7-Fluoroquinoline-3-carbonyl chloride | 1398583-93-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 7-Fluoroquinoline-3-carbonyl chloride
• CAS: 1398583-93-1
• 化学式: C₁₀H₅ClFNO
• 分子量: 209.607
• InChiKey: DVGKTZQMSAUCPO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  30
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] ARYLCARBOXAMIDES AND USES THEREOF<br/>[FR] ARYLCARBOXAMIDES ET LEURS UTILISATIONS
  申请人：INCEPTION 1 INC

  公开号：WO2017192304A1

  公开（公告）日：2017-11-09

  The present disclosure is directed to compounds of formula (I): or a pharmaceutically acceptable salt, solvate or solvate of the salt thereof. Compounds of formula (I) are inhibitors of NOX4 and are useful in the treatment of fibrotic diseases such as scleroderma; lung disease, such as pulmonary fibrosis including idiopathic pulmonary fibrosis (IPF); heart disease, such as heart failure due to ischaemic heart disease, valvular heart disease and hypertensive heart disease, diabetic cardiomyopathy and hypertension; liver disease, such as cirrhosis of the liver; and kidney disease, such as progressive kidney disease glomerulonephritis and diabetic nephropathy; and eye disease such as diabetic retinopathy; skin or subcutaneous scarring, such as keloids, adhesions, hypertrophic scarring or cosmetic scarring; or as an adjuvant or anti-fibrotic in pancreatic cancer to increase chemotherapeutic drug penetration by reducing the density of the connective tissue stroma.

  本公开涉及的化合物具有以下结构式（I）：或其药学上可接受的盐、溶剂或该盐的溶剂。结构式（I）的化合物是NOX4的抑制剂，可用于治疗纤维化疾病，如硬皮病；肺部疾病，如肺纤维化，包括特发性肺纤维化（IPF）；心脏疾病，如缺血性心脏病、瓣膜性心脏病和高血压性心脏病、糖尿病性心肌病和高血压；肝脏疾病，如肝硬化；肾脏疾病，如进行性肾脏疾病肾小球肾炎和糖尿病肾病；眼部疾病，如糖尿病视网膜病变；皮肤或皮下疤痕，如瘢痕、粘连、肥厚性瘢痕或美容瘢痕；或作为胰腺癌的辅助治疗或抗纤维化剂，通过减少结缔组织基质密度来增加化疗药物的渗透性。
• [EN] ARYL SUBSTITUTED CARBOXAMIDE DERIVATIVES AS TRPM8 MODULATORS<br/>[FR] DÉRIVÉS DE CARBOXAMIDE SUBSTITUÉS PAR ARYLE EN TANT QUE MODULATEURS DE TRPM8
  申请人：PFIZER LTD

  公开号：WO2012120398A1

  公开（公告）日：2012-09-13

  The invention provides a compound of the formula (I): wherein A, R1, R2 and R3 are as defined herein, or a pharmaceutically acceptable salt thereof. Such compounds are small molecule TRPM8 blockers and therefore useful in the propylaxis or treatment of a wide range of diseases, conditions or syndromes, including cold allodynia and Raynaulds syndrome.

  本发明提供了一种化合物，其化学式为（I）：其中A、R1、R2和R3如本文所定义，或其药学上可接受的盐。这些化合物是小分子TRPM8阻断剂，因此在预防或治疗包括寒冷痛觉异常和雷诺综合征在内的各种疾病、症状或综合征中有用。