IWEMA BAKKER, WOUTER I.,COOLEN, HEIN K.A.C.,MONS, HARMEN,STOIT, AXEL,RONKEN, ERIC,KAM VAN DER, ELIZABETH,FRANKENA, JURJEN,HOBSON, ADRIAN
申请号：
ES10745659
公开号：
ES2452550T3
申请日:
2010.08.27
申请国别(地区):
ES
年份:
2014
代理人:
摘要：
Derived from (thio) morpholine of formula (I) ** Formula ** where R1 is selected from cyano, (C2-4) alkynyl, (C1-4) alkyl, cycloalkyl (C3-6), cycloalkenyl (C4-6) , bicycloalkyl (C6-8), bicyclic group (C8-10), each optionally substituted with (C1-4) alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (C1 -4) optionally substituted with one or more fluorine atoms, (C2-4) alkynyl, (C1-4) alkoxy optionally substituted with one or more fluorine atoms, amino, dialkyl (C1-4) amino, -SO2-alkyl (C1-4), -CO-C1-4 alkyl, -CO-O-C1-4 alkyl, -NH-CO (C1-4) alkyl and cycloalkyl (C3-6), phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (C1-4) alkyl, monocyclic heterocycle optionally substituted with halogen, (C1-4) alkyl or with phenyl optionally substituted with (C1-4) alkyl, and heterocyclic the bicyclic optionally substituted with (C1-4) alkyl； A is selected from -CO-O-, -O-CO-, -NH-CO-, -CO-NH-, -C>； = C-, -CCH3-O- and the linking group Y- (CH2) n-X30 where Y is attached to R1 and is selected from a link, -O-, -S-, -SO-, -SO2-, -CH2-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 is selected from a bond, -O-, -S-, -SO-, -SO2-, -NH-, -CO-, -C>； = C- and -C≡ C-； the ring structure B optionally contains a nitrogen atom； R2 is H, (C1-4) alkyl optionally substituted with one or more fluorine atoms, (C1-4) alkoxy optionally substituted with one or more fluorine atoms, or halogen； and R3 is (C1-4) alkylene -R5 where the alkylene group may be substituted with (CH2) 2 to form a cyclopropyl moiety or one or two halogen atoms, or R3 is (C3-6) -R5 or -CO- cycloalkylene CH2-R5, where R5 is -OH, -PO3H2, -OPO3H2, -COOH, -COO (C1-4) alkyl or tetrazol-5-yl； R4 is H or (C1-4) alkyl； R6 is one or more substituents independently selected from
