Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof
申请人:Arena Pharmaceuticals, Inc.
公开号:US07241792B2
公开(公告)日:2007-07-10
The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor.
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 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 α-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, DP receptor antagonists, and the like.
本发明涉及公式(Ia)的某些融合吡唑衍生物及其药学上可接受的盐,具有有用的药理特性,例如作为RUP25受体的激动剂。本发明还提供了包含本发明化合物的制药组合物以及使用本发明化合物和组合物治疗代谢相关疾病的方法,包括血脂异常、动脉粥样硬化、冠心病、胰岛素抵抗、2型糖尿病、综合征X等。此外,本发明还提供了将本发明化合物与其他活性剂(如属于α-葡萄糖苷酶抑制剂、醛还原酶抑制剂、双胍类、HMG-CoA还原酶抑制剂、角鲨烷合成抑制剂、纤维酸类、LDL降解增强剂、血管紧张素转化酶(ACE)抑制剂、胰岛素分泌增强剂、DP受体拮抗剂等)组合使用的方法。