LIGANDS FOR MELANOCORTIN RECEPTORS Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine.

SUBSTANCE: invention represents ligands MC-4 and/or MC-3 of the formula (I): , wherein X means hydrogen atom, -OR¹, -NR¹R^1' and -CHR¹R^1' wherein R¹ and R^1' are taken among the group: hydrogen atom, (C₁-C₆)-alkyl and acyl; (1) each R² is taken independently among the group: hydrogen atom, (C₁-C₆)-alkyl; or (2) (a) R² bound with carbon atom that is bound with X and Z¹ and substitute R⁵ can be optionally bound to form carbocyclic or heterocyclic ring that is condensed with phenyl ring J; or (b) R² bound with carbon atom that is bound with ring Ar can be bound with R⁷ to form ring condensed with ring Ar; each among Z¹, Z² and Z³ is taken independently from the following groups: -N(R^3e)C(R³)(R^3a)-, -C(R³)(R^3a)N(R^3e)-, -C(O)N(R^3d)-, -N(R^3d)C(O)-, -C(R³)(R^3a)C(R^3b)(R^3c)-, -SO₂N(R^3d)- and -N(R^3d)SO₂- wherein each among R³, R^3a, R^3b and R^3c, R^3d, R^3e when presents is taken independently among hydrogen atom and (C₁-C₆)-alkyl; p is a whole number from 0 to 5 wherein when p above 0 then R⁴ and R^4' are taken among hydrogen atom, (C₁-C₆)-alkyl and aryl; R⁵ represents 5 substitutes in phenyl ring J wherein each R⁵ is taken among hydrogen atom, hydroxy-, halogen atom, thiol, -OR¹², -N(R¹²)(R^12'), (C₁-C₆)-alkyl, nitro-, aryl wherein R¹² and R^12' are taken among hydrogen atom and (C₁-C₆)-alkyl; or two substitutes R⁵ can be bound optionally to form carbocyclic or heterocyclic ring that is condensed with phenyl ring J; q = 0, 1, 2, 3, 4 or 5 wherein when q above 0 then R⁶ and R^6' are taken among hydrogen atom and (C₁-C₆)-alkyl; Ar is taken among the group consisting of phenyl, thiophene, furan, oxazole, thiazole, pyrrole and pyridine; R⁷ are substitutes at ring Ar wherein each R⁷ is taken among hydrogen, halogen atom, -NR¹³R^13', (C₁-C₆)-alkyl and nitro- wherein R¹³ and R^13' are taken among hydrogen atom and (C₁-C₆)-alkyl; r is a whole number from 0 to 7 wherein when r is above 0 then R⁸ and R^8' are taken among hydrogen atom and (C₁-C₆)-alkyl; B is taken among -N(R¹⁴)C(=NR¹⁵)NR¹⁶R¹⁷, -NR²⁰R²¹, heteroaryl ring and heterocycloalkyl ring wherein R¹⁴-R¹⁷, R²⁰ and R²¹ are taken independently among hydrogen atom and (C₁-C₆)-alkyl; s = 0, 1, 2, 3, 4 or 5 wherein when s is above 0 then R and R^9' are taken among hydrogen atom and (C₁-C₆)-alkyl; R¹⁰ is taken among the group consisting of optionally substituted bicyclic aryl ring and optionally substituted bicyclic heteroaryl ring; D is taken among hydrogen atom, amino- and -C(O)R¹¹ wherein R¹¹ is taken among the following group: hydroxy-, alkoxy-, amino-, alkylamino-, -N(R¹⁹)CH₂C(O)NH₂ wherein R¹⁹ represents (C₁-C₆)-alkyl, -NHCH₂CH₂OH and -N(CH₃)CH₂CH₂OH, or its isomers, salts, hydrates or biohydrolysable ester, amide or imide.

EFFECT: valuable medicinal properties of compounds.

18 cl, 107 ex