| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: claimed invention relates to a compound of Formula,where Y represents a group of formula -(CRR)-; X is selected from the group, consisting of -C(=O)-, -OC(=O)-, -NHC(=O)-, -(CRR)- and -S(-O)-; Z represents a group of formula -(CRR)-; Ris selected from the group, consisting of C-Calkyl, optionally substituted with one substituent, selected from naphthyl, indole and biphenyl; C-Calkenyl, 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, C-Calkyl, methoxy and hydroxy; C-Ccycloalkyl; C-Caryl, optionally substituted with 1-2 substituents, selected from halogen, phenyl, amino, phenoxy, C-Calkyl, methoxy, hydroxyl and carboxy; and C-Cheteroaryl, selected from indole, quinoline, quinoxaline, benzofuranyl, benzothiophene, benzimidazole, benzotriazole, benzodioxin, benzothiasole, pyrazole, furyl and isoxazole, optionally substituted with a substituent, selected from C-Calkyl and phenyl; Rand Reach is independently selected from the group, consisting of H and C-Calkyl; Ris selected from the group, consisting of H, C-Calkyl, optionally substituted with phenyl; C-Calkenyl, C-Ccycloalkyl, Caryl, C(=O)R, C(=O)NRR, C(=O)OR, SORand -C(=NR)-NRR; Rrepresents hydrogen or Rand R, 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 C-Calkyl, hydroxy, halogen, carboxy and oxo; each Rand Rrepresents H, or R, Rand Reach is independently selected from the group, consisting of H, C-Calkyl, C-Ccycloalkyl, C-Caryl, optionally substituted with halogen, or taken together with a carbon atom, which they are bound to, two or more of R, Rand Rform a fragment, selected from the group, consisting of C-Calkenyl; C-Ccycloalkyl, optionally substituted with C-Calkyl; Caryl, optionally substituted with 2 substituents, selected from halogen; each Rand Rrepresents H or C-Calkyl, substituted with naphthyl; each Rand Rrepresents H; Rand Rrepresent H, or each R, Rand Ris independently selected from the group, consisting of H, C-Calkyl, C-Ccycloalkyl, Caryl, substituted with one substituent, selected from C-Calkyl; and C-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 |
