Alfavbeta3 Integrin Inhibitors, a process for their preparation, medicinal products based on these Compounds, Pharmaceutical compositions containing them and Use thereof for preparing a Medicine to fight diseases that are based on the expression and function.

摘要

Describes the alfavbeta3 Integrin inhibitors of formula (1): X - y - Z - CH2 - R2 (R1 - R4 R5) - CH2 - CO, where X means: H2n - C (= NH) H2n -, - C (= NH) - NH, - C (= NH het1) - NH -, - or het1 - NH -, where the primary amino groups can also be fitted with conventional amino Protecting groups; and S Means N - (CH2), or a compound of formula (2) for 1, 2,3 or 4 methylene Group can be replaced by N, and / or s; Z is absent or means - or -, - NH -, na -, - ch - ch (OH) (OA), cha, Ca2 - or - S - phenylene R1 does not; replaced or substituted 1, 2 or 3 times with F, CL, BR, CN, OA, or ocf3; R2 is n, CH or CA; R3 is H, F, CL, B R, a, AB or ocf3 means; R4 phenyl, naphthyl, or het2 unsubstituted or substituted with one or several times,Aryl or Cf3; R5 oa means, NH2, Oh, Nha or NA2; het1 means a Heterocycles 1 or 2 cores with one to four n ATOMS, which can not be replaced or substituted 1 - 2 times with NH2; het2 means a Heterocyclic Aromatic Nuclei with 1 to 1 or 2 3 Atoms of N or and / or s, which may be not 1 or 2 Times replaced or substituted with F, CL, BR, or SA, ocf3, co, CN, CONH2 conha COOA,,,Cona2 or NO2; aryl phenyl substituted or unsubstituted means 1, 2 or 3 times with Hal, or oa means C1 - 12; alkyl; n is 1 to 12; M and mean or independently from 1 to 12; and their Salts and solvates physiologically harmless.These compounds inhibit the interaction of the Receptor with the ligand alfav, being especially effective as alfavbeta3 Integrin ligands.Also described is a process for preparing compounds of formula (1), drugs containing these Compounds, Pharmaceutical compositions containing them and Use thereof for the preparation of a drug to combat diseases that are based on the expression The Function and the Pathological alfavbeta3 Integrin Receptors, in particular,To combat the thrombosis, myocardial infarction, coronary heart disease, arteriosclerosis, Tumors, osteoporosis, fibrosis, inflammation, Infections, lapsoriasis, so as to influence the processes of Wound Healing.