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：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：US20240228468A1

公开(公告)日：2024-07-11

申请号：US18553412

申请日：2022-04-05

Applicant: Vanderbilt University

Inventor： Aaron M. Bender ,  Matthew Spock ,  Trever R. Carter ,  Melissa A. Korkmaz-Vaisys ,  Logan A. Baker ,  P. Jeffrey Conn ,  Craig W. Lindsley

IPC: C07D403/12 ,  A61K31/351 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/5377 ,  C07D237/12 ,  C07D237/24 ,  C07D309/06 ,  C07D309/08 ,  C07D401/14 ,  C07D405/14 ,  C07D495/04

CPC classification number: C07D403/12 ,  A61K31/351 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/5377 ,  C07D237/12 ,  C07D237/24 ,  C07D309/06 ,  C07D309/08 ,  C07D401/14 ,  C07D405/14 ,  C07D495/04

Abstract: The present invention relates to (6-((octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl)benzamide (R2b is —C(O)N(RA1)(RA2) and N-(6-((octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl) phenyl) carboxamide (R2b is —N(RB)C(O)RC) derivatives of formula (I) wherein (II) R2b is —C(O)N(RA1)(RA2) or —N(RB)C(O)RC as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4) for the treatment of neurodegenerative disorders, movement disorders or brain disorders, such as e.g. Parkinson's disease, drug-induced Parkinsonism, dystonia, Tourette's syndrome, dyskinesias, schizophrenia, cognitive deficits associated with schizophrenia, excessive daytime sleepiness, attention deficit hyperactivity disorder (ADHD), Huntington's disease, chorea, cerebral palsy, and progressive supranuclear palsy. An exemplary compound is e.g. N-(4-(6-(((3aR,5s,6aS)-2-(2-fluorobenzyl)octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl) phenyl)acetamide (A1) (III).

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.