(R)-1-(5-bromo-pyridin-2-yl)-pyrrolidin-3-ylamine | 892410-28-5

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (R)-1-(5-bromo-pyridin-2-yl)-pyrrolidin-3-ylamine
• 英文别名: (3R)-1-(5-bromopyridin-2-yl)pyrrolidin-3-amine
• CAS: 892410-28-5
• 化学式: C₉H₁₂BrN₃
• 分子量: 242.118
• InChiKey: VXRQVBVGACECNA-MRVPVSSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (R)-1-(5-bromo-pyridin-2-yl)-pyrrolidin-3-ylamine 在 sodium tetrahydroborate 、 碘 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 生成 2-[(R)-1-(5-bromo-pyridin-2-yl)-pyrrolidin-3-ylamino]-ethanol
  参考文献：
  名称：

  WO2007/146759

  摘要：

  公开号：
• 作为产物：
  描述：

  5-溴-2-氯吡啶 在 盐酸 、 potassium carbonate 作用下， 以 1,4-二氧六环 、 N,N-二甲基甲酰胺 为溶剂， 生成 (R)-1-(5-bromo-pyridin-2-yl)-pyrrolidin-3-ylamine
  参考文献：
  名称：

  Discovery of SB-705498: A potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development

  摘要：

  Small molecule antagonists of the vanilloid receptor TRPV1 (also known as VR1) are disclosed. Pyrrolidinyl ureas such as 8 and 15 (SB-705498) emerged as lead compounds following optimisation of the previously described urea SB-452533. Pharmacological studies using electrophysiological and FLIPR-Ca2+-based assays showed that compounds such as 8 and 15 were potent antagonists versus the multiple chemical and physical modes of TRPV1 activation (namely capsaicin, acid and noxious heat). Furthermore, 15 possessed suitable developability properties to enable progression of this compound into in vivo studies and subsequently clinical development. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2006.03.030

文献信息

• [EN] BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS<br/>[FR] BIS-PYRIDYLPYRIDONES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR 1 DE L'HORMONE DE CONCENTRATION DE LA MÉLANINE
  申请人：GLAXO GROUP LTD

  公开号：WO2009076387A1

  公开（公告）日：2009-06-18

  The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and/or diabetes.

  这项发明提供了新型的双吡啶基吡啉酮，它们是黑素浓集激素受体1（MCHR1）的拮抗剂，包含它们的药物组合物，它们的制备方法，以及它们在治疗和治疗肥胖和/或糖尿病中的用途。
• NOVEL MCH RECEPTOR ANTAGONISTS
  申请人：Amegadzie Albert Kudzovi

  公开号：US20100016350A1

  公开（公告）日：2010-01-21

  The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R 1 , R a , R b , R 2 , L 1 , R 3 , R 4 and R 5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.

  本发明涉及一种公式(I)的黑色素浓集激素拮抗剂化合物：其中R1、Ra、Rb、R2、L1、R3、R4和R5如定义，或其药学上可接受的盐、对映体、非对映体或其混合物，适用于治疗肥胖症及相关疾病。
• MCH receptor antagonists
  申请人：Eli Lilly and Company

  公开号：US08101764B2

  公开（公告）日：2012-01-24

  The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.

  本发明涉及一种公式(I)的黑色素浓集激素拮抗剂化合物：其中R1、Ra、Rb、R2、L1、R3、R4和R5如定义所述，或其药学上可接受的盐、对映体、二对映异构体或其混合物，用于治疗肥胖和相关疾病。
• Urea compounds active as vanilloid receptor antagonist for the treatment of pain
  申请人：Glaxo Group Limited

  公开号：EP2036902A2

  公开（公告）日：2009-03-18

  Certain compounds of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein R1, R2, P, P', n, p, q, r and s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

  某些式(I)化合物、 或其药学上可接受的盐，或其溶液，其中 R1、R2、P、P'、n、p、q、r 和 s 如说明书中所定义；制备此类化合物的工艺；包含此类化合物的药物组合物；以及此类化合物和组合物在医药中的用途。
• UREA-COMPOUNDS ACTIVE AS VANILLOID RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN
  申请人：SmithKline Beecham P.L.C.

  公开号：EP1425277A2

  公开（公告）日：2004-06-09