N-(5-((3S,8aS)-3-benzyl-octahydropyrrolo[1,2-a]pyrazine-2-carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-2,3-difluorobenzamide | 1072099-50-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(5-((3S,8aS)-3-benzyl-octahydropyrrolo[1,2-a]pyrazine-2-carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-2,3-difluorobenzamide
• 英文别名: N-[5-[(3S,8aS)-3-benzyl-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazine-2-carbonyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-c]pyrazol-3-yl]-2,3-difluorobenzamide
• CAS: 1072099-50-3
• 化学式: C₂₉H₃₂F₂N₆O₂
• 分子量: 534.609
• InChiKey: YTDCATVZXIFGNQ-PMACEKPBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  39
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  84.6
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• NOVEL 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H,4H,6H) CARBALDEHYDE DERIVATIVES
  申请人：Botrous Iriny

  公开号：US20100249128A1

  公开（公告）日：2010-09-30

  The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.

  本发明涉及式（I）的化合物和药学上可接受的盐，其中X，R1，R2，R3，R4，R5，R6，R7和R8如上所定义。本发明还涉及包含该化合物和药学上可接受的盐的制药组合物以及治疗糖尿病及其并发症（尤其是糖尿病视网膜病变、肾病或神经病变）、癌症、缺血、炎症、中枢神经系统疾病、心血管疾病、阿尔茨海默病和皮肤病、病毒性疾病、炎症性疾病或肝脏是靶器官的疾病的治疗方法。
• 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H,6H) CARBALDEHYDE DERIVATIVES AS INHIBITORS OF PROTEIN KINASE C
  申请人：Pfizer Inc.

  公开号：EP2195321B1

  公开（公告）日：2016-10-19
• US8114871B2
  申请人：——

  公开号：US8114871B2

  公开（公告）日：2012-02-14
• [EN] NOVEL 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H.6H) CARBALDEHYDE DERIVATIVES<br/>[FR] NOUVEAUX DERIVES DE 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H,4H.6H) CARBALDEHYDE
  申请人：PFIZER

  公开号：WO2008125945A2

  公开（公告）日：2008-10-23

  [EN] The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R¹, R², R³, R⁴, R⁵, R⁶, R⁷, and R⁸ are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
  [FR] L'invention concerne des composés et des sels pharmaceutiquement acceptables de Formule (I) : dans laquelle X, R¹, R², R³, R⁴, R⁵, R⁶, R⁷ et R⁸ sont tels que définis dans la description. L'invention concerne également des compositions pharmaceutiques contenant ces composés et sels pharmaceutiquement acceptables, ainsi que des méthodes de traitement du diabète sucré et de ses complications (en particulier la rétinopathie, la néphropathie ou la neuropathie diabétiques), du cancer, de l'ischémie, des inflammations, des troubles du système nerveux central, des maladies cardiovasculaires, de la maladie d'Alzheimer, des maladies dermatologiques, des maladies virales, des troubles inflammatoires ou des maladies dans lesquelles le foie est un organe cible.