11,14-tetraenamide

• 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: N-(4-hydroxyphenyl)eicosa-5,8,11,14-tetraenamide
• 英文别名: N-(4-hydroxyphenyl)icosa-5,8,11,14-tetraenamide
• 化学式: C₂₆H₃₇NO₂
• 分子量: 395.6
• InChiKey: IJBZOOZRAXHERC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.2
• 重原子数：
  29
• 可旋转键数：
  15
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• Inhibitor of endocannabinoid cellular reuptake
  申请人：University of Bern

  公开号：US10414721B1

  公开（公告）日：2019-09-17

  Provided is a highly potent and selective endocannabioid cellular reuptake inhibitor represented by formula (I): or a pharmaceutically acceptable solvate or co-crystal thereof as well as to a formulation comprising this inhibitor, and to methods of treatment in which this inhibitor is used.

  提供了一种高效且选择性的内源大麻素细胞摄取抑制剂，其化学式表示为（I）：或其药学上可接受的溶剂或共晶体，以及包含该抑制剂的配方，以及使用该抑制剂的治疗方法。
• [EN] AMINES THAT INHIBIT A MAMMALIAN ANANDAMIDE TRANSPORTER, AND METHODS OF USE THEREOF<br/>[FR] AMINES INHIBANT UN TRANSPORTEUR D'ANANDAMIDE DE TYPE MAMMALIEN, ET PROCEDES D'UTILISATION
  申请人：SEPRACOR INC

  公开号：WO2003097573A1

  公开（公告）日：2003-11-27

  One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson’s disease, spasticity. Tourette’s syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton’s headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn’s disease, malignant gliomas, neurodegenerative diseases, Huntington’s chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.

  本发明的一个方面涉及胺类化合物。本发明的另一个方面涉及将这些胺类化合物用作哺乳动物阿南胺酸转运体的抑制剂。本发明的化合物还可用于治疗许多困扰哺乳动物的疾病、病症和疾病，包括但不限于哮喘、神经病性疼痛、持续性疼痛、炎症性疼痛、多动症、高血压、脑缺血、帕金森病、痉挛、托瑞特综合症、精神分裂症、出血性休克、脓毒性休克、心脏休克、偏头痛、霍顿头痛、多发性硬化症、厌食症、艾滋病 wasting 综合症、器官排斥、自身免疫疾病、过敏、关节炎、克罗恩病、恶性胶质瘤、神经退行性疾病、亨廷顿舞蹈病、青光眼、恶心、焦虑、精神病、注意力缺陷多动障碍、早泄和中风。本发明的另一个方面涉及胺类的组合库以及制备这些库的方法。
• Modulation of anxiety through blockade of anandamide hydrolysis
  申请人：The Regents of the University of California

  公开号：US20040127518A1

  公开（公告）日：2004-07-01

  Fatty acid amide hydrolase inhibitors of the Formula: 1 are provided wherein X is NH, CH 2 , O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R 1 and R 2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R 1 and R 2 is absent, and that if Z is N, optionally R 1 and R 2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

  本发明提供了公式1中X为NH，CH2，O或S；Q为O或S；Z为O或N；R为从取代或未取代芳基；取代或未取代联苯基；取代或未取代萘基；取代或未取代苯基；取代或未取代三苯基基；取代或未取代环烷基，杂环芳基或烷基中选择的芳香基；R1和R2分别独立地选择从H，取代或未取代烷基，取代或未取代杂环烷基和取代或未取代苯基，取代或未取代联苯基，取代或未取代芳基和取代或未取代杂环芳基的群中选择；但是如果Z为O，则R1和R2中的一个不存在，如果Z为N，则R1和R2可以选择性地一起形成取代或未取代的N-杂环或取代或未取代的杂环芳基，与它们各自连接的N原子。本发明还提供了包括公式I中化合物的制药组合物以及使用它们来抑制FAAH和/或治疗食欲障碍，青光眼，疼痛，失眠和神经心理障碍，包括焦虑症，癫痫和抑郁症的方法。
• Amines that inhibit a mammalian anandamide transporter, and methods of use thereof
  申请人：——

  公开号：US20040048907A1

  公开（公告）日：2004-03-11

  One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.

  本发明的一个方面涉及胺。本发明的第二个方面涉及使用这些胺作为哺乳动物阿那达胺转运体的抑制剂。本发明的化合物还将在治疗许多影响哺乳动物的疾病、病症和疾病方面发挥作用，包括但不限于哮喘、神经病理性疼痛、持续性疼痛、炎症性疼痛、多动症、高血压、脑缺血、帕金森病、痉挛、杜雷特综合症、精神分裂症、出血性休克、脓毒性休克、心源性休克、偏头痛、霍顿头痛、多发性硬化症、厌食症、艾滋病消耗综合症、器官排斥、自身免疫性疾病、过敏、关节炎、克罗恩病、恶性胶质瘤、神经退行性疾病、亨廷顿舞蹈症、青光眼、恶心、焦虑、精神病、注意力缺陷多动障碍、早泄和中风等方面发挥作用。本发明的另一个方面涉及胺的组合式库，以及制备库的方法。
• MODULATION OF ANXIETY THROUGH BLOCKADE OF ANANDAMIDE HYDROLYSIS
  申请人：Piomelli Daniele

  公开号：US20120010283A1

  公开（公告）日：2012-01-12

  Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH 2 , O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R 1 and R 2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R 1 and R 2 is absent, and that if Z is N, optionally R 1 and R 2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

  提供了公式为的脂肪酸酰胺水解酶抑制剂：其中X为NH，CH2，O或S；Q为O或S；Z为O或N；R为从取代或未取代芳基；取代或未取代联苯基；取代或未取代萘基；取代或未取代苯基；取代或未取代三苯基基；取代或未取代环烷基，杂环芳基或烷基中选择的芳香基；R1和R2分别选择自H，取代或未取代烷基，取代或未取代杂环烷基，取代或未取代苯基，取代或未取代联苯基，取代或未取代芳基和取代或未取代杂环芳基的群中；但是如果Z为O，则R1和R2中的一个不存在，如果Z为N，则可选地将R1和R2结合在一起形成取代或未取代的N-杂环或取代或未取代的杂环芳基，与它们各自连接的N原子。提供了包含公式I化合物的制药组合物以及使用它们来抑制FAAH和/或治疗食欲障碍，青光眼，疼痛，失眠以及神经和心理障碍，包括焦虑症，癫痫和抑郁症的方法。