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作為S1P調節劑的螺-哌啶衍生物
专利权人:
ABBOTT HEALTHCARE PRODUCTS 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.,巴克尔 伍特 伊威玛,巴克爾 伍特 伊威瑪,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,史托伊特 亚克塞尔,史托伊特 亞克塞爾,巴克尔 伍特 伊威玛,巴克爾 伍特 伊威瑪,库兰 汉因,庫蘭 漢因,多根 玛丽亚,多根 瑪麗亞,雷夫乐 尼可拉斯,雷夫樂 尼可拉斯
申请号:
TW100124108
公开号:
TW201211051A
申请日:
2011.07.07
申请国别(地区):
TW
年份:
2012
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 R1and 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)2 to form a cyclopropyl moiety, or
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