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作為S1P調節劑的螺-哌啶衍生物
专利权人:
ABBVIE INC.;ABBVIE B.V.
发明人:
STOIT,AXEL,史托伊特亚克塞尔,史托伊特亞克塞爾,IWEMA BAKKER,WOUTER I.,伊威玛‧巴克尔伍特,伊威瑪‧巴克爾伍特,COOLEN,HEIN K.A.C.,库兰汉因,庫蘭漢因,VAN DONGEN,MARIA J.P.,多根玛丽亚,多根瑪麗亞,LEFLEMME,NICOLAS J.-L.D.,雷夫乐尼可拉斯,雷夫樂尼可拉斯,HOBSON,ADRIAN,霍布森阿德里安,霍布
申请号:
TW105117687
公开号:
TW201643169A
申请日:
2011.07.07
申请国别(地区):
TW
年份:
2016
代理人:
摘要:
The present invention relates spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (3-6C)cycloalkyl, or phenyl optionally substituted with (1-4C)alkyl or halogen, and bicyclic heterocycle optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms; -Y-(Cn-alkylene)-X- is a linking group wherein Y is attached to R1 and selected from a bond, -0-, -CO-, -s -SO-,-SO2-, -NH-, -CH=CH-, -C(CF3)=CH-, -CEC-, -CH2-O-, -O-CO-, -CO-O-, -CO-NH, -NH-CO-, and trans-cyclopropylene; n is an integer from 0 to 10; and X is attached to the phenylene/pyridyl moiety and selected from a bond, -O-, -S-, -SO-, -SO2-, -NH-, -CO-, -CH=CH-, and trans-cyclopropylene; R2 is H or independently selected from one or more substituents selected from halogen, (1-4C)alkoxy and (1-4C)alkyl optionally substituted with one or more fluor atoms; and R3 is (1-4C)alkylene-R4 wherein the alkylene group may be substituted with one or more halogen atoms or with (CH2)2to form a cyclopropyl moiety, o
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