GT 2016

• 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: GT 2016
• 英文别名: 4-[N-(5-cyclohexylpentan-1-one-1-yl)piperidin-4-yl]imidazole；4-(1-CYCLOHEXYLVALEROYL-4-PIPERIDYL) 1H-IMIDAZOLE；GT-2016；1-(4-(1H-Imidazol-5-yl)piperidin-1-yl)-5-cyclohexylpentan-1-one；5-cyclohexyl-1-[4-(1H-imidazol-5-yl)piperidin-1-yl]pentan-1-one
• 化学式: C₁₉H₃₁N₃O
• 分子量: 317.475
• InChiKey: YTCGNPGLMAECND-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.79
• 拓扑面积：
  49
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  5-cyclohexylpentanoyl chloride 、 二环己胺 、 4-(1H-咪唑-4-基)哌啶 以 二氯甲烷 、 乙腈 为溶剂， 生成 GT 2016
  参考文献：
  名称：

  4-[4'-piperodinyl or 3'-pirrolidinyl] substituted imidazoles as H.sub.3

  摘要：

  具有组织胺H3受体拮抗活性的噻唑基化合物，以及用于治疗认知障碍或注意力或唤醒缺陷的药物组合物和使用这些化合物的方法。

  公开号：

  US05639775A1

文献信息

• [EN] C20-C21 SUBSTITUTED GLUCOCORTICOID RECEPTOR AGONISTS<br/>[FR] AGONISTES DU RÉCEPTEUR DE GLUCOCORTICOÏDE SUBSTITUÉS EN C20-C21
  申请人：SCHERING CORP

  公开号：WO2009085879A2

  公开（公告）日：2009-07-09

  The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having general structure (I); wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and Vl, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.

  本发明提供了具有一般结构（I）的化合物，以及该化合物的药用盐、溶剂合物、酯、前药、互变体或异构体（包括L、R1、R2、R3、R4、R5和R6在内独立选择的定义）。本发明还提供了根据本文所定义的化合物（和盐、溶剂合物、酯、前药、互变体和异构体）的II、III、IV、V和VI式化合物。还提供了药物组合物、制备方法以及利用这些化合物在治疗和预防各种免疫、自身免疫和炎症性疾病和症状中的方法。
• Histamine H.sub.3 -receptor antagonists and therapeutic uses thereof
  申请人：The University of Toledo

  公开号：US05486526A1

  公开（公告）日：1996-01-23

  The present invention is directed to compounds of the class of piperidyl-imidazole derivative histamine H.sub.3 -receptor antagonists. Such compounds have affinity for histamine H.sub.3 -receptor, and preferably penetrate the blood-brain barrier. The compounds can block the soporific effect of an H.sub.3 -receptor agonist. Illustrative of the compounds of the invention is the molecule 4-(1-cyclohexylvaleroyl-4-piperidyl)-1H-imidazole. These compounds have been found to have utility in treating cognitive disorders and have been found to be useful as appetite suppressants.

  本发明涉及一类哌啶基-咪唑衍生物组合物，其为组胺H.sub.3受体拮抗剂。这些化合物具有与组胺H.sub.3受体的亲和力，并且优选可穿透血脑屏障。这些化合物可以阻断H.sub.3受体激动剂的催眠效应。本发明的化合物的例子是4-(1-环己基戊酰基-4-哌啶基)-1H-咪唑。这些化合物已被发现在治疗认知障碍方面具有用途，并且被发现可作为食欲抑制剂。
• SUBSTITUTED PHENOXY THIAZOLIDINEDIONES AS ESTROGEN RELATED RECEPTOR-alpha MODULATORS
  申请人：Gaul Michael

  公开号：US20090111855A1

  公开（公告）日：2009-04-30

  The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

  本发明涉及式（I）化合物，制备这些化合物的方法、组合物、中间体和衍生物，用于治疗包括但不限于强直性脊柱炎、动脉粥样硬化、关节炎（如类风湿性关节炎、感染性关节炎、儿童关节炎、银屑病性关节炎、反应性关节炎）、骨相关疾病（包括与骨形成有关的疾病）、乳腺癌（包括对抗雌激素治疗无效的乳腺癌）、心血管疾病、软骨相关疾病（如软骨损伤/丢失、软骨退化和与软骨形成有关的疾病）、软骨发育不良、软骨肉瘤、慢性背部损伤、慢性支气管炎、慢性炎性气道疾病、慢性阻塞性肺疾病、糖尿病、能量稳态紊乱、痛风、假性痛风、脂质代谢紊乱、代谢综合征、多发性骨髓瘤、肥胖症、骨关节炎、成骨不全症、骨转移性溶骨性肿瘤、软骨软化症、骨质疏松症、帕吉特病、牙周病、多肌痛风和Reiter综合征、重复性应力损伤、高血糖、血糖水平升高和胰岛素抵抗等疾病。
• Use of histamine H3 receptor inverse agonists for the control of appetite and treatment of obesity
  申请人：Gliatech, Inc.

  公开号：US20030069295A1

  公开（公告）日：2003-04-10

  A method for the use of histamine H 3 receptor inverse agonists in the regulation of appetite and treatment of obesity is disclosed. Presently preferred inverse agonists are imidazole derivatives.

  使用组胺 H 3 受体反向激动剂调节食欲和治疗肥胖症的方法。目前优选的反向激动剂是咪唑衍生物。
• Use of histamine h3 receptor inverse agonists for the control of appetite and treatment of obesity
  申请人：——

  公开号：US20040006120A1

  公开（公告）日：2004-01-08

  A method for the use of histamine II 3 receptor inverse agonists in the regulation of appetite and treatment of obesity is disclosed. Presently preferred inverse agonists are imidiazole derivatives.

  组胺 II 的使用方法 3 受体反向激动剂调节食欲和治疗肥胖症的方法。目前优选的反向激动剂是咪唑衍生物。