3-AMINOALKYL-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5 RECEPTOR ANTAGONISTS Russian patent published in 2014 - IPC C07D243/08 C07D401/04 C07D401/06 C07D401/12 C07D403/06 C07D403/12 C07D405/12 C07D409/12 A61K31/551 A61P3/04 A61P17/10 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to a compound of Formula

,

where Y represents a group of formula -(CR⁹R¹⁰)-; X is selected from the group, consisting of -C(=O)-, -OC(=O)-, -NHC(=O)-, -(CR¹¹R¹²)- and -S(-O)₂-; Z represents a group of formula -(CR¹³R¹⁴)_q-; R¹ is selected from the group, consisting of C₁-C₁₂alkyl, optionally substituted with one substituent, selected from naphthyl, indole and biphenyl; C₂-C₁₂alkenyl, substituted with a substituent, selected from thienyl, naphthyl and phenyl, with the said phenyl being optionally substituted with 1-2 substituents; selected from halogen, trifluoroalkyl, C₁-C₆alkyl, methoxy and hydroxy; C₃-C₆cycloalkyl; C₆-C₁₀aryl, optionally substituted with 1-2 substituents, selected from halogen, phenyl, amino, phenoxy, C₁-C₆alkyl, methoxy, hydroxyl and carboxy; and C₄-C₉heteroaryl, selected from indole, quinoline, quinoxaline, benzofuranyl, benzothiophene, benzimidazole, benzotriazole, benzodioxin, benzothiasole, pyrazole, furyl and isoxazole, optionally substituted with a substituent, selected from C₁-C₆alkyl and phenyl; R² and R³ each is independently selected from the group, consisting of H and C₁-C₁₂alkyl; R^4a is selected from the group, consisting of H, C₁-C₁₂alkyl, optionally substituted with phenyl; C₂-C₁₂alkenyl, C₃-C₆cycloalkyl, C₆aryl, C(=O)R¹⁵, C(=O)NR¹⁵R¹⁶, C(=O)OR¹⁵, SO₂R¹⁵ and -C(=NR¹⁵)-NR¹⁶R¹⁷; R^4d represents hydrogen or R^4a and R^4b, taken together with a nitrogen atom, which they are bound to, form an optionally substituted heterocyclic fragment, selected from piperidine, morpholine, pyrrolidine and azetidine, where the substituent is selected from C₁-C₁₂alkyl, hydroxy, halogen, carboxy and oxo; each R^5a and R^5b represents H, or R⁶, R⁷ and R⁸ each is independently selected from the group, consisting of H, C₁-C₁₂alkyl, C₃-C₆cycloalkyl, C₆-C₁₀aryl, optionally substituted with halogen, or taken together with a carbon atom, which they are bound to, two or more of R⁶, R⁷ and R⁸ form a fragment, selected from the group, consisting of C₂-C₁₂alkenyl; C₃-C₆cycloalkyl, optionally substituted with C₁-C₆alkyl; C₆aryl, optionally substituted with 2 substituents, selected from halogen; each R⁹ and R¹⁰ represents H or C₁-C₁₂alkyl, substituted with naphthyl; each R¹¹ and R¹² represents H; R¹³ and R¹⁴ represent H, or each R¹⁵, R¹⁶ and R¹⁷ is independently selected from the group, consisting of H, C₁-C₁₂alkyl, C₃-C₆cycloalkyl, C₆aryl, substituted with one substituent, selected from C₁-C₆alkyl; and C₅-heteroaryl, additionally containing one nitrogen atom, with the said heteroaryl representing pyridyl; q represents an integer number, selected from the group, consisting of 2, 3 and 4; r represents 1; or its pharmaceutically acceptable salt. The invention also relates to particular compounds of 1,4-diazepan-2-one derivatives.

EFFECT: obtaining 3-aminoalkyl-1,4-diazepan-2-one melanocortin-5 receptor antagonists.

21 cl, 7 tbl, 110 ex