6-(1-哌啶基甲基)-2-萘胺 | 372149-61-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 中文名称: 6-(1-哌啶基甲基)-2-萘胺
• 英文名称: 6-(1-piperidinylmethyl)-2-naphthalenamine
• 英文别名: 6-(1-piperidinylmethyl)naphthalene-2-amine；6-(piperidin-1-ylmethyl)naphthalen-2-amine
• CAS: 372149-61-6
• 化学式: C₁₆H₂₀N₂
• 分子量: 240.348
• InChiKey: PZJPGXPFQBLOHQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  6-(1-哌啶基甲基)-2-萘胺 生成 4-(4-Fluorophenyl)-N-[6-(1-piperidinylmethyl)-2-naphthyl]-1-piperidinecarboxamide
  参考文献：
  名称：

  MELANIN CONCENTRATING HORMONE ANTAGONISTS

  摘要：

  公开号：

  EP1285651B1
• 作为产物：
  描述：

  6-氨基-2-萘甲醇 在 盐酸 、 四氯化碳 、 polystyrene-triphosphine resin 、 三乙胺 作用下， 以 四氢呋喃 、 乙醇 、 氯仿 为溶剂， 反应 2.67h， 生成 6-(1-哌啶基甲基)-2-萘胺
  参考文献：
  名称：

  6-(4-Chlorophenyl)-3-substituted-thieno[3,2-d]pyrimidin-4(3H)-one-Based Melanin-Concentrating Hormone Receptor 1 Antagonist

  摘要：

  Genetic manipulation studies in mice at both the MCH receptor 1 (MCHR1) as well as the MCH peptide levels have implicated MCHR1 as a key player in energy homeostasis. The phenotype exhibited by these studies, that is, increased metabolic rate, resistance to high fat diet, and subsequent weight loss, has spurred considerable efforts to develop antagonists of MCHR1. In continuation of efforts directed toward this goal, the present work capitalizes on the putative binding mode of an MCH antagonist, resulting in the identification of several novel chemotypes that are potent and selective MCHR1 antagonists. In addition, the favorable pharmacokinetics of representative examples has allowed for the evaluation of an MCHR1 antagonist in a high fat diet-induced obese rodent model of obesity. The tolerability of the right-hand side of the template for diverse chemotypes accompanied by favorable effects on weight loss enhances the attractiveness of this template in the pursuit toward development of effective anti-obesity agents.

  DOI：

  10.1021/jm060814b

文献信息

• Melanin-concentrating hormone antagonist
  申请人：——

  公开号：US20040077628A1

  公开（公告）日：2004-04-22

  A melanin-concentrating hormone antagonist comprising a compound of the formula (I): 1 wherein Ar 1 is a cyclic group which may be substituted; X and Y are the same or different and are a spacer having a main chain of 1 to 6 atoms; Ar is a condensed polycyclic aromatic ring which may be substituted; R 1 and R 2 are the same or different and are hydrogen atom or a hydrocarbon group which may be substituted; or R 1 and R 2 , together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic ring which may be substituted; or R 2 , together with the adjacent nitrogen atom and Y, may form a nitrogen-containing heterocyclic ring which may be substituted; or R 2 , together with the adjacent nitrogen atom, Y and Ar, may form a condensed ring; or a salt thereof is useful as an agent for preventing or treating obesity, etc.

  一种黑色素浓集激素拮抗剂，包括化合物(I)的一种，其中Ar1是一个可以被取代的环状基团；X和Y相同或不同，是具有1至6个原子的主链间隔物；Ar是一个可以被取代的紧凑多环芳香环；R1和R2相同或不同，是氢原子或可以被取代的碳氢基团；或者R1和R2与相邻的氮原子一起可以形成一个可以被取代的含氮杂环；或者R2与相邻的氮原子和Y一起可以形成一个可以被取代的含氮杂环；或者R2与相邻的氮原子、Y和Ar一起可以形成一个紧凑环；或其盐，可用作预防或治疗肥胖等药物。
• US6930185B2
  申请人：——

  公开号：US6930185B2

  公开（公告）日：2005-08-16
• [EN] HETEROCYCLIC MCHR1 ANTAGONISTS<br/>[FR] ANTAGONISTES HETEROCYCLIQUES DE MCHR1
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2004092181A9

  公开（公告）日：2005-01-27

  [EN] This invention relates to novel heterocycles which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), also referred to as 11CBy, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in medicines. Compounds of the invention have formula (I).
  [FR] L'invention concerne des dérivés de benzopyrane substitués, des stéréoisomères et des sels pharmaceutiquement acceptables desdits composés, ainsi que des procédés appropriés pour les préparer. Les composés de la présente invention s'utilisent comme agonistes du récepteur beta des oestrogènes. De tels agonistes s'utilisent dans le traitement d'affections induites par le récepteur beta des oestrogènes, telles que le cancer de la prostate ou l'hyperplasie prostatique bénigne (HPB).
• 6-(4-Chlorophenyl)-3-substituted-thieno[3,2-<i>d</i>]pyrimidin-4(3<i>H</i>)-one-Based Melanin-Concentrating Hormone Receptor 1 Antagonist
  作者：Francis X. Tavares、Kamal A. Al-Barazanji、Michael J. Bishop、Christy S. Britt、David L. Carlton、Joel P. Cooper、Paul L. Feldman、Dulce M. Garrido、Aaron S. Goetz、Mary K. Grizzle、Donald L. Hertzog、Diane M. Ignar、Daniel G. Lang、Maggie S. McIntyre、Ronda J. Ott、Andrew J. Peat、Hui-Qiang Zhou

  DOI：10.1021/jm060814b

  日期：2006.11.30

  Genetic manipulation studies in mice at both the MCH receptor 1 (MCHR1) as well as the MCH peptide levels have implicated MCHR1 as a key player in energy homeostasis. The phenotype exhibited by these studies, that is, increased metabolic rate, resistance to high fat diet, and subsequent weight loss, has spurred considerable efforts to develop antagonists of MCHR1. In continuation of efforts directed toward this goal, the present work capitalizes on the putative binding mode of an MCH antagonist, resulting in the identification of several novel chemotypes that are potent and selective MCHR1 antagonists. In addition, the favorable pharmacokinetics of representative examples has allowed for the evaluation of an MCHR1 antagonist in a high fat diet-induced obese rodent model of obesity. The tolerability of the right-hand side of the template for diverse chemotypes accompanied by favorable effects on weight loss enhances the attractiveness of this template in the pursuit toward development of effective anti-obesity agents.
• MELANIN CONCENTRATING HORMONE ANTAGONISTS
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1285651B1

  公开（公告）日：2010-09-01