公开(公告)号：US20240279232A1

公开(公告)日：2024-08-22

申请号：US18567191

申请日：2021-06-07

Applicant: UWM Research Foundation, Inc.

Inventor： Alexander E. Arnold ,  Douglas C. Stafford ,  James M. Cook ,  Amanda N. Nieman ,  Michael Ming-Jin Poe ,  Guanguan Li

IPC: C07D487/04 ,  A61K31/5517 ,  A61P29/00

CPC classification number: C07D487/04 ,  A61K31/5517 ,  A61P29/00

Abstract: Substituted 5-(4-methyl-6-phenyl-4H-benzo[f]imidazo[1,5-a][1.4]diazepin-3-yl)-1.2.4-oxadiazole compounds are ligands for the k opioid receptor and inhibit inducible nitric oxide synthase. The compounds have utility to inhibit NO production and treat associated inflammatory conditions.

公开(公告)号：US20240083905A1

公开(公告)日：2024-03-14

申请号：US18363933

申请日：2023-08-02

Applicant: UWM Research Foundation, Inc. ,  Centre for Addiction and Mental Health ,  University of Belgrade - Faculty of Pharmacy

Inventor： James M. Cook ,  Guanguan Li ,  Michael Ming-Jin Poe ,  Miroslav M. Savic ,  Etienne Sibille

IPC: C07D487/04 ,  A61P25/22

CPC classification number: C07D487/04 ,  A61P25/22

Abstract: Provided herein are alpha5-containing GABAA receptor agonists and pharmaceutical compositions and methods of treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders using them.

公开(公告)号：US20230103216A1

公开(公告)日：2023-03-30

申请号：US17886403

申请日：2022-08-11

Applicant: UWM Research Foundation, Inc. ,  The Trustees of Columbia University in the City of New York

Inventor： Alexander E. Arnold ,  Douglas C. Stafford ,  James M. Cook ,  Charles W. Emala ,  Gloria Forkuo ,  Rajwana Jahan ,  Revathi Kodali ,  Guanguan Li ,  Michael Rajesh Stephen

IPC: C07D487/14 ,  A61P11/06 ,  C07D487/04

Abstract: Pyrrolobenzodiazepines target alpha-4 and alpha-5 GABAA receptors for use in the treatment of airway hyperresponsiveness and inflammation in asthma. Compounds selectively partition to the peripheral compartment and have reduced CNS effects.

公开(公告)号：US12054491B2

公开(公告)日：2024-08-06

申请号：US17886403

申请日：2022-08-11

Applicant: UWM Research Foundation, Inc. ,  The Trustees of Columbia University in the City of New York

Inventor： Alexander E. Arnold ,  Douglas C. Stafford ,  James M. Cook ,  Charles W. Emala ,  Gloria Forkuo ,  Rajwana Jahan ,  Revathi Kodali ,  Guanguan Li ,  Michael Rajesh Stephen

IPC: C07D487/04 ,  A61P11/06 ,  C07D487/14

CPC classification number: C07D487/14 ,  A61P11/06 ,  C07D487/04

Abstract: The present invention describes substituted benzo[f]imidazo[1,5-a][1,4]diazepines of the formula (I):




wherein R1, R2, R2′, R3, and X are as disclosed herein. These compounds target alpha-4 and alpha-5 GABAa receptors and are useful for the treatment of airway hyperresponsiveness and inflammation in asthma.

公开(公告)号：US20200181146A1

公开(公告)日：2020-06-11

申请号：US16086053

申请日：2017-03-20

Applicant: UWM Research Foundation, Inc. ,  Centre for Addiction and Mental Health ,  University of Belgrade - Faculty of Pharmacy

Inventor： James M. Cook ,  Guanguan Li ,  Michael Ming-Jin Poe ,  Miroslav M. Savic ,  Etienne Sibille

IPC: C07D487/04 ,  A61P25/22

Abstract: Provided herein are alpha5-containing GABAA receptor agonists and pharmaceutical compositions and methods of treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders using them.

公开(公告)号：US12180216B2

公开(公告)日：2024-12-31

申请号：US18363933

申请日：2023-08-02

Applicant: UWM Research Foundation, Inc. ,  Centre for Addiction and Mental Health ,  University of Belgrade—Faculty of Pharmacy

Inventor： James M. Cook ,  Guanguan Li ,  Michael Ming-Jin Poe ,  Miroslav M. Savic ,  Etienne Sibille

IPC: C07D487/04 ,  A61K31/551 ,  A61P25/00 ,  A61P25/22

Abstract: Provided herein are alpha5-containing GABAA receptor agonists and pharmaceutical compositions and methods of treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders using them.

公开(公告)号：US11447495B2

公开(公告)日：2022-09-20

申请号：US16325080

申请日：2017-08-16

Applicant: UWM Research Foundation, Inc. ,  The Trustees of Columbia University in the City of New York

Inventor： Alexander E. Arnold ,  Douglas C. Stafford ,  James M. Cook ,  Charles W. Emala ,  Gloria Forkuo ,  Rajwana Jahan ,  Revathi Kodali ,  Guanguan Li ,  Michael Rajesh Stephen

IPC: A61K31/5517 ,  C07D487/04 ,  C07D487/14 ,  A61P11/06

Abstract: Substituted benzo[f]imidazo[1,5-α][1,4]diazepines of formula (I′) target alpha-4 and alpha-5 GABAA receptors for use in the treatment of airway hyperresponsiveness and inflammation in asthma. Compounds selectively partition to the peripheral compartment and have reduced CNS effects.

公开(公告)号：US10906909B2

公开(公告)日：2021-02-02

申请号：US16086053

申请日：2017-03-20

Applicant: UWM Research Foundation, Inc. ,  Centre for Addiction and Mental Health ,  University of Belgrade—Faculty of Pharmacy

Inventor： James M. Cook ,  Guanguan Li ,  Michael Ming-Jin Poe ,  Miroslav M. Savic ,  Etienne Sibille

IPC: A61K31/5517 ,  A61P25/00 ,  C07D487/04 ,  A61P25/22

Abstract: Provided herein are alpha5-containing GABAA receptor agonists and pharmaceutical compositions and methods of treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders using them.

公开(公告)号：US10259815B2

公开(公告)日：2019-04-16

申请号：US15560002

申请日：2016-03-18

Applicant: UWM Research Foundation, Inc.

Inventor： James Cook ,  Michael Ming-Jin Poe ,  Kashi Reddy Methuku ,  Guanguan Li

IPC: A61K31/5517 ,  A61P25/18 ,  C07D487/04

Abstract: Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.

公开(公告)号：US20180065967A1

公开(公告)日：2018-03-08

申请号：US15560002

申请日：2016-03-18

Applicant: UWM Research Foundation, Inc.

Inventor： James Cook ,  Michael Ming-Jin Poe ,  Kashi Reddy Methuku ,  Guanguan Li

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.