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    • 1. 发明申请
    • COMPOUNDS AND METHOD FOR REDUCING URIC ACID
    • 化合物和减少尿酸的方法
    • WO2009151695A4
    • 2010-03-04
    • PCT/US2009037128
    • 2009-03-13
    • WELLSTAT THERAPEUTICS CORPO'NEIL JAMES DENNENBAMAT MICHAEL KVON BORSTEL REID WSHARMA SHALINIARUDCHANDRAN RAMACHANDRAN
    • O'NEIL JAMES DENNENBAMAT MICHAEL KVON BORSTEL REID WSHARMA SHALINIARUDCHANDRAN RAMACHANDRAN
    • A01N43/08
    • C07C59/68A23G3/36A23G3/38A23G3/42A23G3/48A23G3/563A61K8/498A61K9/0056A61K31/192A61K31/216A61K31/352A61K31/704A61K45/06A61Q11/00C07C59/66C07C59/84C07C59/88C07C59/90C07C61/39C07C69/716C07C69/734C07C69/738C07C2601/02
    • Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or a pharmaceutically acceptable salt thereof. In Formula (I) m is 0, 1, 2, 3 or 4; n is 0 or 1; m + n is not more than 4; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R6 is hydrogen, methyl or ethyl and R12 is hydrogen or methyl, or R6 is hydroxy and R12 is hydrogen, or R6 is O and R12 is absent, or R6 and R12 together are -CH2CH2-. R7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R8 and R9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R11) wherein R11 is hydrogen or alkyl having from 1 to 3 carbon atoms. A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of Formula (I) by a ring carbon; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently monosubstituted by methyl or ethyl. The uric acid-lowering effects of the Compounds of Formula (I) 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, and cognitive impairment.
    • 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。 式(I)中,m为0,1,2,3或4; n为0或1; m + n不大于4; t为0或1; q为0或1; R6是氢,甲基或乙基,R12是氢或甲基,或R6是羟基,R12是氢,或R6是O,R12不存在,或者R6和R12一起是-CH 2 CH 2 - 。 R7是氢或具有1至3个碳原子的烷基。 R8和R9中的一个是具有1至3个碳原子的烷基,另一个是氢或具有1至3个碳原子的烷基。 R 10是氢,卤素,具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基。 X为C(O),r为0且t为0; 或X是NH(R 11),其中R 11是氢或具有1至3个碳原子的烷基。 A是未取代或被1或2个选自卤素,羟基,甲基,乙基,全氟甲基,甲氧基,乙氧基和全氟甲氧基的基团取代的苯基; 或具有1或2个选自N,S和O的环杂原子的5或6元杂芳环,杂芳环通过环碳与式(I)化合物的其余部分共价结合; 或具有3至6个环碳原子的环烷基,其中环烷基是未取代的或一个或两个环碳原子被甲基或乙基独立地单取代。 式(I)化合物的尿酸降低作用用于治疗或预防各种病症,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,肾功能不全的水平, 肾结石,心血管疾病,发生心血管疾病的风险,肿瘤溶解综合征和认知障碍。
    • 3. 发明申请
    • COMPOUNDS AND METHOD FOR REDUCING URIC ACID
    • 化合物和减少尿酸的方法
    • WO2009151695A1
    • 2009-12-17
    • PCT/US2009/037128
    • 2009-03-13
    • WELLSTAT THERAPEUTICS CORPORATIONO'NEIL, James, DennenBAMAT, Michael, K.VON BORSTEL, Reid, W.SHARMA, ShaliniARUDCHANDRAN, Ramachandran
    • O'NEIL, James, DennenBAMAT, Michael, K.VON BORSTEL, Reid, W.SHARMA, ShaliniARUDCHANDRAN, Ramachandran
    • A01N43/08
    • C07C59/68A23G3/36A23G3/38A23G3/42A23G3/48A23G3/563A61K8/498A61K9/0056A61K31/192A61K31/216A61K31/352A61K31/704A61K45/06A61Q11/00C07C59/66C07C59/84C07C59/88C07C59/90C07C61/39C07C69/716C07C69/734C07C69/738C07C2601/02
    • Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula (I) or a pharmaceutically acceptable salt thereof. In Formula (I) m is 0, 1, 2, 3 or 4; n is 0 or 1; m + n is not more than 4; t is 0 or 1; q is 0 or 1; and r is 0, 1 or 2. R 6 is hydrogen, methyl or ethyl and R 12 is hydrogen or methyl, or R 6 is hydroxy and R 12 is hydrogen, or R 6 is O and R 12 is absent, or R 6 and R 12 together are -CH 2 CH 2 -. R 7 is hydrogen or alkyl having from 1 to 3 carbon atoms. One of R 8 and R 9 is alkyl having from 1 to 3 carbon atoms, and the other is hydrogen or alkyl having from 1 to 3 carbon atoms. R 10 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms or alkoxy having from 1 to 3 carbon atoms. X is C(O) and r is 0 and t is 0; or X is NH(R 11 ) wherein R 11 is hydrogen or alkyl having from 1 to 3 carbon atoms. A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from halo, hydroxy, methyl, ethyl, perfluoromethyl, methoxy, ethoxy, and perfluoromethoxy; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of Formula (I) by a ring carbon; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently monosubstituted by methyl or ethyl. The uric acid-lowering effects of the Compounds of Formula (I) 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, and cognitive impairment.
    • 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。 式(I)中,m为0,1,2,3或4; n为0或1; m + n不大于4; t为0或1; q为0或1; R6是氢,甲基或乙基,R12是氢或甲基,或R6是羟基,R12是氢,或R6是O,R12不存在,或者R6和R12一起是-CH 2 CH 2 - 。 R7是氢或具有1至3个碳原子的烷基。 R8和R9中的一个是具有1至3个碳原子的烷基,另一个是氢或具有1至3个碳原子的烷基。 R 10是氢,卤素,具有1至3个碳原子的烷基或具有1至3个碳原子的烷氧基。 X为C(O),r为0且t为0; 或X是NH(R 11),其中R 11是氢或具有1至3个碳原子的烷基。 A是未取代或被1或2个选自卤素,羟基,甲基,乙基,全氟甲基,甲氧基,乙氧基和全氟甲氧基的基团取代的苯基; 或具有1或2个选自N,S和O的环杂原子的5或6元杂芳环,杂芳环通过环碳与式(I)化合物的其余部分共价结合; 或具有3至6个环碳原子的环烷基,其中环烷基是未取代的或一个或两个环碳原子被甲基或乙基独立地单取代。 式(I)化合物的尿酸降低作用用于治疗或预防各种病症,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,肾功能不全的水平, 肾结石,心血管疾病,发生心血管疾病的风险,肿瘤溶解综合征和认知障碍。