公开(公告)号：US20230183218A1

公开(公告)日：2023-06-15

申请号：US17920899

申请日：2021-04-23

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Aaron M. Bender ,  Changho Han

IPC: C07D405/14 ,  C07D403/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04

CPC classification number: C07D405/14 ,  C07D403/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04

Abstract: Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds, which may be useful as antagonists 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 disorders using the compounds and compositions.

公开(公告)号：US11142532B2

公开(公告)日：2021-10-12

申请号：US16261108

申请日：2019-01-29

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Sean Bollinger ,  James C. Tarr ,  Paul Spearing ,  Julie L. Engers ,  Madeline Long ,  Thomas M. Bridges

IPC: C07D495/14 ,  C07D493/14 ,  C07D519/00

Abstract: Disclosed herein are tricyclic compounds, including pyrimido[4′,5′:4,5]thieno[2,3-c]pyridazine-8-amine, pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine-4-amine, pyrazino[2′,3′:4,5]thieno[3,2-d]pyrimidin-4-amine, pyrido[3′,2′:4,5]furo[3,2-d]pyrimidin-4-amine, and pyrimido[4′,5′:4,5]furo[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：US11008335B2

公开(公告)日：2021-05-18

申请号：US16347446

申请日：2017-11-07

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  Darren W. Engers ,  P. Jeffrey Conn ,  Sean R. Bollinger ,  Julie L. Engers

IPC: C07D495/14

Abstract: Disclosed herein are pyrido[3′,2′:4,5]thieno[2,3-d]pyridazin-8-amine and thieno[2,3-c:4,5-d′]dipyridazin-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：US20210130348A1

公开(公告)日：2021-05-06

申请号：US17122694

申请日：2020-12-15

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Katrina A. Bollinger ,  Darren W. Engers ,  Anna L. Blobaum ,  Julie L. Engers ,  Jerri M. Rook

IPC: C07D471/04 ,  C07D495/04

Abstract: Described are 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：US10927126B2

公开(公告)日：2021-02-23

申请号：US16347457

申请日：2017-11-07

Applicant: Vanderbilt University

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

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

Abstract: 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：US20200339547A1

公开(公告)日：2020-10-29

申请号：US16760010

申请日：2018-10-31

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Kayla J. Temple

IPC: C07D403/14 ,  C07D405/14

Abstract: Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds, which may be useful as antagonists 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 disorders using the compounds and compositions.

公开(公告)号：US10745400B2

公开(公告)日：2020-08-18

申请号：US16353745

申请日：2019-03-14

Applicant: Vanderbilt University

Inventor： Corey R. Hopkins ,  Matthew Ritter ,  Charles C. Hong ,  Anish Vadukoot ,  Darren W. Engers ,  Craig W. Lindsley

IPC: C07D471/10 ,  A61K31/438 ,  C07D471/04 ,  A61P35/00

Abstract: Provided herein are substituted imidazo[1,2-a]pyridines useful as inhibitors of BMP signaling. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted imidazo[1,2-a]pyridines.

公开(公告)号：US20190330225A1

公开(公告)日：2019-10-31

申请号：US16347450

申请日：2017-11-07

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  Darren W. Engers ,  P. Jeffrey Conn ,  Katrina A. Bollinger ,  Rory Capstick ,  Paul Spearing ,  Sean R. Bollinger

IPC: C07D495/04

Abstract: Disclosed herein are pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine and pyrimido[4′,5′:4,5]thieno[2,3-c]pyridazine compounds, which may be useful as positive allostenc 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：US20190167688A1

公开(公告)日：2019-06-06

申请号：US16210495

申请日：2018-12-05

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Julie L. Engers

IPC: A61K31/519 ,  A61P25/28

Abstract: Disclosed herein are tricyclic compounds, including thieno[2,3-d:4,5-d′]dipyrimidin-4-amine and pyrido[4′,3′:4,5]thieno[2,3-d]pyrimidin-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：US10239887B2

公开(公告)日：2019-03-26

申请号：US15630200

申请日：2017-06-22

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Sean Bollinger ,  James C. Tarr ,  Paul Spearing ,  Julie L. Engers ,  Madeline Long ,  Thomas M. Bridges

IPC: C07D491/14 ,  C07D495/14 ,  C07D493/14 ,  C07D519/00

Abstract: Disclosed herein are tricyclic compounds, including pyrimido[4′,5′:4,5]thieno[2,3-c]pyridazine-8-amine, pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine-4-amine, pyrazino[2′,3′:4,5]thieno[3,2-d]pyrimidin-4-amine, pyrido[3′,2′:4,5]furo[3,2-d]pyrimidin-4-amine, and pyrimido[4′,5′:4,5]furo[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.