SUBSTITUTED β-ALANINES Russian patent published in 2004 - IPC

FIELD: organic chemistry, amino acids, pharmacy. SUBSTANCE: invention relates to compounds of the general formula (I): β 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; C_1-6 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