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：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：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：US09963466B2

公开(公告)日：2018-05-08

申请号：US15452686

申请日：2017-03-07

Applicant: Vanderbilt University

Inventor： Heidi E. Hamm ,  Shaun R. Stauffer ,  Craig W. Lindsley ,  Matthew T. Duvernay ,  Kayla J. Temple

IPC: C07D513/04

CPC classification number: C07D513/04

Abstract: Embodiments of the invention include compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition.

公开(公告)号：US12139498B1

公开(公告)日：2024-11-12

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 M4 (mAChR M4) and may have use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

公开(公告)号：US11884676B2

公开(公告)日：2024-01-30

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: A61K31/519 ,  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 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

Applicant: Vanderbilt University ,  H. LUNDBECK A/S

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, 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：US20210188820A1

公开(公告)日：2021-06-24

申请号：US16757245

申请日：2018-10-20

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

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：US20170253617A1

公开(公告)日：2017-09-07

申请号：US15452686

申请日：2017-03-07

Applicant: Vanderbilt University

Inventor： Heidi E. Hamm ,  Shaun R. Stauffer ,  Craig W. Lindsley ,  Matthew T. Duvernay ,  Kayla J. Temple

IPC: C07D513/04

CPC classification number: C07D513/04

Abstract: Embodiments of the invention include compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition.

公开(公告)号：US20250026743A1

公开(公告)日：2025-01-23

申请号：US18691617

申请日：2022-09-14

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  Kayla J. Temple ,  Katherine E. Crocker ,  Aaron M. Bender ,  Jackson P. Waters ,  Matthew Spock ,  Cori A. Malinky ,  Cayden J. Dodd

IPC: C07D413/14 ,  A61K31/4439 ,  A61K31/444 ,  C07D401/14 ,  C07D417/14

Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGlu5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate 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.