公开(公告)号：US20240343718A1

公开(公告)日：2024-10-17

申请号：US18526732

申请日：2023-12-01

申请人： TORQUR AG ,  UNIVERSITÄT BASEL

发明人： Denise RAGEOT ,  Paul HEBEISEN ,  Florent BEAUFILS ,  Doriano FABBRO ,  Petra HILLMAN-WULLNER ,  Hoa Huu Phuc NGUYEN ,  Wolfgang LOSCHER ,  Claudia BRANDT ,  Alexander Markus SELE

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

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

摘要： 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 X1X2 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-C2fhioroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(0)0-C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6- selected from Ci-C3alkylene optionally substituted with 1 to 4 F, —CH2-0-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 Ci-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxyC1-C3 alkyl, C3-C6cycloalkyl; or two R7 substituents form together a bivalent residue —R8R9— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2-0-CH2— or —O—CH2CH2-0-; 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.

公开(公告)号：US20190284178A1

公开(公告)日：2019-09-19

申请号：US16301729

申请日：2017-05-17

申请人： PIQUR THERAPEUTICS AG ,  UNIVERSITÄT BASEL

发明人： Denise RAGEOT ,  Paul HEBEISEN ,  Florent BEAUFILS ,  Doriano FABBRO ,  Petra HILLMANN-WÜLLNER ,  Hoa Huu Phuc NGUYEN ,  Wolfgang LÖSCHER ,  Claudia BRANDT ,  Alexander Markus SELE

IPC分类号： C07D413/14 ,  C07D451/02 ,  C07D417/14 ,  C07D451/14 ,  C07D498/08 ,  C07D519/00 ,  A61P25/08 ,  A61P25/28

摘要： 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 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.

公开(公告)号：US20220135551A1

公开(公告)日：2022-05-05

申请号：US17125012

申请日：2020-12-17

申请人： PIQUR THERAPEUTICS AG ,  UNIVERSITÄT BASEL

发明人： Denise RAGEOT ,  Paul HEBEISEN ,  Florent BEAUFILS ,  Doriano FABBRO ,  Petra HILLMANN-WÜLLNER ,  Hoa Huu Phuc NGUYEN ,  Wolfgang LÖSCHER ,  Claudia BRANDT ,  Alexander Markus SELE

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

摘要： 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 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.