您的位置: 首页 > 农业专利 > 详情页

BISARYL (THIO)MORPHOLINE DERIVATIVES AS S1P MODULATORS
专利权人:
ABBOTT HEALTHCARE PRODUCTS B.V.
发明人:
IWEMA BAKKER, Wouter I.,BRONGER, Raymond
申请号:
EPEP2011/061590
公开号:
WO2012/004375A1
申请日:
2011.07.08
申请国别(地区):
WO
年份:
2012
代理人:
摘要:
The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I) wherein R1 is an aryl substitutent selected from phenyl, pyridyl, pyrimidinyl, biphenyl and naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, -SO2-(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl and -NH-CO-(1-4C)alkyl, or substituted with phenoxy, benzyl, benzyloxy, phenylethyl or morpholinyl, each optionally substituted with (1-4C)alkyl, and (8-10C)bicyclic group, bicyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms or oxo A is selected from -CO-, -NH-, -O-, -S-, -SO- or -SO2- ring structure B optionally contains one nitrogen atom R2 is H, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, or halogen and R3 is (1-4C)alkylene-R6 wherein the alkylene group may be substituted with (CH2)2 to form a cyclopropyl moiety or with one or more halogen atoms, or R3 is (3-6C)cycloalkylene-R5 or -CO-CH2-R6, wherein R6 is -OH, -PO3H2, -OPO3H2, -COOH, -COO(1-4C)alkyl or tetrazol-5-yl R4 is H or (1-4C)alkyl R5 is one or more substituents independently selected from H, (1-4C)alkyl or oxo W is -O-, -S-, -SO- or -SO2- or a pharmaceutically acceptable salt, a solvate or hydrate thereof, with the proviso that the derivative of formula (I) is not 2-[4-(4-chlorophenoxy)-2-chloro-phenyl]-4-morpholineethanol. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.La présente invention se rapporte à des dérivés bisaryl (thio)morpholines de formule (I) où R1 est un substituant aryle choisi parmi phényle, pyridyle, pyrimidinyle, biphén
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充