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：US20150258128A1

公开(公告)日：2015-09-17

申请号：US14637334

申请日：2015-03-03

Applicant: UWM Research Foundation, Inc.

Inventor： James M. Cook ,  Terry S. Clayton ,  Hiteshkumar D. Jain ,  Yun Teng Johnson ,  Jie Yang ,  Sundari K. Rallipalli ,  Zhi-jian Wang ,  Ojas A. Namjoshi ,  Michael Ming-Jin Poe

IPC: A61K31/695 ,  A61K31/551

CPC classification number: A61K31/695 ,  A61K31/551 ,  C07D487/04 ,  C07D487/14 ,  C07D519/00

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.

Abstract translation: 本文描述的是α3或α2或α2/α3GABA能受体亚型选择性配体，药物组合物，以及这些配体和组合物在治疗焦虑症，癫痫和精神分裂症以及降低镇静和共济失调副作用中的应用的方法。 在实施方案中，诸如α3或α2或α2/α3GABA能受体亚型选择性配体缺少酯键，因此可能因酯酶水解而相对不敏感。

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：US09879020B2

公开(公告)日：2018-01-30

申请号：US14429808

申请日：2013-09-20

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

Inventor： Douglas C. Stafford ,  James M. Cook ,  Alexander E. Arnold ,  Charles W. Emala ,  George Gallos ,  Michael Rajesh Stephen

IPC: C07D487/04 ,  C07D487/14 ,  C07D487/22

CPC classification number: C07D487/22 ,  C07D487/14

Abstract: Novel methods of treating inflammation and airway constriction using GABAergic compounds with reduced benzo-diazepine-like CNS activity are provided. Novel compounds which selectively target alpha-4 and alpha-5 GABAA receptors and methods of using those compounds to treat bronchoconstriction and inflammation are provided herein.

公开(公告)号：US09597342B2

公开(公告)日：2017-03-21

申请号：US14637334

申请日：2015-03-03

Applicant: UWM Research Foundation, Inc.

Inventor： James M. Cook ,  Terry S. Clayton ,  Hiteshkumar D. Jain ,  Yun Teng Johnson ,  Jie Yang ,  Sundari K. Rallipalli ,  Zhi-jian Wang ,  Ojas A. Namjoshi ,  Michael Ming-Jin Poe

IPC: A61K31/551 ,  C07D487/04 ,  A61K31/695 ,  C07D487/14 ,  C07D519/00

CPC classification number: A61K31/695 ,  A61K31/551 ,  C07D487/04 ,  C07D487/14 ,  C07D519/00

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：US20150232473A1

公开(公告)日：2015-08-20

申请号：US14429808

申请日：2013-09-20

Applicant: UWM RESEARCH FOUNDATION, INC.

Inventor： Douglas C. Stafford ,  James M. Cook ,  Alexander E. Arnold ,  Charles W. Emala ,  George Gallos ,  Michael Rajesh Stephen

IPC: C07D487/22

CPC classification number: C07D487/22 ,  C07D487/14

Abstract: Novel methods of treating inflammation and airway constriction using GABAergic compounds with reduced benzo-diazepine-like CNS activity are provided. Novel compounds which selectively target alpha-4 and alpha-5 GABAA receptors and methods of using those compounds to treat bronchoconstriction and inflammation are provided herein.

Abstract translation: 提供了使用具有还原的苯并二氮杂类CNS活性的GABA能化合物治疗炎症和气道收缩的新方法。 本文提供了选择性靶向α-4和α-5 GABA A受体的新型化合物和使用这些化合物治疗支气管收缩和炎症的方法。

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.