2-butyl-6-[[(2R)-1-[1-[(4-chloro-3-methylphenyl)methyl]piperidin-4-yl]-5-oxopyrrolidine-2-carbonyl]amino]-N,N-dimethylpyridine-4-carboxamide | 1251529-03-9

• 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: 2-butyl-6-[[(2R)-1-[1-[(4-chloro-3-methylphenyl)methyl]piperidin-4-yl]-5-oxopyrrolidine-2-carbonyl]amino]-N,N-dimethylpyridine-4-carboxamide
• CAS: 1251529-03-9
• 化学式: C₃₀H₄₀ClN₅O₃
• 分子量: 554.132
• InChiKey: GMZNPEVSWOSGIT-AREMUKBSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  39
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  85.8
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  (R)-2-bromo-6-(1-(1-(4-chloro-3-methylbenzyl)piperidin-4-yl)-5-oxopyrrolidine-2-carboxamido)-N,N-dimethylisonicotinamide 、 BUTYLZINC BROMIDE 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 反应 1.08h， 生成 2-butyl-6-[[(2R)-1-[1-[(4-chloro-3-methylphenyl)methyl]piperidin-4-yl]-5-oxopyrrolidine-2-carbonyl]amino]-N,N-dimethylpyridine-4-carboxamide
  参考文献：
  名称：

  SUBSTITUTED PIPERIDINES AS CCR3 ANTAGONISTS

  摘要：

  本发明的对象是公式1的新型取代化合物，其中A、R1、R2、R3和R4的定义如描述中所述。本发明的另一个对象是提供CCR3的拮抗剂，更具体地提供包含药用可接受载体和本发明化合物中至少一种或其药用可接受盐的治疗有效量的药物组合物。

  公开号：

  US20100261687A1

文献信息

• CO-CRYSTALS AND SALTS OF CCR3-INHIBITORS
  申请人：Frank Markus

  公开号：US20120264729A1

  公开（公告）日：2012-10-18

  This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.

  本发明涉及公式1的CCR3抑制剂的共晶体和盐，包含相同物质的药物组合物，以及将其用作治疗和/或预防与CCR3受体相关疾病的药剂的方法。
• [EN] CO-CRYSTALS AND SALTS OF CCR3-INHIBITORS<br/>[FR] CO-CRISTAUX ET SELS D'INHIBITEURS DE CCR3
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2012045803A1

  公开（公告）日：2012-04-12

  This invention relates to co-crystals and salts of CCR3 inhibitors of formula (1), pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.

  本发明涉及公式（1）的CCR3抑制剂的共晶体和盐、包含它们的制药组合物，以及将它们用作治疗和/或预防与CCR3受体相关疾病的药物的方法。
• Methods and compositions for treating aging-associated impairments using CCR3-inhibitors
  申请人：Alkahest, Inc.

  公开号：US11382907B2

  公开（公告）日：2022-07-12

  Methods of improving neurodegenerative disease with CCR3 modulating agents are provided. The methods include administering a therapeutically effective amount of the CCR3 modulating agent to the subject, with a concomitant improvement in cognition, motor, or other neurodegenerative-affected function. Cognitive and motor diseases upon which the methods of the invention can improve cognition include Alzheimer's disease, Parkinson's disease, frontotemporal dementia, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, glaucoma, myotonic dystrophy, vascular dementia, progressive supranuclear palsy.

  本文提供了利用 CCR3 调节剂改善神经退行性疾病的方法。这些方法包括向受试者施用治疗有效量的 CCR3 调节剂，同时改善认知、运动或其他受神经退行性疾病影响的功能。本发明方法可改善认知的认知和运动疾病包括阿尔茨海默病、帕金森病、额颞叶痴呆症、亨廷顿氏病、肌萎缩侧索硬化症、多发性硬化症、青光眼、肌营养不良症、血管性痴呆症、进行性核上性麻痹。
• Methods and Compositions for Treating Aging-Associated Impairments Using CCR3-Inhibitors
  申请人：Alkahest, Inc.

  公开号：US20190105314A1

  公开（公告）日：2019-04-11

  Methods of improving neurodegenerative disease with CCR3 modulating agents are provided. The methods include administering a therapeutically effective amount of the CCR3 modulating agent to the subject, with a concomitant improvement in cognition, motor, or other neurodegenerative-affected function. Cognitive and motor diseases upon which the methods of the invention can improve cognition include Alzheimer's disease, Parkinson's disease, frontotemporal dementia, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, glaucoma, myotonic dystrophy, vascular dementia, progressive supranuclear palsy.
• Methods and Compositions for Treating Pruritus, Xerosis, and Associated Disease Using CCR-Inhibitors
  申请人：Alkahest, Inc.

  公开号：US20190111042A1

  公开（公告）日：2019-04-18

  Methods of treating symptoms of skin disorders with CCR3 modulating agents are provided. The methods include administering a therapeutically effective amount of the CCR3 modulating agent to the subject, with a concomitant improvement in pruritis, xerosis, or other skin disorder-affected function. Skin disorders upon which the methods of the invention can improve symptoms and causes of the disorders include eczema, bullous pemphigoid, atopic dermatitis, and psoriasis.