SELECTIVE CYCLOPEPTIDES Russian patent published in 2004 - IPC

FIELD: organic chemistry, peptides.

SUBSTANCE: invention describes compounds of the formula (1)

wherein R¹ and R¹² in common with X and Y form phenyl ring; X means carbon atom (C); Y means carbon atoms (C); or R¹ means hydrogen atom or group of the formula indicated in cl. 1; R¹² means hydrogen atom being each among X and Y means carbon atom (C) and a bind between X and Y is a double bind; either each among X and Y means CH and a bind between X and Y is an ordinary bind; R² means alkyl comprising from 1 to 5 carbon atoms, alkenyl comprising from 2 to 5 carbon atoms, or alkynyl comprising from 2 to 5 carbon atoms; R¹⁴ means alkyl comprising from 1 to 5 carbon atoms; n = 0 or 1; Q means group of the formula indicated in cl. 1 wherein each among R³, R⁴ and R⁵ means independently hydrogen, halogen atom, alkyl comprising from 1 to 4 carbon atoms, hydroxy-group or alkoxy-radical comprising from 1 to 4 carbon atoms being when R⁴ doesn't means hydrogen atom then both R³ and R⁵ mean hydrogen atom; R⁶ means hydrogen atom, alkyl comprising from 1 to 3 carbon atoms, alkoxy-radical comprising from 1 to 3 carbon atoms, phenoxy-group or halogen atom; each among R¹¹ and R¹³ means independently hydrogen atom, alkyl comprising 3 or 4 carbon atoms, cycloalkyl comprising 5 or 6 carbon atoms, or both R¹¹ and R¹³ mean phenyl; R⁷ means oxygen atom (O) or NH; R⁸ means hydrogen atom or methyl group; R⁹ means group of the formula indicated in cl. 1; R¹⁰ means hydrogen atom or methyl group; p = 0 or 1; m = 0, 1, 2 or 3; Z means group of the formula indicated in cl. 1; R¹⁷ means hydrogen atom or (lower)-alkyl, and their pharmaceutically acceptable salts. Compounds are selective agonists with respect to melanocortin-4. Also, invention describes a method for preparing these compounds and pharmaceutical composition comprising thereof.

EFFECT: valuable medicinal properties of compounds.

47 cl, 1 tbl, 83 ex