N-hydroxyl-5-substituted-1H-pyrazol-3-formamide compound as well as preparation method and use thereof

• Main Authors: YANG KAN, WANG JINXIN, ZHI ZHUO'ER, NONG KEYI
• Format: Patent
• Language: Chinese; English
• Published: 18.01.2019
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention belongs to the field of medicine chemistry, and particularly relates to an N-hydroxyl-5-substituted-1H-pyrazol-3-formamide compound as well as a preparation method and use thereof. The specific structure of the compound is as shown in a formula I. The invention also provides a synthesis method of the compound in the formula I and inhibition activity thereof for acidic sphingomyelinase. The compound can be used for developing drugs for treating atherosclerosis (AS), diabetes, emphysema, pulmonary edema, pulmonary fibrosis, cystic fibrosis, chronic obstructive pulmonary disease, pulmonary arterial hypertension, non-alcoholic fatty liver disease, Alzheimers (AD), multiple sclerosis (MS), cerebral stroke and depression diseases. (the formula I is shown in the description). 本发明属于药物化学领域，具体涉及种N-羟基-5-取代-1H-吡唑-3-甲酰胺化合物及其制备方法和用途。本发明提供的该类化合物具体结构为式I所示.本发明还提供了式I中化合物的合成方法及其对酸性鞘磷脂酶的抑制活性。该类化合物可用于开发治疗动脉粥样硬化(AS)、糖尿病、肺气肿、肺水肿、肺部纤维化、囊性纤维化、慢阻肺、肺动脉高压、非酒精性脂肪肝、阿尔兹海默(AD)、多发性硬化症(MS)、脑卒中、抑郁症相关药物。