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SPIROCYCLIC AMINE DERIVATIVES AS S1P MODULATORS
专利权人:
EBBVI B.V.
发明人:
STOJT Aksel (NL),СТОЙТ Аксел (NL),IVEMA BAKKER Vauter I. (NL),ИВЕМА БАККЕР Ваутер И. (NL),KOLEN KHejn K.A.S. (NL),КОЛЕН Хейн К.А.С. (NL),VAN DONGEN Maria J.P. (NL),ВАН ДОНГЕН Мариа Й.П. (NL),LEFLEMME,STOJT Aksel,СТОЙТ Аксел,IVEMA BAKKER Vauter I.,ИВЕМА БАККЕР Ваутер И.,KOLEN KHejn K.A.S.,КОЛЕН Хейн К.А.С.,VAN DONGEN Maria J.P.,ВАН ДОНГЕН Мариа Й.П.,LEFLEMME Nikolas J.-L.D.,ЛЕФЛЕММЕ Николас Й.-Л.Д.
申请号:
RU2013105490/04
公开号:
RU0002602800C2
申请日:
2011.07.08
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
FIELD: pharmaceutics.SUBSTANCE: invention relates to spirocyclic amine derivatives of formula (I), where R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl, each of which is optionally substituted with CN or one or more fluorine atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or (8-10C)bicyclic group, where each of said groups is optionally substituted with halogen or (1-4C)alkyl, phenyl, optionally substituted with one or more substitutes, independently selected from halogen, (1-6C)alkyl, optionally substituted with one or more fluorine atoms, (1-6C)alkoxy, optionally substituted with one or more fluorine atoms, and (3-6C)cycloalkyl, optionally substituted with phenyl; biphenyl, optionally substituted with halogen; naphthyl; phenyl, substituted with monocyclic heterocycle; Monocyclic heterocycle, optionally independently substituted with halogen, (1-6C)alkyl, optionally substituted with one or more fluorine atoms, (3-6C)cycloalkyl or phenyl, optionally substituted (1-4C)alkyl or halogen, and bicyclic heterocycle, optionally substituted with halogen or (1-4C)alkyl, optionally substituted with one or more fluorine atoms; -Y-(Cn-alkylene)-X- is a binding group, where Y is bonded to R1 and is selected from a bond, -O-, -CO-, -S-, -SO-, -SO2-, -CH=CH-, -C(CF3)=CH-, -C≡C-, -CH2-O-, -CO-NH-, -NH-CO- and trans-cyclopropylene; n is an integer between 0 and 10; and X is bonded to a phenylene group and is selected from a bond -O-, -S-, -SO-, -SO2-, -NH-, -CO-, -CH=CH- and trans-cyclopropylene; R2 is H or is independently selected from one or more substitutes selected from halogen, (1-4C)alkyl, optionally substituted with one or more fluorine atoms; R3 is (1-4C)alkylene-R4, where alkylene group can be substituted with one or more halogen atoms or (CH2)2 to form by a cyclopropyl group, or R3 is (3-6C)cycloalkylene-R4, or -CO-CH2-R4, where R4 is -OH, -PO3H2, -OPO3H2, -COOH, -COO(1-4C)alkyl or tetrazol-5-yl; Q is a bond; -W-T- is selected from -CH=CH-, -CH2-CH2-, -C
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