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3-AMINOALKYL-1,4-DIAZEPAN-2-ONE MELANOCORTIN-5 RECEPTOR ANTAGONISTS
专利权人:
MIMETIKA PTI LTD
发明人:
BLASKOVICh Mark Arnol'd Tomas (AU),БЛАСКОВИЧ Марк Арнольд Томас (AU),KEhSSIDI Piter Dzhozef (AU),КЭССИДИ Питер Джозеф (AU),BLASKOVICH MARK ARNOLD TOMAS,БЛАСКОВИЧ Марк Арнольд Томас,KEHSSIDI PITER DZHOZEF,КЭССИДИ Питер Джозеф
申请号:
RU2010137034/04
公开号:
RU0002530017C2
申请日:
2009.02.27
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
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; R4a 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; R4d represents hydrogen or R4a and R4b, 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 R5a and R5b 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 fragm
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