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    • 6. 发明申请
    • 5-SUBSTITUTED 2H-PYRAZONE-3-CARBOXYLIC ACID DERIVATIVES AS ANTILIPOLYTIC AGENTS FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS SUCH AS DYSLIPIDEMIA
    • 5-取代的2H-吡唑-3-羧酸衍生物作为治疗与代谢相关的疾病如抗坏血酸的抗血小板剂
    • WO2004032928A1
    • 2004-04-22
    • PCT/US2003/032174
    • 2003-10-09
    • ARENA PHARMACEUTICALS, INC.SEMPLE, GraemeAVERBUJ, ClaudiaSKINNER, PhilipGHARBAOUI, TawfikSHIN, Young-Jun
    • SEMPLE, GraemeAVERBUJ, ClaudiaSKINNER, PhilipGHARBAOUI, TawfikSHIN, Young-Jun
    • A61K31/45
    • C07D231/16C07D231/14
    • The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R 2 is H, halogen, C 1-12 alkyl or C 1-12 haloalkyl; and R 3 is C 3-6 cycloalkyl, C 1-12 alkyl, C 1-12 haloalkyl, C 3-6 cycloalkyl-C 1-4 -alkylene, aryl-C 1-4 -alkylene or heteroaryl-C 1-4 -alkylene, wherein said aryl-C 1-4 -alkylene and heteroaryl-C 1-4 -alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. 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 pharmaceutical compositions in combination with other active agents, for example, those agents 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, thiazolidinedione and the like.
    • 本发明涉及某些式(Ia)的吡唑羧酸衍生物及其药学上可接受的盐,作为抗脂解剂和抗受体RUP25,其中:R2是H,卤素,C1-12烷基或C1-12卤代烷基; 且R 3为C 3-6环烷基,C 1-12烷基,C 1-12卤代烷基,C 3-6环烷基-C 1-4亚烷基,芳基-C 1-4亚烷基或杂芳基-C 1-4 - 亚烷基,其中所述芳基-C1 -4-亚烷基和杂芳基-C 1-4 - 亚烷基可以是任选取代的1至5个选自权利要求中所列取代基的取代基。 本发明还提供含有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治疗代谢相关疾病包括血脂异常,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,本发明还提供了与其它活性剂(例如属于α-葡糖苷酶抑制剂,醛糖还原酶抑制剂,双胍类,HMG-CoA还原酶抑制剂,角鲨烯合成抑制剂,贝特类)的那些试剂组合的药物组合物 ,LDL分解代谢增强剂,血管紧张素转换酶(ACE)抑制剂,胰岛素分泌增强剂,噻唑烷二酮等。