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3-SUBSTITUTED-1,4-DIAZEPAN-2-ONE ANTAGONISTS OF MELANOCORTIN 5-RECEPTOR
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:
RU2010137033/04
公开号:
RU0002524245C2
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: invention relates to a compound of formula (I)where Y represents a group of formula -(CR9R10)n-; X represents -C(=O)-; Z represents a group of formula -(CR13R14)q-; R1 is selected from a group, consisting of (a) C2-C12alkenyl, substituted with 4-chlorophenyl; or (b) C6-C10aryl, optionally substituted with one or two halogen atoms; R2 and R3 represent H; R4 is selected from a group, consisting of H, C1-C12alkyl, optionally substituted with hydroxyl, methoxy or benzyloxy, C3-C12cycloalkyl, C6aryl, optionally substituted with an amino group or pyperidine, C-bound C1-C18heteroaryl, selected from pyridine and imidazole, C(=O)R15, C(=O)NR16R17 and ONR16C(=NR17)NR18R19; each R5a and R5b represents H, each R6, R7 and R8 is independently selected from a group, consisting of H, C1-C12alkyl and C6-C18aryl, each R9 and R10 represents H; each R13 and R14 represents H; R15 represents H, each R16, R17, R18, R19 and R20 is independently selected from a group, consisting of H, C1-C12alkyl, C3-C12cycloalkyl, C6aryl and pyridyl, or any two of R16, R17, taken together with atoms, to which they are bound, form a cyclic group, containing 5 carbon atoms, or n equals to 1; q represents an integer number, selected from a group, consisting of 1, 2, 3, 4 and 5; r equals to 1; or its pharmaceutically acceptable salt.EFFECT: invention relates to a pharmaceutical composition for treatment of MC5R-associated conditions, which contains a formula (I) compound and a pharmaceutically acceptable carrier, a diluent or a filling agent.23 cl, 6 tbl, 53 exИзобретение относится к соединению формулы (I), где Y представляет собой группу формулы -(CR9R10)n-; Х представляет собой -C(=O)-; Z представляет собой группу формулы -(CR13R14)q-; R1 выбран из группы, состоящей из (a) C2-C12алкенила, замещенного 4-хлорфенилом; или (b) C6-C10арила, необязательно замещенного одним или двумя атомами галогена; R2 и R3 представляют собой Н; R4 выбран из группы, состоящей из Н, C1-C
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