N-(5-((2R,5S)-2,5-dimethyl-1-((tetrahydro-2H-pyran-4-yl)methyl)piperazine-4-carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)picolinamide | 1072100-81-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: N-(5-((2R,5S)-2,5-dimethyl-1-((tetrahydro-2H-pyran-4-yl)methyl)piperazine-4-carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)picolinamide
• 英文别名: PF-04577806；2-Pyridinecarboxamide, N-(5-(((2S,5R)-2,5-dimethyl-4-((tetrahydro-2H-pyran-4-yl)methyl)-1-piperazinyl)carbonyl)-1,4,5,6-tetrahydro-6,6-dimethylpyrrolo(3,4-c)pyrazol-3-yl)-；N-[5-[(2S,5R)-2,5-dimethyl-4-(oxan-4-ylmethyl)piperazine-1-carbonyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-c]pyrazol-3-yl]pyridine-2-carboxamide
• CAS: 1072100-81-2
• 化学式: C₂₆H₃₇N₇O₃
• 分子量: 495.625
• InChiKey: WIUOWTNXQICTJG-MSOLQXFVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  36
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  107
• 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。
• NOVEL 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H,6H) CARBALDEHYDE DERIVATIVES
  申请人：Botrous Iriny

  公开号：US20120108588A1

  公开（公告）日：2012-05-03

  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.

  本发明涉及公式（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。
• Compositions and methods for promoting the generation of endocrine cells
  申请人：President and Fellows of Harvard College

  公开号：US10941384B2

  公开（公告）日：2021-03-09

  Disclosed herein are compositions and methods for the generation of insulin positive β cells, for example by exposing Pdx+ pancreatic progenitor cells to one or more compounds, and compositions and kits comprising isolated populations of insulin positive cells.

  本文公开了生成胰岛素阳性β细胞的组合物和方法，例如通过将Pdx+胰腺祖细胞暴露于一种或多种化合物，以及包含分离的胰岛素阳性细胞群的组合物和试剂盒。
• Treatment of cancer
  申请人：MingSight Pharmaceuticals, Inc.

  公开号：US11154555B2

  公开（公告）日：2021-10-26

  Provided herein are compositions and methods for the treatment of a hematological malignancy. Also disclosed herein are compositions and methods for the treatment of Ewings Sarcoma. Said compositions comprise isoform selective pyrrolo-pyrazole PKC inhibitors.

  本文提供了治疗血液恶性肿瘤的组合物和方法。 本文还公开了治疗尤文肉瘤的组合物和方法。 所述组合物包括同工酶选择性吡咯-吡唑PKC抑制剂。
• 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：EP2195321A2

  公开（公告）日：2010-06-16