| 摘要 |
FIELD: organic chemistry, amino acids, pharmacy. SUBSTANCE: invention relates to compounds of the general formula (I): beta wherein is hydrogen atom or lower alkyl; R1 represent independently X1, X2, X6 being one among CR3 represents CR2 and other represent independently X3, X4, X5 wherein CR2 is hydrogen atom, lower alkyl or lower alkoxy-group; R2 represents group R3 wherein -L1-(CH2)n-C(=O)-NR4-CH2-CH2- is aryl or heteroaryl; or R4 is alkyl or alkenyl being each is optionally substituted with one or more groups taken among halogen atom, oxo-group, R4 or NH-R5; or C(=O)R7 is cycloalkyl or heterocyclo- alkyl being each is optionally substituted with one or more groups taken among oxo-group, R4 or R6; -L2-R6; is carboxy-group. Aryl. cycloalkyl, heteroaryl, heterocycloalkyl, R5 or -ZR7; -NY1Y2 is aryl or heterocycloalkyl; R6 is alkyl or aryl; R7 is alkylene; L2 and Y1 are independently hydrogen atom, alkyl or aryl; or group Y2 can form 5-7-membered cyclic amine that: (i) can be optionally substituted with one or more substituent taken among oxo-group or alkyl; and (ii) can comprise also oxygen as additional heteroatom; Z represents oxygen atom; -NY1Y2 represents L1-bond wherein R9-R10 means direct or branched R9-alkylene chain; C1-6 is R10; -C(=Z)-NR11- represents hydrogen atom or R11; Y represents carboxy-group; n is a whole number from 1 to 6; and to its prodrugs and pharmaceutically acceptable salts, solvates of such compounds and their prodrugs. Also, invention relates to compounds of the formula (Ia) wherein one among R4 or X4 means the group: C-X5-Y; -R9-CON(R11)-CH2-CON(R4)-CH2-CH2- and X1 mean X2; CR2 and X3 mean CH; another group X6 or X4 is CH; pharmaceutical composition showing ability to regulate interaction of VCAM-1 and fibronectin with integrin VLA-4 (X5); to method for treatment of humans or animals suffering or predisposed to such diseases that can be treated by administration of the cellular adhesion inhibitor. EFFECT: valuable biological and medicinal properties of compounds. 30 cl, 16 tbl |
