| abstract |
Compounds useful in modulating blood uric acid levels, formulations containing them and methods for using them are described herein. The compounds described herein are used in the treatment or prevention of disorders related to aberrant uric acid levels. Such disorders include polycythemia, myeloid metaplasia, gout, hyperuricemia, hypertension, coronary heart disease, stones and kidney failure, among others. Claim 1: A compound of the formula (1), wherein: Ra and Rb are selected from H, halogen, C1-6 alkyl; or Ra and Rb, together with the carbon atom to which they adhere, form a 3-, 4-, 5- or 6- membered ring, optionally containing one or two heteroatoms selected from O, N and S; M is H, C1-3 alkyl or a pharmaceutically acceptable cation; X1 is N, CH, C (halogen) or C (C1-4 alkyl); X2 is N or CH; X3 is N, CH, C (halogen) or C (C1-4 alkyl); X4 is N or CH; wherein at least one of X1, X2, X3 or X4 is N; Y1 is N or CR1; Y2 is N or CR2; R1 is H, CF3, CH3, OCH3, F or Cl; R2 is H, methyl, ethyl, propyl, isopropyl, tert-butyl, cyclopropyl, cyclobutyl, CF3, OH, OCH3, ethoxy, SH, SCH3, SCH2CH3, CH2OH, C (CH3) 2OH, Cl, F, CN, COOH, COOR2 ', CONH2, CONHR2' or SO2NH2; wherein R2 ’is H or C1-3 alkyl; R3 is H, halogen, -CN, C1-6 alkyl, C1-6 alkoxy; and R4 is H, halogen, -CN, C1-6 alkyl, C1-6 alkoxy; or R3 and R4 together with the carbon atoms to which they adhere form an optionally substituted 5 or 6 member ring, optionally containing one or two heteroatoms selected from O, N and S, wherein said 5 or 6 member ring it can be a saturated ring, an unsaturated ring or an aromatic ring; and since: if X2 and X4 are both N, then X1 cannot be C (halogen); or if X2 and X4 are both N, then R4 cannot be Cl; or if X2 and X4 are both N, then Y2 cannot be C-Cl; if X1 and X2 are both N, then X3 cannot be C-Cl; and since the compound of the formula (1) is not 1- (3- (4-cyanophenyl) pyridin-4-ylthio) cyclopropanecarboxylic acid. |