公开(公告)号：US20180179205A1

公开(公告)日：2018-06-28

申请号：US15902547

申请日：2018-02-22

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Michael R. Wood ,  Corey R. Hopkins ,  Bruce J. Melancon ,  Michael S. Poslusney ,  Darren W. Engers

IPC: C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07D275/06 ,  C07D417/10 ,  C07D403/10 ,  C07D401/10 ,  C07D401/14 ,  C07D405/10

CPC classification number: C07D471/04 ,  C07D275/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/10 ,  C07D417/10 ,  C07D487/04 ,  C07D519/00

Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for 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. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：US20170313701A1

公开(公告)日：2017-11-02

申请号：US15652100

申请日：2017-07-17

Applicant: Vanderbilt University

Inventor： Corey R. Hopkins ,  Charles C. Hong ,  Craig W. Lindsley ,  Darren W. Engers

IPC: C07D471/04 ,  A61K31/519 ,  A61K31/4709 ,  A61K31/5025 ,  C07D519/00 ,  C07D487/04

CPC classification number: C07D471/04 ,  A61K31/4709 ,  A61K31/5025 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.

公开(公告)号：US20250011320A1

公开(公告)日：2025-01-09

申请号：US18750829

申请日：2024-06-21

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  Darren W. Engers ,  Kayla J. Temple ,  Alison R. Gregro ,  Alexa E. Richardson ,  Madeline F. Long

IPC: C07D471/04 ,  A61K31/4545 ,  C07B59/00

Abstract: Deuterium-labeled 4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidines substituted with pyrrolo[3,4-b]pyridin-5-one, furo[3,4-b]pyridin-5(7H)-one, or [1,2,4]triazolo[4,3-a]pyrimidin-3(2H)-one are positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4) and may have use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

公开(公告)号：US12065433B2

公开(公告)日：2024-08-20

申请号：US17287442

申请日：2019-10-24

Applicant: Vanderbilt University

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

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

CPC classification number: C07D405/14 ,  C07D405/10 ,  C07D413/10 ,  C07D413/14 ,  C07B2200/05

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：US11820757B2

公开(公告)日：2023-11-21

申请号：US17688709

申请日：2022-03-07

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Julie L. Engers ,  Kayla J. Temple ,  Aaron M. Bender ,  Logan A. Baker

IPC: C07D403/14 ,  C07D209/52 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D493/08

CPC classification number: C07D403/14 ,  C07D209/52 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D493/08

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：US11111251B2

公开(公告)日：2021-09-07

申请号：US15998899

申请日：2017-02-16

Applicant: Vanderbilt University

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

IPC: C07D413/14 ,  C07D403/14 ,  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：US10934276B2

公开(公告)日：2021-03-02

申请号：US16469972

申请日：2017-12-15

Applicant: Vanderbilt University

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

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

Abstract: 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：US10899759B2

公开(公告)日：2021-01-26

申请号：US16337977

申请日：2017-08-16

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：US20200369666A1

公开(公告)日：2020-11-26

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: C07D487/04

Abstract: Disclosed herein are octahydropyrrolo[3,4-b]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：US20200369650A1

公开(公告)日：2020-11-26

申请号：US16966306

申请日：2019-02-01

Applicant: Vanderbilt University

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

IPC: C07D403/14 ,  C07D403/12 ,  C07D405/14

Abstract: Disclosed herein are 3-azabicyclo[3.1.0]hexan-6-amine 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.