公开(公告)号：US20190161498A1

公开(公告)日：2019-05-30

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：US10196392B2

公开(公告)日：2019-02-05

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: A61K31/4709 ,  A61K31/5025 ,  A61K31/519 ,  C07D471/04 ,  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：US20180086776A1

公开(公告)日：2018-03-29

申请号：US15703451

申请日：2017-09-13

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Bruce J. Melancon ,  Alison R. Gregro

IPC: C07D495/14 ,  A61K31/5025 ,  A61K45/06 ,  C07B59/00

CPC classification number: C07D495/14 ,  A61K31/5025 ,  A61K45/06 ,  A61P25/00 ,  C07B59/002 ,  C07B2200/05

Abstract: Disclosed herein are substituted 8-aminothieno[3,2-e][1,2,4]triazolo[4,3-b]pyridazine-7-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：US20180022746A1

公开(公告)日：2018-01-25

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: C07D471/04 ,  C07D519/00 ,  C07D413/14 ,  C07D487/04 ,  C07D403/12

Abstract: Compounds 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.

公开(公告)号：US20250122199A1

公开(公告)日：2025-04-17

申请号：US19002103

申请日：2024-12-26

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：US20250026764A1

公开(公告)日：2025-01-23

申请号：US18903075

申请日：2024-10-01

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 ,  A61K31/519 ,  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：US20240368188A1

公开(公告)日：2024-11-07

申请号：US18639255

申请日：2024-04-18

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  Darren W. Engers ,  Kayla J. Temple ,  Alison R. Gregro ,  Madeline F. Long ,  Anna E. Ringuette ,  Julie L. Engers

IPC: C07D513/04 ,  A61K31/444 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  C07D519/00

Abstract: 6,7-Dihydrothiazolo[5,4-c]pyridines substituted in the 5-position with heterocyclic rings are positive allosteric modulators of the muscarinic acetylcholine receptor Ma (mAChR MA) and may have use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

公开(公告)号：US20230348490A1

公开(公告)日：2023-11-02

申请号：US18344555

申请日：2023-06-29

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 ,  A61K31/519 ,  C07D493/14 ,  C07D519/00

CPC classification number: C07D495/14 ,  A61K31/519 ,  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：US20230286991A1

公开(公告)日：2023-09-14

申请号：US18187868

申请日：2023-03-22

Applicant: Vanderbilt University

Inventor： 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: C07D487/04

CPC classification number: C07D487/04

Abstract: 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：US20230183219A1

公开(公告)日：2023-06-15

申请号：US17920904

申请日：2021-04-23

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Aaron M. Bender ,  Changho Han ,  Trever R. Carter ,  Matthew Spock

IPC: C07D405/14 ,  C07D403/14 ,  C07D401/14 ,  C07D403/12 ,  C07D493/08 ,  C07D417/14

CPC classification number: C07D405/14 ,  C07D403/14 ,  C07D401/14 ,  C07D403/12 ,  C07D493/08 ,  C07D417/14 ,  C07B2200/05

Abstract: Disclosed herein are substituted hexahydro-1//-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.