公开(公告)号：US20240228489A1

公开(公告)日：2024-07-11

申请号：US18554867

申请日：2022-04-14

申请人： Vanderbilt University

发明人： Craig W. Lindsley ,  Darren W. Engers ,  Julie L. Engers ,  Changho Han ,  Alison R. Gregro ,  Madeline F. Long ,  Jinming Li ,  Joseph D. Bungard ,  Cayden J. Dodd

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  C07D519/00

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  C07D519/00

摘要： Described are deuterium-labeled 6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one and isoindolin-1-one positive allosteric modulators of muscarinic acetylcholine receptor M1(mAChR M1), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating neurological disorders, psychiatric disorders, or a combination thereof.

公开(公告)号：US10934276B2

公开(公告)日：2021-03-02

申请号：US16469972

申请日：2017-12-15

申请人： Vanderbilt University

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Julie L. Engers ,  Madeline F. Long

IPC分类号： C07D401/14 ,  A61P25/28 ,  C07D237/28 ,  C07D403/12 ,  C07D403/14

摘要： Disclosed herein are 2,4-dimethylquinoline-6-carboxamide compounds and 3,4-dimethylcinnoline-6-carboxamide compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4(mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

公开(公告)号：US20200079756A1

公开(公告)日：2020-03-12

申请号：US16469972

申请日：2017-12-15

申请人： Vanderbilt University

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Julie L. Engers ,  Madeline F. Long

IPC分类号： C07D401/14 ,  C07D237/28 ,  C07D403/14 ,  C07D403/12 ,  A61P25/28

摘要： Disclosed herein are 2,4-dimethylquinoline-6-carboxamide compounds and 3,4-dimethylcinnoline-6-carboxamide compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4(mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

公开(公告)号：US20230286991A1

公开(公告)日：2023-09-14

申请号：US18187868

申请日：2023-03-22

申请人： Vanderbilt University

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Alison R. Gregro ,  Kayla J. Temple ,  Madeline F. Long ,  Anna E. Ringuette ,  Logan A. Baker ,  Thomas Jensen

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Disclosed herein are analogues of 6-(4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidin-1-yl)-[1,2,4]triazolo[4,3-b]pyridazine, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

公开(公告)号：US10927126B2

公开(公告)日：2021-02-23

申请号：US16347457

申请日：2017-11-07

申请人： Vanderbilt University

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Alison R. Gregro ,  Kayla Temple ,  Paul K. Spearing ,  Madeline F. Long ,  Julie L. Engers

IPC分类号： C07D495/14 ,  A61K31/4375 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D519/00

摘要： Disclosed herein are thieno[2,3-b:5,4-c′]dipyridin-8-amine and pyrido[4′,3′:4,5]thieno[2,3-c]pyridazin-8-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

公开(公告)号：US11884676B2

公开(公告)日：2024-01-30

申请号：US18187868

申请日：2023-03-22

申请人： Vanderbilt University

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Alison R. Gregro ,  Kayla J. Temple ,  Madeline F. Long ,  Anna E. Ringuette ,  Logan A. Baker ,  Thomas Jensen

IPC分类号： A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04

摘要： Disclosed herein are analogues of 6-(4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidin-1 -yl)-[1,2,4]triazolo[4,3-b]pyridazine of formula (Ib), which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

公开(公告)号：US20230257381A1

公开(公告)日：2023-08-17

申请号：US18005301

申请日：2021-07-15

申请人： Vanderbilt University ,  H. LUNDBECK A/S

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Alison R. Gregro ,  Kayla J. Temple ,  Madeline F. Long ,  Anna E. Ringuette ,  Logan A. Baker ,  Thomas Jensen

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Disclosed herein are analogues of 6-(4-((2,3-dihydrobenzo[b] [1,4]dioxin-6-yl)oxy)piperidin-1-yl)-[1,2,4]triazolo[4,3-b]pyridazine, i.e. 7-(4-((phenyl or pyridin-3-yl)oxy)piperidin-1-yl)-4H-pyrimido[1,2-b]pyridazin-4-one derivatives of formula (I) which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

公开(公告)号：US20190330231A1

公开(公告)日：2019-10-31

申请号：US16347457

申请日：2017-11-07

申请人： Vanderbilt University

发明人： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Alison R. Gregro ,  Kayla Temple ,  Paul K. Spearing ,  Madeline F. Long ,  Julie L. Engers

IPC分类号： C07D495/14 ,  A61K45/06 ,  A61K31/5025 ,  A61K31/4375 ,  A61K31/5377 ,  A61K31/506 ,  C07D519/00

摘要： Disclosed herein are thieno[2,3-b:5,4-c′]dipyridin-8-amine and pyrido[4′,3′:4,5]thieno[2,3-c]pyridazin-8-amine compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.