4-(pyrimidin-2-ylamino)-piperidine-1-carboxylic acid ethyl 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-(pyrimidin-2-ylamino)-piperidine-1-carboxylic acid ethyl ester
• 英文别名: ethyl 4-(2-pyrimidinylamino)-1-piperidinecarboxylate；ethyl 4-(pyrimidin-2-ylamino)piperidine-1-carboxylate
• 化学式: C₁₂H₁₈N₄O₂
• mdl: MFCD11118512
• 分子量: 250.301
• InChiKey: YWPZNKNNUDFQFZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.583
• 拓扑面积：
  67.4
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-(pyrimidin-2-ylamino)-piperidine-1-carboxylic acid ethyl ester 在 水 、 氢溴酸 作用下， 反应 18.0h， 生成 piperidin-4-yl-pyrimidin-2-yl-amine dihydrobromide
  参考文献：
  名称：

  Pyrimidine, quinazoline, pteridine and triazine derivatives

  摘要：

  这项发明涉及以下式的化合物 其中A，R1至R5和G如描述和声明中所定义，并其药学上可接受的盐。该发明还涉及含有这种化合物的药物组合物，以及用于制备它们的方法和它们用于治疗和/或预防与调节SST受体亚型5相关的疾病的用途。

  公开号：

  US20070225271A1
• 作为产物：
  描述：

  2-氯嘧啶 、 4-氨基-1-哌啶甲酸乙酯 在 溴化亚铜 乙酸乙酯 、 magnesium sulfate 、 silica 、 二氯甲烷 、 甲醇 、 title compound 作用下， 以 N,N-二甲基乙酰胺 、 三乙胺 为溶剂， 反应 0.33h， 生成 4-(pyrimidin-2-ylamino)-piperidine-1-carboxylic acid ethyl ester
  参考文献：
  名称：

  Pyrimidine, quinazoline, pteridine and triazine derivatives

  摘要：

  本发明涉及以下式子的化合物，其中A，R1至R5和G如描述和权利要求中所定义，并且其药学上可接受的盐。本发明还涉及含有这种化合物的药物组合物，以及制备它们的过程和它们用于治疗和/或预防与SST受体亚型5调节相关的疾病的用途。

  公开号：

  US07855194B2

文献信息

• (BENZODIOXAN, BENZOFURAN OR BENZOPYRAN)-ALKYLAMINO] ALKYL SUBSTITUTED GUANIDINES AS SELECTIVE VASCOCONSTRICTORS
  申请人：JANSSEN PHARMACEUTICA N.V.

  公开号：EP0639192A1

  公开（公告）日：1995-02-22
• PYRIMIDINE, QUINAZOLINE, PTERIDINE AND TRIAZINE DERIVATIVES
  申请人：F. Hoffmann-La Roche AG

  公开号：EP2001867B1

  公开（公告）日：2009-07-01
• PIPERIDINE/PIPERAZINE DERIVATIVES
  申请人：Janssen Pharmaceutica NV

  公开号：US20170029440A1

  公开（公告）日：2017-02-02

  The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NR x —C(═O)—; —Z—C(═O)—; —Z—NR x —C(═O)—; —S(═O)p-; —C(═S)—; —NR x —C(═S)—; —Z—C(═S)—; —Z—NR x —C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R 1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R 2 represents R 3 ; R 3 represents C 3-6 cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C 3 - 6 cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
• DRUG COMBINATIONS COMPRISING A DGAT INHIBITOR AND A PPAR-AGONIST
  申请人：Janssen Pharmaceutica NV

  公开号：US20180028660A1

  公开（公告）日：2018-02-01

  The present invention relates to combinations of a DGAT inhibitor and a peroxisome proliferator-activator receptor (PPAR) agonist or a prodrug thereof. The invention further relates to methods for preparing such combinations, pharmaceutical compositions comprising said combinations as well as the use as a medicament of said combinations. The present invention also relates to novel DGAT inhibitors. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicament of said compounds.
• US4126689A
  申请人：——

  公开号：US4126689A

  公开（公告）日：1978-11-21