Purdue Research Foundation

National Institutes of Health, a Component of the US Dept. of Health & Human Services

Other

National Institutes of Health (nih)

United States of America As Represented by the Secretary of the Air Force

The United States of America As Represented by the United States

The United States of America As Represented by the Department of Health

Mark Stanley Cushman

Yves Pommier

Andrew E Morrell

Keli K Agama

Daniel Edward Beck

Rudiger D Haugwitz

Muthukaman Nagarajan

Smitha Antony

Mohamed S A Elsayed

Mohamed Seleem

Trung X Nguyen

Martin M Conda-Sheridan

Evgeny A Kiselev

Abdelrahman S Mayhoub

Richard M Van Rijn

Markus Lill

O M Zack Howard

Jurjus Jurayj

Robert J Cassell

Amr Hamed Mahmoud Abdallah

Rajesh Devraj

Agustin Casimiro-Garcia

William G Rice

Christophe Marchand

Venkatachala L Narayanan

Ping Wang

Yunlong Song

Ernest Hamel

Muthusamy Jayaraman

Pamela M Nagafuji

Ankush B Argade

Peng-Cheng Lu

Venkatachiala L Narayanan

Wieslaw M Golebiewski

John M Pezzuto

Arup Mati

Wei Lv

Alexandra S Ioanoviciu

Li-Ming Zhao

Yves G Pommier

The present disclosure relates to novel &#x3b4;-opioid receptor agonists, and the method of making and using the novel &#x3b4;-opioid receptor agonists. The novel &#x3b4;-opioid receptor agonists are selective &#x3b4;-opioid receptor agonists that have substantially no beta-arrestin 2 recruitment or low beta-arrestin 2 recruitment. The novel &#x3b4;-opioid receptor agonists may be used for the treatment for alcohol use disorders and other co-occurring psychiatric disorders.

Delta-opioid receptor agonists

Tyrosyl-DNA Phosphodiesterases 1 and 2 (Tdp1 and Tdp2) can repair damaged DNA resulting from topoisomerase inhibitors (e.g. Top1) and a variety of other DNA-damaging agents. 7-Azaindenoisoquinolines that are inhibitors of each of Top1, Tdp1 and Tdp2 are disclosed. Also described are methods for preparing azaindenoisoquinoline and methods for treating patients of a cancer using the disclosed azaindenoisoquinoline compounds or a pharmaceutical formulation thereof.

Azaindenoisoquinoline compounds and uses thereof

The invention described herein pertains to four series of aza-A-ring indenoisoquinolines, which are inhibitors of topoisomerase IB (Top1), and the processes for preparing said aza-A-ring indenoisoquinolines. Also described are methods for treating cancer in mammals using the described aza-A-ring indenoisoquinoline compounds or pharmaceutical formulations thereof.

Aza-A-ring indenoisoquinoline topoisomerase I poisons

Series of 2-phenyl-4-methylthiazole analogs are disclosed as potential therapeutic agents for the treatment of bacterial infections, especially methicillin-resistant(MRSA) related infections. A method for the treatment of MRSA-related infections is also claimed.

Phenylthiazoles and uses thereof

The invention described herein pertains to selective Janus kinase (JAK) inhibitors and methods of use thereof. Also described are methods for treating diseases involved abnormal JAK/STAT signaling pathway in mammals using the described selective JAK inhibitors or a pharmaceutical formulation thereof.

Janus kinase inhibitors and uses thereof

Triphenylethylene compounds of formula (II) as dual aromatase inhibitors and selective estrogen receptors modulators are described. Also described are methods for treating patients of breast cancers, and patients of breast cancer comorbid with osteoporosis, using the described triphenylethylence compounds or pharmaceutical formulations thereof.

Triphenylethylene compounds and uses thereof

Disclosed are compositions having activity against MRSA and/or VRSA, and methods of using the compositions to treat microbial infections.

Antimicrobial substituted thiazoles and methods of use

N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.

N-substituted indenoisoquinolines and syntheses thereof

The invention described herein pertains to substituted indenoisoquinoline compounds as described herein, wherein R, R, W, X and Y are defined herein, pharmaceutical compositions and formulations comprising the indenoisoquinoline compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.

Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors

The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds.

Synthesis and use of dual tyrosyl-DNA phosphodiesterase I (Tdp1)&#x2014;topoisomerase I (Top1) inhibitors

Growing community of inventors

West Lafayette, IN, United States of America

Mark Stanley Cushman