Iwema Bakker, Wouter I.,Coolen, Hein K.A.C.,Mons, Harmen,Stoit, Axel,Ronken, Eric,Kam, Van der Elizabeth,Frankena, Jurjen
申请号：
AU2010288477
公开号：
AU2010288477A1
申请日:
2010.08.27
申请国别(地区):
AU
年份:
2012
代理人:
摘要：
The present invention relates to (thio)morpholine derivatives of the formula (I), wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyloptionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms,amino, di(1-4C)alkylamino, -SO-(1-4C)alkyl, -CO-(1-4C)alkyl, -CO-O-(1-4C)alkyl, -NH-CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl； A is selected from -CO-O-, -O-CO-, -NH-CO-, -CO-NH, -C=C-, -CCH-O- and the linking group –Y-(CH)-X- wherein Y is attached to R1 and selected from a bond, -O-, -S-, -SO-, -SO-, -CH-O-, -CO-, -O-CO-, -CO-O-, -CO-NH-, -NH-CO-, -C=C-and -C≡C-； n is an integer from 1 to 10； and X is attached to the phenylene / pyridyl group and selected from a bond, -O-, -S-, -SO-, -SO -, -NH, -CO-, -C=C-and -C≡C-； 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-R5 wherein the alkylene group may be substituted with (CH) to form a cyclopropyl moiety or one or two halogen atoms, or R3 is is (3-6C)cycloalkylene-R5 or -CO-CH-R5, wherein R5 is -OH, -POH, -OPOH, -COOH, -COO(1-4C)alkyl or tetrazol-5-yl； R4 is H or (1-4C)alkyl； R6 is one or more substituents independently selected from H, (1-4C)alkyl or oxo； W is -O-, -S-, -SO- or -SO-； o
