New 3-acylamino-3-phenyl-propionic acid derivatives, are integrin inhibitors useful e.g. for treating thrombosis, cardiac infarction, angina pectoris, tumor diseases, inflammation, osteoporosis or infections

摘要

3-(Acylamino-acylamino)-3-phenyl-propionic acid derivatives (I) and their stereoisomers, salts and solvates are new. 3-(Acylamino-acylamino)-3-phenyl-propionic acid derivatives of formula (I) and their stereoisomers, salts and solvates are new. R1 = H, A, Ar, Het1, halo, NO2, CN, OR4, COA, NHCOA, NHCHO, NR4, COOR4 or CONH(R4)2 (sic); R2 = Ar, (CH2)m-Q or (CH2)m-X-(CH2)q-Q'; Q = XA, OH, NH2, NHA, NA2, NHCOA, NO2, COOR1, CONH2, XCOYA, XCOY(CH2)q-Ar, NHCONHR2, CH2A, CHA2, CA3, Ar, CHAr2, CAr3, Het1, CH(Het1)2, C(Het1)3, cycloalkyl, NHC(=NH)NH2 or C(=NH)NH2; Q' = Ar, CHAr2, CAr3, Het1, CH(Het1)2, C(Het1)3, YA or NHCOA; R'2 = H or A; or R2 + R'2 = (CH2)p; X, Y = S, O, SO, SO2 or NH, provided that X and Y are other than SO or SO2 in (CH2)mXCOYA and (CH2)mXCOY(CH2)qAr; R3 = H2N-C(=NH)-, H2N-C(=NH)-NH-, A-C(=NH)-NH-, Het2 or Het2-NH- (where primary amino groups are optionally protected); R4 = H, A, Het1, halo, NO2 or CN; A = 1-8C alkyl; Ar = phenyl, naphthyl, anthranyl or biphenylyl (all optionally substituted by one or more of halo, A, OA, OH, COA, CN, COOA, COOH, CONH2, CONHA, CONA2, CF3, OCF3 or NO2); Het1 = mono- or binuclear aromatic heterocycle containing 1-3 N, O and/or S heteroatom(s) (optionally substituted by 1 or 2 of F, Cl, Br, A, OA, SA, OCF3, COA, CN, COOA, CONH2, CONHA, CONA2, NA2 or NO2); Het2 = mono- or binuclear heterocycle containing 1-4 N heteroatoms (optionally substituted by 1 or 2 of NH2 or NHA); m = 0-6 or 8; n = 1-6; p = 2-5; q = 0-3. An Independent claim is included for the preparation of (I).