| abstract |
The present invention provides IbIX glycoprotein antagonist compounds of formula (I), pharmaceutically acceptable salts and solvates thereof, wherein R and R 1 are independently H, A, OH, OA, Hal, N (R 5) 2, NO 2, CN, C ( O) R2, CON (R5) 2, COOR5, allyl, CH = CH- -COOR5, CH = CHCON (R5) 2, SO2A or phenyl optionally substituted with A; R2 and R3 are independently H, A, cycloalkyl, -Het3, - (CH2) o-OR5, - (CH2) o-OR6, - (CH2) o-Het1, - (CH2) o-NR5-Het1, - ( CHA) p- (CH2) oN (R5) 2, - (CH2) p- (CHA) p- (CH2) m-Ar, - (CH2) oZ- - (CH2) qN (R5) 2- or (a ) or (b) a group of the general formula, provided that R2 and R3 cannot be a hydrogen atom or the NR2R3 moiety forms an optionally substituted monocyclic heterocyclic group having 1 or 2 N atoms; R4 is Ar or Het1, wherein Ar is optionally substituted phenyl, naphthyl or biphenyl, Het1 and Het3 are saturated or partially unsaturated, optionally substituted 5-10 membered bicyclic heterocyclic groups having 1 or 2 N atoms and / or 1 or 2 Or the O atom may contain the latter S and O atoms (Het1-only); Y is (CH = CH) m, wherein m is 0-6; A is C1-6 alkyl. SHE |