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：US20210284649A1

公开(公告)日：2021-09-16

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: 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：US20180362500A1

公开(公告)日：2018-12-20

申请号：US16116663

申请日：2018-08-29

Applicant: UWM Research Foundation, Inc. ,  Women and Infants Hospital of Rhode Island

Inventor： Alexander E. Arnold ,  Preetpal Singh Sidhu ,  Premchendar Nandhikonda ,  Rakesh K. Singh

IPC: C07D401/12 ,  C07D407/12 ,  A61K45/06 ,  C07D209/16 ,  A61K31/404 ,  C07D209/10 ,  C07D209/14

Abstract: Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.

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：US20170174655A1

公开(公告)日：2017-06-22

申请号：US15238305

申请日：2016-08-16

Applicant: UWM Research Foundation, Inc. ,  Women and Infants' Hospital of Rhode Island

Inventor： Alexander E. Arnold ,  Preetpal Singh Sidhu ,  Premchendar Nandhikonda ,  Rakesh K. Singh

IPC: C07D401/12 ,  C07D209/10 ,  C07D209/14

CPC classification number: C07D401/12 ,  A61K31/404 ,  A61K45/06 ,  C07D209/10 ,  C07D209/14 ,  C07D209/16 ,  C07D407/12 ,  A61K2300/00

Abstract: Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.

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：US10093653B2

公开(公告)日：2018-10-09

申请号：US15238305

申请日：2016-08-16

Applicant: UWM Research Foundation, Inc. ,  Women and Infants Hospital of Rhode Island

Inventor： Alexander E. Arnold ,  Preetpal Singh Sidhu ,  Premchendar Nandhikonda ,  Rakesh K. Singh

IPC: C07D401/12 ,  A61K45/06 ,  A61K31/404 ,  C07D407/12 ,  C07D209/16 ,  C07D209/10 ,  C07D209/14

Abstract: Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.

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：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：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。