Patent ID: 6833387
Filing Date: 2004-12-21
Classification: A61K,A61P,C07D

Abstract:
A method for treating â€˜rheumatoid arthritis, glomerular nephritides, lung fibrosis, restenosis, asthma, atherosclerosis, psoriasis, delayed-type hypersensitivity reactions of the skin, inflammatory bowel disease, multiple sclerosis, inflammation resulting from brain trauma, stroke, ischemia, myocardial infarction and transplant rejectionâ€™ comprising inhibiting monocyte chemoattractant protein-1 and/or RANTES-induced chemotaxis, said method comprising administering to a patient in need thereof an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or ester thereof; wherein X is CH2 or SO2; R1 is an optionally substituted aryl ring; R2 is carboxy, cyano, â€”C(O)CH2OH, â€”CONHR8, â€”SO2NHR9, or SO3H, where R8 is selected from hydrogen, alkyl, aryl, cyano, hydroxy, â€”SO2R12 where R12 is alkyl, aryl, or haloalkyl, or R8 is a group â€”(CHR13)râ€”COOH where r is an integer of 1-3 and each R13 group is independently selected from hydrogen or alkyl; R9 is hydrogen, alkyl, or optionally substituted aryl, or a group COR14 where R14 is alkyl, aryl, or haloalkyl; and R10 and R11 are independently selected from hydrogen or alkyl, particularly C1-4 alkyl; R3 is a group OR15, S(O)qR15, NHCOR16, NHSO2R16, (CH2)sCOOH, (CH2)tCONR17R18, NR17R18, SO2NR17R18 or optionally substituted alkenyl, where q is 0, 1 or 2, s is 0 or an integer of from 1 to 4, t is 0 or an integer of from 1 to 4, R15 is a substituted cycloalkyl group or an alkyl group substituted with one or more groups selected from halogen, hydroxy, cyano, amino, mono- or di-alkylamino, C1-4 alkoxy, carboxy, sulphonamido, CONH2, morpholino, pyridyl, pyrimidinyl, phenyl optionally substituted by halogen, carboxy, alkoxy, carbamoyl, acyl groups, or hydroxyalkyl wherein the alkyl group in the hydroxyalkyl moiety includes at least two carbon atoms, R16 is optionally substituted alkyl or optionally substituted aryl, and R17 and R18 are independently selected from hydrogen, optionally substituted alkyl, and optionally substituted aryl, with the proviso that at least one of R17 or R18 is other than hydrogen; and R4 is selected from hydrogen, hydroxyl, halo, alkoxy, aryloxy, araalkyl, carboxyalkyl; and R5, R6, and R7 are independently selected from hydrogen, hydroxyl, halo, alkoxy, or an optionally substituted hydrocarbyl group.