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    • 9. 发明申请
    • 3-BENZYLOXYPHENYLOXOACETIC ACID COMPOUNDS FOR REDUCING URIC ACID
    • 用于减少尿酸的3-苄氧基苯甲酸酸化合物
    • WO2012125533A1
    • 2012-09-20
    • PCT/US2012/028723
    • 2012-03-12
    • WELLSTAT THERAPEUTICS CORPORATIONSHARMA, ShaliniVON BORSTEL, Reid, W.
    • SHARMA, ShaliniVON BORSTEL, Reid, W.
    • A01N35/00A61K31/12
    • C07C59/215A61K31/12A61K31/192A61K31/495A61K31/52A61K45/06C07C59/90Y02A50/411A61K2300/00
    • Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or its pharmaceutically acceptable salts. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum -induced inflammation. R 1 is hydrogen or alkyl having from 1 to 3 carbon atoms. R 2 is alkyl having from 1 to 3 carbon atoms, alkoxy having from 1 to 3 carbon atoms, hydroxy, nitro, halo, thio, alkylthio, or cyano. R 3 and R 4 are each independently hydrogen, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, perfluoromethoxy, halo, hydroxy, nitro, or amino.
    • 通过施用式(I)的化合物或其药学上可接受的盐,减少哺乳动物受试者的尿酸并增加尿酸的排泄。 本发明化合物的尿酸降低作用用于治疗或预防多种病症,包括痛风,高尿酸血症,升高的尿酸水平,不符合常规诊断为高尿酸血症,肾功能不全,肾结石的水平 心血管疾病,发展心血管疾病的风险,肿瘤溶解综合征,认知障碍,早发性原发性高血压和恶性疟原虫诱发的炎症。 R 1是氢或具有1至3个碳原子的烷基。 R2是具有1至3个碳原子的烷基,具有1至3个碳原子的烷氧基,羟基,硝基,卤素,硫代,烷硫基或氰基。 R 3和R 4各自独立地为氢,甲基,乙基,全氟甲基,甲氧基,乙氧基,全氟甲氧基,卤素,羟基,硝基或氨基。