公开(公告)号：US11851406B2

公开(公告)日：2023-12-26

申请号：US17251649

申请日：2019-06-13

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Julie L. Engers ,  Aaron M. Bender ,  Madeline Long

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/14

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D413/14

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：US11376254B2

公开(公告)日：2022-07-05

申请号：US16769684

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 ,  A61K45/06 ,  C07D495/14 ,  C07D519/00 ,  A61P25/00

Abstract: Disclosed herein are tricyclic compounds, including 3-(difluoromethyl)-4-methylpyrimido[4′,5′: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：US11352344B2

公开(公告)日：2022-06-07

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: C07D401/14 ,  C07D403/14 ,  C07D405/14

Abstract: Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds of formula (Ia), 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：US11225484B2

公开(公告)日：2022-01-18

申请号：US16636887

申请日：2018-08-08

Applicant: Vanderbilt University

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

IPC: A61K31/407 ,  C07D403/04 ,  C07D487/04

Abstract: Disclosed herein are octahydropyrrolo[3,4-b]pyrrole compounds of formula (I), 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：US20210355114A1

公开(公告)日：2021-11-18

申请号：US17287442

申请日：2019-10-24

Applicant: Vanderbilt University

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

IPC: C07D405/14 ,  C07D405/10 ,  C07D413/14 ,  C07D413/10

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：US11149022B2

公开(公告)日：2021-10-19

申请号：US16756430

申请日：2018-10-17

Applicant: Vanderbilt University

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

IPC: C07D401/14 ,  C07D401/12 ,  C07D409/14 ,  C07D405/14

Abstract: Disclosed herein are substituted 7-azaspiro[3.5]nonane 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：US20210261526A1

公开(公告)日：2021-08-26

申请号：US17251649

申请日：2019-06-13

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Julie L. Engers ,  Aaron M. Bender ,  Madeline Long

IPC: C07D401/14 ,  C07D405/14 ,  C07D413/14

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：US20210188811A1

公开(公告)日：2021-06-24

申请号：US16756430

申请日：2018-10-17

Applicant: Vanderbilt University

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

IPC: C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14

Abstract: Disclosed herein are substituted 7-azaspiro[3.5]nonane 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：US20200181166A1

公开(公告)日：2020-06-11

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：US10526323B2

公开(公告)日：2020-01-07

申请号：US15547781

申请日：2016-02-01

Applicant: Vanderbilt University

Inventor： P. Jeffrey Conn ,  Corey R. Hopkins ,  Craig W. Lindsley ,  Colleen M. Niswender ,  Darren W. Engers ,  Joe Panarese ,  Joanne Bronson ,  Yong-Jin Wu ,  Jason Guernon

IPC: C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4162 ,  A61K45/06 ,  A61K31/416 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/5377 ,  C07D231/56 ,  C07D519/00 ,  C07D413/14

Abstract: Compounds, including those of the following formula: wherein the variables are defined herein, which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.