| abstract |
Inhibitors of integrin alfavbeta3 of formula (1) are described: XYZ-R1-CH2-R2 (R4) -CH2-CO-R5, wherein: X means H2N-C (= NH) -, H2N-C (= NH ) -NH, AC (= NH) -NH-, Het1- or Het1-NH-, where the primary amino groups may also be provided with conventional amino protecting groups; Y means - (CH2) n, or a compound of formula (2) where 1, 2, 3 or 4 methylene group may be replaced by N, O and / or S; Z is absent or means -O-, -NH-, -NA-, -CH (OH) -, -CH (OA) -, -CHA-, -CA2- or -S-; R1 means phenylene unsubstituted or substituted 1, 2 or 3 times with F, Cl, Br, A, OA, OCF3 or CN; R2 means N, CH or CA; R3 means H, F, Cl, Br, A, OA or OCF3; R4 means phenyl, naphthyl or Het2 not substituted or substituted once or several times with A, aryl or CF3; R5 means OH, OA, NH2, NHA or NA2; Het1 means a heterocycle of 1 or 2 nuclei with 1 to 4 N atoms, which may be unsubstituted or substituted 1-2 times with NH2; Het2 means an aromatic heterocycle of 1 or 2 nuclei with 1 to 3 atoms of N, O and / or S, which may be unsubstituted or substituted 1 or 2 times with F, Cl, Br, A, OA, SA, OCF3, -CO-A, CN, COOA, CONH2, CONHA, CONA2 or NO2; Aryl means phenyl unsubstituted or substituted 1, 2 or 3 times with Hal, A or OA; A means C1-12 alkyl; n means from 1 to 12; m and or independently of each other mean from 1 to 12; as well as its physiologically harmless salts and solvates. These compounds especially inhibit the interactions of alphav receptors with ligands, being especially effective as ligands of integrin alfavbeta3. A process for preparing the compounds of formula (1), the medicines based on these compounds, the pharmaceutical compositions containing them and the use thereof for the preparation of a medicament for combating diseases based on the disease is also described. expression and pathological function of integrin alfavbeta3 receptors, in particular, to combat thrombosis, myocardial infarction, coronary heart disease, arteriosclerosis, tumors, osteoporosis, fibrosis, inflammations, infections, lapsoriasis, as well as to influence wound healing processes. |