Denise RAGEOT,Paul HEBEISEN,Florent BEAUFILS,Doriano FABBRO,Petra HILLMANN-WÜLLNER,Hoa Huu Phuc NGUYEN,Wolfgang LÖSCHER,Claudia BRANDT,Alexander Markus SELE
申请号:
US16301729
公开号:
US20190284178A1
申请日:
2017.05.17
申请国别(地区):
US
年份:
2019
代理人:
摘要:
The present invention is relates to a compound of formula (I),whereinX1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two ofX1, X2 and X3 are N;Y is N or CH;R1 and R2 are independently of each other (iii) a morpholinyl of formula (II)wherein the arrow denotes the bond in formula (I); andwherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—;C1-C2alkyl; or R3 and R4 form together a bivalent residue —;R5R6—; selected from C1-C3alkylene optionally substituted with 1 to 4 F, —;CH2—;O—;CH2—;, —;CH2—;NH—;CH2—;, or any of the structureswherein the arrows denote the bonds in formula (II); or(iv) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxyC1-C3alkyl, C3-C6cycloalkyl; or two R7 substituents form together a bivalent residue —;R8R9—; selected from C1-C3alkylene optionally substituted with 1 to 4 F, —;CH2—;O—;CH2—; or —;O—;CH2CH2—;O—;;with the proviso that at least one of R1 and R2 is a morpholinyl of formula II;and prodrugs, metabolites, tautomers, solvates and pharmaceutically acceptable salts thereof, for use in the prevention or treatment of a neurological disorder in a subject.