(R)-4-methyl-2-(4-(1-methyl-1H-pyrazol-4-yl)-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)pentanamide | 1312691-59-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (R)-4-methyl-2-(4-(1-methyl-1H-pyrazol-4-yl)-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)pentanamide
• 英文别名: (2R)-4-methyl-2-[[4-(1-methylpyrazol-4-yl)-3-oxo-1,2-dihydropyrrolo[3,4-c]pyridin-6-yl]amino]pentanamide
• CAS: 1312691-59-0
• 化学式: C₁₇H₂₂N₆O₂
• 分子量: 342.401
• InChiKey: WCEHKVNTHSOADA-GFCCVEGCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  115
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-氯-4-碘烟酸甲酯 在 trans-bis(triphenylphosphine)palladium dichloride 、 20 % Pd(OH)2/C potassium fluoride 、 氢气 、 过氧化脲素 、 溶剂黄146 、 三氟乙酸酐 、 三氯氧磷 作用下， 以 甲醇 、 乙二醇二甲醚 、 二氯甲烷 、 异丁酰胺 为溶剂， 150.0 ℃ 、101.33 kPa 条件下， 反应 40.0h， 生成 (R)-4-methyl-2-(4-(1-methyl-1H-pyrazol-4-yl)-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)pentanamide
  参考文献：
  名称：

  FUSED HETEROAROMATIC PYRROLIDINONES

  摘要：

  本公开涉及公式1的化合物及其药学上可接受的盐，其中G、L1、L2、R1、R2、R3和R4在说明书中有定义。本公开还涉及制备公式1化合物的材料和方法，含有它们的药物组合物，以及它们在治疗涉及免疫系统和炎症的紊乱、疾病和病况，包括类风湿关节炎、血液恶性肿瘤、上皮癌（即癌症）和其他需要抑制SYK的紊乱、疾病和病况的用途。

  公开号：

  US20110152273A1

文献信息

• FUSED HETEROAROMATIC PYRROLIDINONES AS SYK INHIBITORS
  申请人：Arikawa Yasuyoshi

  公开号：US20130116260A1

  公开（公告）日：2013-05-09

  Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L 1 , L 2 , R 1 , R 2 , R 3 , and R 4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

  本发明涉及式1的化合物及其药学上可接受的盐，其中G、L1、L2、R1、R2、R3和R4如规范中所定义。本公开还涉及制备式1化合物的材料和方法，包含它们的药物组合物，以及它们用于治疗涉及免疫系统和炎症的疾病、疾患和病况，包括类风湿性关节炎、血液恶性肿瘤、上皮癌（即癌症）和其他需要抑制SYK的疾病、疾患和病况。
• Fused heteroaromatic pyrrolidinones
  申请人：Arikawa Yasuyoshi

  公开号：US08440689B2

  公开（公告）日：2013-05-14

  Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

  本发明涉及一种公式1的化合物及其药学上可接受的盐，其中G、L1、L2、R1、R2、R3和R4在规范中定义。本公开还涉及制备公式1化合物的材料和方法、含有它们的制药组合物，以及它们用于治疗涉及免疫系统和炎症的疾病、疾病和病况，包括类风湿性关节炎、血液恶性肿瘤、上皮癌（即癌症）和其他需要抑制SYK的疾病、疾病和病况。
• Fused heteroaromatic pyrrolidinones as SYK inhibitors
  申请人：Arikawa Yasuyoshi

  公开号：US09181255B2

  公开（公告）日：2015-11-10

  Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

  本发明涉及公式1的化合物及其药学上可接受的盐，其中G、L1、L2、R1、R2、R3和R4在规范中定义。本公开还涉及制备公式1化合物的材料和方法、含有它们的药物组合物以及它们用于治疗涉及免疫系统和炎症的疾病、疾病和状况，包括类风湿性关节炎、血液恶性肿瘤、上皮癌（即癌瘤）和其他需要抑制SYK的疾病、疾病和状况。
• PROCESS FOR THE PREPARATION OF FUSED HETEROAROMATIC PYRROLIDINONES
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP3489236A1

  公开（公告）日：2019-05-29

  Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

  公开了式 1 的化合物、 及其药学上可接受的盐类，其中 G、L1、L2、R1、R2、R3 和 R4 的定义见说明书。本公开还涉及制备式 1 化合物的材料和方法、含有它们的药物组合物，以及它们在治疗涉及免疫系统和炎症的紊乱、疾病和病症方面的用途，包括类风湿性关节炎、血液恶性肿瘤、上皮癌（即癌），以及其它需要抑制 SYK 的紊乱、疾病和病症。
• Use of fused heteroaromatic pyrrolidones for treatment and prevention of diseases in animals
  申请人：Bayer Animal Health GmbH

  公开号：US11077111B2

  公开（公告）日：2021-08-03

  The present application relates to the use of fused heteroaromatic pyrrolidones for treatment and/or prophylaxis of allergic and/or inflammatory diseases in animals and to the use thereof for production of medicaments for treatment and/or prophylaxis of allergic and/or inflammatory diseases in animals, especially of atopic dermatitis and/or Flea Allergy Dermatitis, and especially in domestic animals, particularly in dogs.

  本申请涉及融合杂芳基吡咯烷酮用于治疗和/或预防动物过敏性和/或炎症性疾病的用途，以及将其用于生产治疗和/或预防动物过敏性和/或炎症性疾病，特别是特应性皮炎和/或跳蚤过敏性皮炎的药物，尤其是用于家畜，特别是狗。