CYLLOPEPTIDE DERIVATIVES Russian patent published in 2001 - IPC

FIELD: medicine. SUBSTANCE: described are new compounds of formula 1 R¹-Q¹-X-Q²-R², wherein Q¹ Q² in each case is undependable either not present or is NH--(CH₂)_n-CO-, n is 1,2,3,4,5,6,7,8,9 or 10; R¹,R² in each case independently are either not present or cyclo (Arg-Gly-Asp-Z) wherein Z is bonded in side chain with Q¹ or Q², or if Q¹ and/or Q² is (are) mot present, with X and where at least one of radicals R¹ or R² must be always present, X is -CO-R¹⁸-CO- and if R¹-Q¹- or R²-Q² is not present, R¹⁰,R¹³,R¹⁶, residue of fluorescent dye which is bonded by means of CONH-, -COO-, -NH-C-(=S)-NH bonded or salicyloyl; in each case Z is independently residue of amino acid or di- or tri-peptide, amino acids are independently selected from group consisting Ala, Asn, Asp, Arg, Cys, Gln, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr, Val or M where said amino acids are derivatives and residues of amino acids bonded one with the other like peptide by means of alpha-amina and alpha-carboxy groups and where M is always present, M is NH(R⁸)CH(R³)COOH,R³-R⁵-R⁴,-R⁶-R⁴; R⁴ is OH, SH; R⁵ is alkylene having 1-6 carbon atoms; R⁶ is alkylene phenylene having 7-14 carbon atoms; R⁸ is H; R¹⁰ is alkanoyl which has 1-18 carbon atoms and is unsubstituted and has one substitute selected from group consisting of COOH, SR¹¹ or NR¹²R¹²; R¹¹ is H or trityl; R¹²,R¹², is each independently alkyl having 1-8 carbon atoms or protective group of amino group R¹³ is aroyl which has 7-11 carbon atoms and is unsubstituted and has one or two substitutes selected from group consisting of alkyl having 1-6 carbon atoms, R¹⁶ is aralcanoyl which has 7-19 carbon atoms and which is not substituted or substituted by one Hal substituent in aryl fragment; R¹⁸ is not present or is alkenyl having 1-8 carbon atoms; Hal is F, Cl, Br or I. New compounds are useful as integrine inhibitors, more particularly, for prophylaxis and treatment of diseases of blood circulation, thrombosis, cardiac infarct of coronary heart diseases, arteriosclerosis and diseases associated with development of vessels and also therapy of tumors. EFFECT: improved properties of title compounds. 6 cl