The United States of America, As Represented by the Secretary, Department of Health and Human Services

Other

Purdue Research Foundation

Sun Yat-senuniversity

An, Linkun

Christophe Marchand

Yves Pommier

Terrence R Burke, Jr

Stephen H Hughes

Barry Johnson

Xue Zhi Zhao

Steven Smith

Mathieu Metifiot

Linkun An

Mark Stanley Cushman

Marino Artico

Keli K Agama

Thomas S Dexheimer

Roberto Di Santo

Roberta Costi

Peng-Cheng Lu

Laurent Thibaut

Periyasamy Selvam

Kasthuraiah Maddali

Compounds of Formula I and the pharmaceutically acceptable salts thereof are disclosed The variables X, X, and Rare disclosed herein. The compounds are useful for treating cancer and related proliferative diseases. Pharmaceutical compositions containing compounds of Formula I and methods of treatment comprising administering compounds of Formula I are also disclosed.

Furoquinolinediones as inhibitors of TDP2

Compounds of Formula I and the pharmaceutically acceptable salts thereof are disclosed Formula I. The variables X, X, and Rare disclosed herein. The compounds are useful for treating cancer and related proliferative diseases. Pharmaceutical compositions containing compounds of Formula I and methods of treatment comprising administering compounds of Formula I are also disclosed. 

A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is N, C(OH), or CH;Y is H or OH;each of Z-Zis independently H or halogen;Ris H, OH, NH, NHR, NRRor R;R, R, and Ris each independently H, halogen, OR, R, NHR, NRR, COR, CONRR, SONRR, or Rand Rtogether with the carbon atoms to which Rand Rare attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; andRand Ris each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or Rand Rtogether with the nitrogen to which Rand Rare attached form an optionally-substituted heterocycle.

Compounds for inhibiting drug-resistant strains of HIV-1 integrase

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 instant invention is directed towards tetracycline compositions, and methods of inhibiting Tdp1 activity, and methods of treating Tdp1-associated disorders.

Tetracycline compounds as tyrosyl-DNA phosphodiesterase I inhibitors

A method for treating cancer in a subject, comprising administering to a subject having cancer a therapeutically effective amount of (i) a fluoroquinolone derivative that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity or (ii) a sulfonamide moiety-containing compound that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity, thereby treating the cancer in the subject. In certain embodiments, the fluoroquinolone derivative or sulfonamide moiety-containing compound is co-administered with a topoisomerase I (TopI) inhibitor.

Fluoroquinolone derivatives or sulfonamide moiety-containing compounds as inhibitors of tyrosyl-dnaphosphodiesterase (TDP1)

Novel quinoline inhibitors of retroviral integrase, particularly HIV-1 integrase. The quinoline inhibitors are oxoquinolines that can be used for preventing or treating AIDS or HIV infection in a subject.

Quinolin-4-ones as inhibitors of retroviral integrase for the treatment of HIV, AIDS and AIDS related complex (ARC)

Growing community of inventors

Silver Spring, MD, United States of America

Christophe Marchand