公开(公告)号：US11878972B2

公开(公告)日：2024-01-23

申请号：US17125012

申请日：2020-12-17

Applicant: TORQUR AG ,  UNIVERSITÄT BASEL

Inventor： Denise Rageot ,  Paul Hebeisen ,  Florent Beaufils ,  Doriano Fabbro ,  Petra Hillmann-Wüllner ,  Hoa Huu Phuc Nguyen ,  Wolfgang Löscher ,  Claudia Brandt ,  Alexander Markus Sele

IPC: C07D413/14 ,  A61P25/28 ,  A61P25/08 ,  C07D417/14 ,  C07D451/02 ,  C07D451/14 ,  C07D498/08 ,  C07D519/00 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/53

CPC classification number: C07D413/14 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61P25/08 ,  A61P25/28 ,  C07D417/14 ,  C07D451/02 ,  C07D451/14 ,  C07D498/08 ,  C07D519/00

Abstract: The present invention is relates to a compound of formula (I),






wherein
X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of
X1, 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); and
wherein 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 structures










wherein 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 R 7 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.