1-(5-iodo-pyridin-2-yl)-4-methyl-piperazine | 690264-76-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-(5-iodo-pyridin-2-yl)-4-methyl-piperazine
• 英文别名: 1-(5-iodopyridin-2-yl)-4-methylpiperazine
• CAS: 690264-76-7
• 化学式: C₁₀H₁₄IN₃
• 分子量: 303.146
• InChiKey: RYQYFQBERWMOQO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  19.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(5-iodo-pyridin-2-yl)-4-methyl-piperazine 、 5-(4-chloro-phenyl)-2-ethynyl-pyridine 生成 1-{5-[5-(4-Chloro-phenyl)-pyridin-2-ylethynyl]-pyridin-2-yl}-4-methyl-piperazine
  参考文献：
  名称：

  Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds

  摘要：

  本发明涉及一般式I的炔烃化合物，其中基团和残基A、B、W、X、Y、Z、R1和R2具有权利要求1中所给出的含义。本发明还涉及含有至少一种根据本发明的炔烃的药物组合物。鉴于它们的MCH受体拮抗活性，本发明的药物组合物适用于治疗代谢紊乱和/或饮食紊乱，尤其是肥胖症、暴食症、厌食症、过度进食和糖尿病。

  公开号：

  US08618132B2
• 作为产物：
  描述：

  1-(5-溴吡啶-2-基)-4-甲基哌嗪 生成 1-(5-iodo-pyridin-2-yl)-4-methyl-piperazine
  参考文献：
  名称：

  Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds

  摘要：

  本发明涉及一般式I的炔烃化合物 1 其中基团和残基A、B、W、X、Y、Z、R 1 和R 2 具有权利要求中给出的含义。本发明还涉及含有根据本发明至少一种炔烃的药物组合物。鉴于它们的MCH受体拮抗活性，根据本发明的药物组合物适用于治疗代谢紊乱和/或进食紊乱，特别是肥胖症、暴食症、厌食症、过度进食和糖尿病。

  公开号：

  US20040209865A1

文献信息

• ALKYNE COMPOUNDS WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS
  申请人：Stenkamp Dirk

  公开号：US20090069282A1

  公开（公告）日：2009-03-12

  The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R 1 and R 2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

  本发明涉及一般式I的炔化合物，其中A、B、W、X、Y、Z、R1和R2的基团和残基具有权利要求1中给出的含义。本发明还涉及包含至少一种根据本发明的炔烃的制药组合物。鉴于它们的MCH受体拮抗活性，根据本发明的制药组合物适用于治疗代谢性疾病和/或进食障碍，特别是肥胖症、暴食症、厌食症、过度进食和糖尿病。
• 4,6,7-TRISUBSTITUTED 1,2-DIHYDROPYRROL[3,4-C]PYRIDIN/PYRIMIDIN-3-ONE DERIVATIVE AND USE
  申请人：Shanghai Haiyan Pharmaceutical Technology Co., Ltd.

  公开号：EP3689871A1

  公开（公告）日：2020-08-05

  The present disclosure relates to 4,6,7-trisubstituted 1,2-dihydropyrrolo[3,4-c]pyridin/pyrimidin-3-one derivatives, and their preparations and medicinal use. Specifically, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof, wherein the definition of each group is as described in the specification and claims.

  本公开涉及4,6,7-三取代的1,2-二氢吡咯并[3,4-c]吡啶/嘧啶-3-酮衍生物及其制剂和药用。具体地说，本公开公开了式(I)化合物或其药学上可接受的盐、立体异构体、溶媒或原药及其制备方法和用途，其中各组的定义如说明书和权利要求书中所述。
• NEUE ALKIN-VERBINDUNGEN MIT MCH-ANTAGONISTISCHER WIRKUNG UND DIESE VERBINDUNGEN ENTHALTENDE ARZNEIMITTEL
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：EP1558578B1

  公开（公告）日：2013-03-13
• MDM2-BASED MODULATORS OF PROTEOLYSIS AND ASSOCIATED METHODS OF USE
  申请人：Arvinas Operations, Inc.

  公开号：US20220127279A1

  公开（公告）日：2022-04-28

  The description relates to MDM2 binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the MDM2 E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
• US7452911B2
  申请人：——

  公开号：US7452911B2

  公开（公告）日：2008-11-18