公开(公告)号：US11299481B2

公开(公告)日：2022-04-12

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 ,  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：US20210230180A1

公开(公告)日：2021-07-29

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: C07D495/04 ,  C07D471/04

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：US10961253B2

公开(公告)日：2021-03-30

申请号：US16347450

申请日：2017-11-07

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  Darren W. Engers ,  P. Jeffrey Conn ,  Katrina A. Bollinger ,  Rory Capstick ,  Paul Spearing ,  Sean R. Bollinger

IPC: C07D495/04

Abstract: Disclosed herein are pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine and pyrimido[4′,5′:4,5]thieno[2,3-c]pyridazine compounds, which may be useful as positive allostenc 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：US10654847B2

公开(公告)日：2020-05-19

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

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：US20190218214A1

公开(公告)日：2019-07-18

申请号：US16333201

申请日：2017-09-14

Applicant: Vanderbilt University

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

IPC: C07D471/04 ,  C07D519/00 ,  A61P35/00

CPC classification number: C07D471/04 ,  A61P35/00 ,  C07D519/00

Abstract: Provided herein are substituted imidazo[1,2-a]pyridines useful as inhibitors of BMP signaling. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted imidazo [1,2-a] pyridines.

公开(公告)号：US10342782B2

公开(公告)日：2019-07-09

申请号：US15661786

申请日：2017-07-27

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Carrie K. Jones ,  Thomas M. Bridges ,  Changho Han ,  Andrew S. Felts

IPC: C07D495/14 ,  A61K31/4196 ,  A61K31/381 ,  A61K31/4162 ,  A61K31/166 ,  A61K31/437 ,  A61P25/28 ,  A61P25/04 ,  A61P25/20 ,  A61P25/00

Abstract: Disclosed herein are thieno[3,2-e][1,2,4]triazolo[1,5-a]pyridin-6-amine, thieno[3,2-e][1,2,4]triazolo[4,3-a]pyridin-3-amine, and imidazo[1,2-a]thieno[3,2-e]pyridin-3-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：US10221172B2

公开(公告)日：2019-03-05

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 ,  C07D519/00 ,  C07D487/04 ,  A61K31/55 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06

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：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.