3-fluoro-4-(methyl(1-methyl-1H-imidazo[4,5-c]pyridin-6-yl)amino)benzonitrile | 1449670-14-7

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 3-fluoro-4-(methyl(1-methyl-1H-imidazo[4,5-c]pyridin-6-yl)amino)benzonitrile
• 英文别名: 3-Fluoro-4-(methyl(1-methyl-1H-imidazo[4,5-c]pyridin-6-yl)amino)benzonitrile；3-fluoro-4-[methyl-(1-methylimidazo[4,5-c]pyridin-6-yl)amino]benzonitrile
• CAS: 1449670-14-7
• 化学式: C₁₅H₁₂FN₅
• 分子量: 281.292
• InChiKey: HAXHNMAAQGRYKR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  57.7
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  3-fluoro-4-(methyl(1-methyl-1H-imidazo[4,5-c]pyridin-6-yl)amino)benzonitrile 在 sodium tetrahydroborate 、 nickel(II) chloride hexahydrate 、 三氟乙酸 作用下， 以 甲醇 为溶剂， 反应 3.0h， 生成 N-(4-(aminomethyl)-2-fluorophenyl)-N,1-dimethyl-1H-imidazo[4,5-c]pyridin-6-amine
  参考文献：
  名称：

  [EN] IMIDAZO [4, 5 -C] PYRIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
  [FR] DÉRIVÉS D'IMIDAZO[4, 5-C]PYRIDINES UTILES POUR LE TRAITEMENT DE MALADIES DÉGÉNÉRATIVES ET INFLAMMATOIRES

  摘要：

  在此，R1、L1、R3、R4、Cy、L2和R5的定义如下。根据公式I披露了新型咪唑吡啶类化合物，能够抑制JAK，这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，例如过敏性或炎症性疾病、自身免疫疾病、增生性疾病、移植排斥、涉及软骨周转障碍的疾病、先天软骨畸形以及与IL6或干扰素过度分泌相关的疾病。

  公开号：

  WO2013117645A1

文献信息

• NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS
  申请人：MENET Christel Jeanne Marie

  公开号：US20150203455A1

  公开（公告）日：2015-07-23

  The present invention discloses compounds according to Formula I: wherein Cy, R 1 , L 1 , R 3 , R 4 , R 5 , L a , and R a are as defined herein. Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

  本发明公开了根据以下公式I的化合物：其中Cy、R1、L1、R3、R4、R5、La和Ra如本文所定义。根据公式I的新型苯并咪唑，能够抑制JAK，这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，包括但不限于过敏性疾病、炎症性疾病、自身免疫性疾病、增殖性疾病、移植排斥反应、涉及软骨周转障碍的疾病、先天性软骨畸形以及与IL6过度分泌或干扰素过度分泌相关的疾病。
• NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
  申请人：MENET Christel Jeanne Marie

  公开号：US20130217664A1

  公开（公告）日：2013-08-22

  Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. Wherein R 1 , L 1 , R 3 , R 4 , Cy, L 2 and R 5 are as defined herein.

  公开了一种能够抑制JAK的新型咪唑吡啶化合物，其化学式为I，这些化合物可以制备成药物组合物，并可用于预防和治疗哺乳动物，包括人类的各种疾病，例如过敏或炎症性疾病、自身免疫疾病、增殖性疾病、移植排斥、涉及软骨周转障碍的疾病、先天性软骨畸形以及与IL6或干扰素过度分泌相关的疾病。其中R1、L1、R3、R4、Cy、L2和R5如本文所定义。
• Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders
  申请人：Menet Christel Jeanne Marie

  公开号：US10179771B2

  公开（公告）日：2019-01-15

  The present invention discloses compounds according to Formula I: wherein Cy, R1, L1, R3, R4, R5, La, and Ra are as defined herein. Novel benzimidazoles according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic diseases, inflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or hypersecretion of interferons.

  本发明公开了符合式 I 的化合物： 其中 Cy、R1、L1、R3、R4、R5、La 和 Ra 如本文所定义。 根据式 I 披露了能够抑制 JAK 的新型苯并咪唑类化合物，这些化合物可制备成药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，包括非限制性举例的过敏性疾病、炎症性疾病、自身免疫性疾病、增殖性疾病、移植排斥反应、涉及软骨周转障碍的疾病、先天性软骨畸形和/或与 IL6 分泌过多或干扰素分泌过多有关的疾病。
• US9440929B2
  申请人：——

  公开号：US9440929B2

  公开（公告）日：2016-09-13
• [EN] IMIDAZO [4, 5 -C] PYRIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES<br/>[FR] DÉRIVÉS D'IMIDAZO[4, 5-C]PYRIDINES UTILES POUR LE TRAITEMENT DE MALADIES DÉGÉNÉRATIVES ET INFLAMMATOIRES
  申请人：GALAPAGOS NV

  公开号：WO2013117645A1

  公开（公告）日：2013-08-15

  Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein. Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

  在此，R1、L1、R3、R4、Cy、L2和R5的定义如下。根据公式I披露了新型咪唑吡啶类化合物，能够抑制JAK，这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，例如过敏性或炎症性疾病、自身免疫疾病、增生性疾病、移植排斥、涉及软骨周转障碍的疾病、先天软骨畸形以及与IL6或干扰素过度分泌相关的疾病。