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AGONISTS AND ANTAGONISTS OF S1P5-RECEPTORS AND WAYS OF THEIR APPLICATION
专利权人:
ЭББОТТ ЛЭБОРЕТРИЗ (US)
发明人:
ХАРРИС Кристофер М. (US),ХОБСОН Эдриан Д. (US),УИЛСОН Ноэль С. (US)
申请号:
RU2011137454/13
公开号:
RU2011137454A
申请日:
2010.02.10
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
1. The compound of formula (I) or a pharmaceutically acceptable salt, biologically active metabolite, solvate, hydrate, prodrug, enantiomer or stereoisomer thereof; wherein ring 1 is optionally substituted aryl or optionally substituted heteroaryl; L is —N (R) -, —O— or C (R), where R is independently H or optionally substituted alkyl; X is N when L is C (R); or X represents CR; when L is —N— or —O—; R and R independently represent a hydrogen atom, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyalkyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted, bridged cycloalkyl, optionally substituted heterocyclyl or - (CH) C (= W) R; where W represents O or S; and R is —OR, —N (R) or —SR; where R independently represents a hydrogen atom, optionally substituted alkyl or halogenated; or when X represents N or C, then R and R, taken together with the carbon or nitrogen atom to which they are bonded, form an optionally substituted cycloalkyl, optionally substituted azetidine, optionally substituted pyrrolidine, optionally substituted piperidine or optionally substituted octahydrocyclopenta [c] pyrrolyl ring, provided that the azetidine ring formed by R and R, taken together with the carbon or nitrogen atom to which they are bonded, is not substituted with one or more phenyl; phenyl and OH; phenyl and —N (H) C (CH); —CH — O -not byazatelno substituted pyridinyl; -NH-optionally substituted hinazolinilom; -O-optionally substituted pyridinyl; -O-Si (CH) -C (CH); - C (OH) (4- (trifluoromethoxy) phenyl) (4-1. Соединение формулы (I)или его фармацевтически приемлемая соль, биологически активный метаболит, сольват, гидрат, пролекарство, энантиомер или стереоизомер; в которомкольцо 1 представляет необязательно замещенный арил или необязательно замещенный гетероарил;L представляет -N(R)-, -O- или C(R), гдеRнезависимо представляет Н или необязательно замещенный алкил;Х представляет N, когда L является
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