4-chloro-6-(trifluoromethyl)cinnoline | 1352935-11-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 4-chloro-6-(trifluoromethyl)cinnoline
• CAS: 1352935-11-5
• 化学式: C₉H₄ClF₃N₂
• 分子量: 232.592
• InChiKey: VRPZDNRVXYUSOD-UHFFFAOYSA-N

物化性质

• 沸点：
  303.3±52.0 °C(Predicted)
• 密度：
  1.496±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-chloro-6-(trifluoromethyl)cinnoline 在 三乙胺 、 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 2-(6-(trifluoromethyl)cinnolin-4-ylamino)acetic acid
  参考文献：
  名称：

  [EN] CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
  [FR] ANTAGONISTES DU CCR2 À BASE DE CYCLOHEXYL-AZÉTIDINYLE

  摘要：

  本发明包括公式(I)的化合物。其中：R1、R2、R4、J、Q和A如说明书所述定义。本发明还包括预防、治疗或改善综合征、障碍或疾病的方法，其中所述综合征、障碍或疾病为2型糖尿病、肥胖和哮喘。本发明还包括通过管理治疗有效量的至少一种公式(I)化合物来抑制哺乳动物中的CCR2活性的方法。

  公开号：

  WO2011159854A1
• 作为产物：
  描述：

  4-(benzyloxy)-6-iodocinnoline 在 palladium 10% on activated carbon potassium fluoride 、 copper(l) iodide 、 氢气 、 三氯氧磷 作用下， 以 N-甲基吡咯烷酮 、 甲醇 、 乙酸乙酯 、 乙腈 为溶剂， 反应 26.0h， 生成 4-chloro-6-(trifluoromethyl)cinnoline
  参考文献：
  名称：

  [EN] CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
  [FR] ANTAGONISTES DU CCR2 À BASE DE CYCLOHEXYL-AZÉTIDINYLE

  摘要：

  本发明包括公式(I)的化合物。其中：R1、R2、R4、J、Q和A如说明书所述定义。本发明还包括预防、治疗或改善综合征、障碍或疾病的方法，其中所述综合征、障碍或疾病为2型糖尿病、肥胖和哮喘。本发明还包括通过管理治疗有效量的至少一种公式(I)化合物来抑制哺乳动物中的CCR2活性的方法。

  公开号：

  WO2011159854A1

文献信息

• CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
  申请人：Lanter James C.

  公开号：US20110312936A1

  公开（公告）日：2011-12-22

  The present invention comprises compounds of Formula I. wherein: R 1 , R 2 , R 4 , J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

  本发明涉及I式化合物，其中：R1、R2、R4、J、Q和A如规范中所定义。本发明还涉及一种预防、治疗或改善综合症、紊乱或疾病的方法，其中所述综合症、紊乱或疾病是II型糖尿病、肥胖和哮喘。本发明还涉及通过给哺乳动物施加至少一种I式化合物的治疗有效量来抑制CCR2活性的方法。
• Cyclohexyl-azetidinyl antagonists of CCR2
  申请人：Janssen Pharmaceutica NV

  公开号：US09062048B2

  公开（公告）日：2015-06-23

  The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

  本发明涉及公式I的化合物，其中：R1、R2、R4、J、Q和A如规范中所定义。该发明还涉及一种预防、治疗或改善综合症、疾病或疾患的方法，其中所述综合症、疾病或疾患是2型糖尿病、肥胖症和哮喘。该发明还涉及通过给哺乳动物施用公式I中至少一种化合物的治疗有效量来抑制CCR2活性的方法。
• LANCL ligands
  申请人：Landos Biopharma, Inc.

  公开号：US11459310B2

  公开（公告）日：2022-10-04

  Provided are compounds of Formula (I): The compounds target the lanthionine synthetase C-like (LANCL) family of proteins, including LANCL2 and LANCL3. The compounds can be used to treat conditions such as inflammatory diseases, metabolic diseases, autoimmune diseases, cancers, and infectious diseases. Exemplary conditions include inflammatory conditions of the liver, such as nonalcoholic fatty liver disease, nonalcoholic steatohepatitis, and cirrhosis; inflammatory conditions of the bile duct, such as primary biliary cholangitis, primary sclerosing cholangitis; inflammatory bowel disease, such as Crohn's disease and ulcerative colitis; lupus, such as systemic lupus erythematosus, lupus nephritis, and cutaneous lupus; arthritis, such as rheumatoid arthritis; hyperglycemia, such as type 1 diabetes, type 2 diabetes, and prediabetes and associated conditions such as atherosclerosis and diabetic kidney disease; psoriasis; and multiple sclerosis.

  提供的是式 (I) 化合物： 这些化合物以兰硫宁合成酶 C-样（LANCL）家族蛋白为靶标，包括 LANCL2 和 LANCL3。这些化合物可用于治疗炎症性疾病、代谢性疾病、自身免疫性疾病、癌症和传染性疾病。示例性病症包括肝脏炎症，如非酒精性脂肪肝、非酒精性脂肪性肝炎和肝硬化；胆管炎症，如原发性胆汁性胆管炎、原发性硬化性胆管炎；炎症性肠病，如克罗恩病和溃疡性结肠炎；狼疮，如系统性红斑狼疮、狼疮肾炎和皮肤狼疮；关节炎，如类风湿性关节炎；高血糖，如 1 型糖尿病、2 型糖尿病和糖尿病前期，以及动脉粥样硬化和糖尿病肾病等相关疾病；银屑病和多发性硬化症。
• LANCL LIGANDS
  申请人：Landos Biopharma, Inc.

  公开号：US20220127250A1

  公开（公告）日：2022-04-28

  Provided are compounds that target the lanthionine synthetase C-like (LANCL) family of proteins, including LANCL2 and LANCL3. The compounds can be used to treat conditions such as inflammatory diseases, metabolic diseases, autoimmune diseases, cancers, and infectious diseases. Exemplary conditions include inflammatory conditions of the liver, such as nonalcoholic fatty liver disease, nonalcoholic steatohepatitis, and cirrhosis; inflammatory conditions of the bile duct, such as primary biliary cholangitis, primary sclerosing cholangitis; inflammatory bowel disease, such as Crohn's disease and ulcerative colitis; lupus, such as systemic lupus erythematosus, lupus nephritis, and cutaneous lupus; arthritis, such as rheumatoid arthritis; hyperglycemia, such as type 1 diabetes, type 2 diabetes, and prediabetes and associated conditions such as atherosclerosis and diabetic kidney disease; psoriasis; and multiple sclerosis.
• US8518969B2
  申请人：——

  公开号：US8518969B2

  公开（公告）日：2013-08-27