New thiazol-2-yl-morpholine compounds are akt phosphorylation inhibitors useful for treating glioblastomas, thyroid cancer, bladder cancer, breast cancer, melanoma, sarcomas, cancer of bone and pancreas, and hamartomas
CARRY JEAN CHRISTOPHE,JEAN CHRISTOPHE CARRY,CERTAL VICTOR,VICTOR CERTAL,HALLEY FRANK,FRANK HALLEY,KARLSSON KARL ANDREAS,KARL ANDREAS KARLSSON,SCHIO LAURENT,LAURENT SCHIO
申请号：
FR1061304
公开号：
FR2969611A1
申请日:
2010.12.28
申请国别(地区):
FR
年份:
2012
代理人:
摘要：
Thiazol-2-yl-morpholine compounds (I) and their racemic forms, enantiomers, diastereoisomers, and addition salts with mineral and organic acids or bases are new. Thiazol-2-yl-morpholine compounds of formula (I) and their racemic forms, enantiomers, diastereoisomers, and addition salts with mineral and organic acids or bases are new. R1a, R1b : H, halo or alkyl (optionally substituted by one or more halo atoms)； R1c : NH 2, OH, or alkoxy； R1 : aryl or heteroaryl (both optionally substituted by halo, OH, CN, nitro, -COOH, -COOalk, -NR1xR1y, -CONR1xR1y, NR1xCOR1y-, -COR1y, NR1xCO 2R1z, alkoxy, phenoxy, alkylthio, alkyl, alkenyl, alkynyl, cycloalkyl, O-cycloalkyl, heterocycloalkyl, aryl or heteroaryl), where heterocycloalkyl and heteroaryl optionally contain one or more oxo, and the alkoxy, phenoxy, alkylthio, alkyl, alkenyl, alkynyl, heterocycloalkyl, cycloalkyl, aryl or heteroaryl are optionally substituted by halo, OH, alkoxy or NR1vR1w, and the aryl and heteroaryl are optionally substituted alkyl or alkoxy optionally substituted by halo； either R : H； or RR1 : optionally and partially saturated 5 or 6-membered aryl or heteroaryl ring (optionally containing one or more other heteroatoms comprising O, S, N, NH or Nalk), or bicyclic radical (optionally substituted by halo, OH, alkyl, or alkoxy), (hetero)aryl or NR1xR1y, where the alkyl, alkoxy, aryl and heteroaryl are optionally substituted by halo, OH, oxo, alkyl, heterocycloalkyl, alkoxy, NR1vR1w or SO 2Alk； or two substituents on the same carbon atom of the ring formed by R with R1 may form together with the carbon atom (CRR1) : a 3-10-membered cyclic group (spirocycloalkyl) optionally containing one or more heteroatoms (preferably spiroheterocycloalkyl) of O, S, or NH, where the cyclic group is optionally substituted by one or more halo, alkyl, hydroxyl, oxo, alkoxy, NH 2, NHalk or N(alk) 2； or two adjacent substituents of the ring formed by R with R1 may optionally form, together with the carbon atoms to which the
