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5-substituted 2H-pyrazole-3-carboxylic acid derivatives as agonists for the nicotinic acid receptor RUP25 for the treatment of dyslipidemia and related diseases

机译:5-取代的2H-吡唑-3-羧酸衍生物作为烟酸受体RUP25的激动剂,用于治疗血脂异常和相关疾病

摘要

The present invention relates to certain pyrazole carboxylic acid and ester derivatives, and pharmaceutically acceptable salts thereof, which exhibit useful pharmaceutical properties, for example as agonists for the RUP25 receptor. (I) Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of alpha-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like the substituents are defined in claim 1.
机译:本发明涉及某些吡唑羧酸及其酯衍生物,及其药学上可接受的盐,它们具有有用的药学特性,例如作为RUP25受体的激动剂。 (I)本发明还提供了包含本发明化合物的药物组合物,以及使用本发明化合物和组合物预防或治疗与代谢相关的疾病,包括血脂异常,动脉粥样硬化,冠心病,胰岛素的方法。抵抗,2型糖尿病,X综合征等。另外,本发明还提供了本发明化合物与其他活性剂如α-葡萄糖苷酶抑制剂,醛糖还原酶抑制剂,双胍类,HMG-CoA还原酶抑制剂,角鲨烯合成的组合的用途。权利要求1中定义了抑制剂,贝特类,LDL分解代谢增强剂,血管紧张素转化酶(ACE)抑制剂,胰岛素分泌增强剂等。

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