| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: invention relates to new compounds of formula , in which: Ra and Ra' denote hydrogen, R1 denotes cycloalkyl; R2 denotes a group of formula -(CH2)x-(CO)y-Y or -(CO)y-(CH2)x-Y, in which x=0, y=1, Y denotes -N-R11R12;- R11 and R12 denote alkyl; R3 denotes a halogen atom; R5 denotes a hydrogen atom; R4 is selected from: (1) a group of formula : in which each of the rings in formulae (a) and (b) can be substituted in any position with 1-4 R7 groups which are identical or different from each other, and in which: a=0; p=0, 1, 2 or 3; m=1; X is an oxygen or sulphur atom or a C(R6)(R7)- or -N(R10)- group; R6 is selected from: a hydrogen atom; a -(CH2)x-NR8R9 group in which x=0, aryl, alkylaryl; R7 is selected from hydrogen atoms; aryl, alkylaryl groups; -OR group; -NRR' groups; R8 and R9 are selected from a hydrogen atom; R10 is selected from: hydrogen atom; aryl, alkylaryl; R and R' denote a hydrogen atom; (2) a group of formula -A-R18, -A-CH=N-R19, in which A denotes a straight or branched alkyl; R18 denotes a halogen atom or a -NH2 group; R19 denotes hydroxyl; (3) a group of formula : in which r equals 1; s equals 1, and one of U, V and W denotes a nitrogen atom while the others denote a methylene group; or (4) -(CH2)r-heteroaryl, where r equals 1; where the heteroaryl denotes a 5-6-member aromatic group containing 1-2 heteroatoms such as nitrogen, oxygen, in form of a base or additive acid salt. The invention also relates to a method for synthesis of formula (I) compounds, to compounds of formulae (IV) and (V), to a medicinal agent, to a pharmaceutical composition, as well as to use of formula (I) compounds. ^ EFFECT: obtaining new biologically active compounds having melanocortin receptor agonist activity. ^ 11 cl, 28 ex, 1 tbl |
