公开(公告)号：US20240140943A1

公开(公告)日：2024-05-02

申请号：US18263052

申请日：2022-01-26

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Changho Han ,  Jinming Li, I

IPC: C07D471/04 ,  A61P25/00

CPC classification number: C07D471/04 ,  A61P25/00

Abstract: Arylsulfonamides of 4-heteroaryl-cyclohexyls, and their derivatives, are competitive and non-competitive inhibitors of the muscarinic acetylcholine receptor M5 (mAChR M5) and have utility in the treatment of psychiatric disorders such as substance-related misuse, substance-related disorder relapse, anxiety, depression, and psychosis.

公开(公告)号：US20230150986A1

公开(公告)日：2023-05-18

申请号：US17784365

申请日：2020-12-10

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Aaron M. Bender ,  Katrina A. Bollinger ,  Trever R. Carter ,  Jerri M. Rook ,  Jonathan W. Dickerson ,  Julie L. Engers ,  Kayla J. Temple ,  Changho Han ,  Matthew Spock ,  Logan A. Baker ,  Thomas M. Bridges

IPC: C07D405/14 ,  C07D401/14 ,  C07D403/12 ,  C07D498/04 ,  C07D409/14

CPC classification number: C07D405/14 ,  C07D401/14 ,  C07D403/12 ,  C07D498/04 ,  C07D409/14 ,  C07B2200/05 ,  C07B2200/09

Abstract: Disclosed herein are 2,3,5-trifluorophenyl-pyridazine substituted hexahydro-1H-cyclopenta[c]pyrrole 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：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：US20230303552A1

公开(公告)日：2023-09-28

申请号：US18002004

申请日：2021-06-18

Applicant: Vanderbilt University

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

IPC: C07D417/14 ,  C07D405/14 ,  C07D498/04 ,  C07D417/12 ,  C07D471/04

CPC classification number: C07D417/14 ,  C07D405/14 ,  C07D417/12 ,  C07D471/04 ,  C07D498/04

Abstract: Arylsulfonamides of carboxamido-piperidines, -pyrrolidines, and -azetidines, and their derivatives, are competitive and non-competitive inhibitors of the muscarinic acetylcholine receptor M5 (mAChR M5) and have utility in the treatment of psychiatric disorders such as substance-related misuse, substance- related disorder relapse, anxiety, depression, and psychosis.

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.

公开(公告)号：US20230183218A1

公开(公告)日：2023-06-15

申请号：US17920899

申请日：2021-04-23

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  P. Jeffrey Conn ,  Darren W. Engers ,  Aaron M. Bender ,  Changho Han

IPC: C07D405/14 ,  C07D403/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04

CPC classification number: C07D405/14 ,  C07D403/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D403/14 ,  C07D401/14 ,  C07D487/04

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：US10807959B2

公开(公告)日：2020-10-20

申请号：US16543303

申请日：2019-08-16

Applicant: Vanderbilt University

Inventor： Rocco D. Gogliotti ,  Shaun R. Stauffer ,  KyuOk Jeon ,  James M. Salovich ,  Jonathan D. Macdonald ,  Jonathan J. Mills ,  Kenneth M. Meyers ,  Joseph R. Alvarado ,  Changho Han ,  Stephen W. Fesik ,  Taekyu Lee

IPC: C07D233/48 ,  C07D401/12 ,  C07D401/14 ,  C07D207/22 ,  C07D401/06 ,  C07D405/12 ,  C07D233/26 ,  C07D413/12 ,  C07D263/28 ,  C07D213/58

Abstract: Benzamides and picolinamides that are meta-substituted with imino-, guanidino-, or heterocycle-containing groups disrupt the WDR5-MLL1 protein-protein interaction, and have use in pharmaceutical compositions and in treating proliferative disorders and conditions in a subject, such as cancer.

公开(公告)号：US20180028501A1

公开(公告)日：2018-02-01

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: A61K31/4196 ,  A61K31/381 ,  A61K31/166 ,  A61K31/4162

CPC classification number: A61K31/4196 ,  A61K31/166 ,  A61K31/381 ,  A61K31/4162 ,  A61K31/437 ,  C07D495/14 ,  Y02A50/401

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：US20230183237A1

公开(公告)日：2023-06-15

申请号：US17998901

申请日：2021-05-21

Applicant: Vanderbilt University

Inventor： Craig W. Lindsley ,  Carrie K. Jones ,  P. Jeffrey Conn ,  Changho Han ,  Andrew S. Felts ,  Douglas L. Orsi ,  Julie L. Engers ,  Jinming Li ,  Rory A. Capstick ,  David L. Whomble ,  Kayla J. Temple

IPC: C07D471/04 ,  C07D417/14 ,  C07D405/14 ,  C07D513/04 ,  C07D495/04 ,  C07D487/04 ,  C07D491/048 ,  C07D519/00 ,  C07D401/14 ,  C07D413/14 ,  C07D498/04 ,  C07D401/12

CPC classification number: C07D471/04 ,  C07D417/14 ,  C07D405/14 ,  C07D513/04 ,  C07D495/04 ,  C07D487/04 ,  C07D491/048 ,  C07D519/00 ,  C07D401/14 ,  C07D413/14 ,  C07D498/04 ,  C07D401/12 ,  C07B2200/05

Abstract: Arylsulfonamides of 4-heteroaryl-piperidines, and their derivatives, are competitive and non-competitive inhibitors of the muscarinic acetylcholine receptor M5 (mAChR M5) and have utility in the treatment of psychiatric disorders such as substance-related misuse, substance-related disorder relapse, anxiety, depression, and psychosis.

公开(公告)号：US20200055824A1

公开(公告)日：2020-02-20

申请号：US16543303

申请日：2019-08-16

Applicant: Vanderbilt University

Inventor： Rocco D. Gogliotti ,  Shaun R. Stauffer ,  KyuOk Jeon ,  James M. Salovich ,  Jonathan D. Macdonald ,  Jonathan J. Mills ,  Kenneth M. Meyers ,  Joseph R. Alvarado ,  Changho Han ,  Stephen W. Fesik ,  Taekyu Lee

IPC: C07D233/48 ,  C07D401/12 ,  C07D401/14 ,  C07D207/22 ,  C07D213/58 ,  C07D405/12 ,  C07D233/26 ,  C07D413/12 ,  C07D263/28 ,  C07D401/06

Abstract: Benzamides and picolinamides that are meta-substituted with imino-, guanidino-, or heterocycle-containing groups disrupt the WDR5-MLL1 protein-protein interaction, and have use in pharmaceutical compositions and in treating proliferative disorders and conditions in a subject, such as cancer.