Hein K.A.C. Coolen;Eric Ronken;Jurjen Frankena;Harmen Mons;Elizabeth Van Der Kam;Wouter I. Iwema Bakker;Axel Stoit
发明人:
Wouter I. Iwema Bakker,Hein K.A.C. Coolen,Axel Stoit,Harmen Mons,Eric Ronken,Elizabeth Van Der Kam,Jurjen Frankena
申请号：
US13393497
公开号：
US20120220552A1
申请日:
2010.08.27
申请国别(地区):
US
年份:
2012
代理人:
摘要：
The present disclosure relates to (thio)morpholine derivatives of the formula (I)whereinR1 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)alkyl optionally 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, —SO2-(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,andbicyclic heterocycle optionally substituted with (1-4C)alkyl；A is selected from —CO—O—, —O—CO—, —NH—CO—, —CO—NH, —C═C—, —CCH3—O— and the linking group —Y—(CH2)n—X— wherein Y is attached to R1 and selected from a bond, —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； andX is attached to the phenylene/pyridyl group and selected from a bond, —O—, —S—, —SO—, —SO2—, —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； andR3 is (1-4C)alkylene-R5 wherein the alkylene group may be substituted with (CH2)2 to form a cyclopropyl moiety or one or two halogen atoms, or R3 is (3-6C)cycloalkylene-R5 or —CO—CH2—R5, wherein R5 is —OH, —PO3H2, —OPO3H2, —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
