公开(公告)号：US20180022745A1

公开(公告)日：2018-01-25

申请号：US15547775

申请日：2016-02-01

Applicant: Vanderbilt University

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

IPC: C07D471/04 ,  A61K31/496 ,  A61K31/437 ,  A61K31/554 ,  A61K31/553 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/4725 ,  A61K31/541 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/502 ,  C07D401/12 ,  A61K31/4375 ,  C07D519/00 ,  A61K31/519 ,  A61K45/06

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/502 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/553 ,  A61K31/554 ,  A61K45/06 ,  C07D401/12 ,  C07D487/04 ,  C07D519/00 ,  A61K2300/00

Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); 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：US20180022744A1

公开(公告)日：2018-01-25

申请号：US15540239

申请日：2016-01-13

Applicant: Vanderbilt University

Inventor： P. Jeffrey Conn ,  Corey R. Hopkins ,  Craig W. Lindsley ,  Colleen M. Niswender ,  Darren W. Engers ,  Sean Bollinger

IPC: C07D471/04 ,  C07D487/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  C07D487/04 ,  C07D519/00 ,  A61K2300/00

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：US20180021312A1

公开(公告)日：2018-01-25

申请号：US15540972

申请日：2016-01-13

Applicant: Vanderbilt University

Inventor： P. Jeffrey Conn ,  Corey R. Hopkins ,  Craig W. Lindsley ,  Colleen M. Niswender ,  Darren W. Engers ,  Joe Panarese ,  Sean Bollinger ,  Julie Engers

IPC: A61K31/423 ,  C07D413/12 ,  A61K45/06 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4985

CPC classification number: A61K31/423 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  A61K2300/00 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04

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：US20170129889A1

公开(公告)日：2017-05-11

申请号：US15410449

申请日：2017-01-19

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 ,  C07D417/10 ,  C07D519/00 ,  C07D401/14 ,  C07D487/04 ,  C07D403/10 ,  C07D401/10

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：US20250017935A1

公开(公告)日：2025-01-16

申请号：US18700120

申请日：2022-10-14

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Julie L. Engers ,  Madeline F. Long ,  Charlotte Park ,  Aaron M. Bender ,  Logan A. Baker

IPC: A61K31/519 ,  A61K31/517 ,  A61P25/18 ,  A61P25/28 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to 7,8-dihydro-5H-1,6-naphthyridine derivatives of formula (I) The present compounds are positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4) for use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction. An exemplary compound is e.g. example 1: 5,6-dimethyl-4-[3-(trifluoromethyl)-7,8-dihydro-5H-1,6-naphthyridin-6-yl]thieno[2,3-d]pyrimidine (compound 1): Data on the activity of exemplary compounds in an mAChR M4 cell-based assay is provided.

公开(公告)号：US20240208983A1

公开(公告)日：2024-06-27

申请号：US18553398

申请日：2022-04-01

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Andrew S. Felts ,  Rory A. Capstick ,  David L. Whomble

IPC: C07D487/04 ,  A61K31/4375 ,  A61P25/24 ,  A61P25/28

CPC classification number: C07D487/04 ,  A61K31/4375 ,  A61P25/24 ,  A61P25/28

Abstract: Described are 6-aryl [1,2,4]triazolo[4,3-a]pyridin-3(2H)-ones as negative allosteric modulators of metabotropic glutamate receptor 2 (mGlu2), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, anxiety, obsessive-compulsive disorder, cognitive disorders, Alzheimer's disease, or autism spectrum disorders in a subject.

公开(公告)号：US20240174655A1

公开(公告)日：2024-05-30

申请号：US18553408

申请日：2022-04-01

Applicant: Vanderbilt University

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

IPC: C07D405/14

CPC classification number: C07D405/14

Abstract: Disclosed herein are (6-(2H-indazol-5-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine compounds, 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：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：US20220259190A1

公开(公告)日：2022-08-18

申请号：US17730112

申请日：2022-04-26

Applicant: Vanderbilt University

Inventor： P. Jeffrey Conn ,  Craig W. Lindsley ,  Andrew S. Felts ,  Colleen M. Niswender ,  Rory A. Capstick ,  Paul K. Spearing ,  Sean R. Bollinger

IPC: C07D405/14 ,  C07D407/14 ,  A61P25/00 ,  C07D409/14 ,  C07D519/00 ,  C07D401/12 ,  C07D471/04

Abstract: Indazole 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 states associated with glutamate dysfunction.