Rita M. O'NEIL;WELLSTAT THERAPEUTICS CORPORATION;Rita M. ONEIL
发明人:
James Dennen O'NEIL,Michael K. BAMAT,Reid W. von BORSTEL,Shalini SHARMA,Ramachandran ARUDCHANDRAN,James Dennen ONEIL
申请号：
US13890789
公开号：
US20130259850A1
申请日:
2013.05.09
申请国别(地区):
US
年份:
2013
代理人:
摘要：
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.
