University of Southern California

University of Michigan

University of Texas System

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

Yunnan University

UniversitÀ Degli Studi Di Sassari

Nouri Neamati

Antonio Garofalo

Raveendra S Dayam

Jia Zhou

Yves Pommier

Min Wei

Valter D Longo

Vito Nacci

Na Ye

Kyunghwan Kim

Woojin An

Jun Lin

Yuting Kuang

Priya Balasubramanian

Mario Sechi

Wange Lu

Yi Jin

Jinxia Deng

Shuai Mao

Raveendra Dayam

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having an oxadiazole-oxadiazolone structure (e.g., oxadiazole-phenyl-oxadiazolone compounds, oxadiazole-pyridine-oxadiazolone compounds, oxadiazole-indole-oxadiazolone compounds, oxadiazole-quinoline-oxadiazolone compounds, oxadiazole-pyrrole-oxadiazolone compounds, and oxadiazole-vinyl-oxadiazolone compounds), and their use as therapeutics for the treatment of cancer and other diseases.

Small molecule inhibitors of MYC and uses thereof

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinazolinedione structure which function as reactive oxygen species (ROS) inducers and inhibitors of mitochondrial activity within cancer cells (e.g., pancreatic cancer cells), and their use as therapeutics for the treatment of cancer (e.g., pancreatic cancer) and other diseases.

Small molecule inducers of reactive oxygen species and inhibitors of mitochondrial activity

This invention is in the field of medicinal chemistry. In particular, the invention relates to novel small molecule compounds having a quinolin-8-yl-nicotinamide structure (e.g., a compound having Formula I: which are useful in treating, ameliorating, or preventing various forms of cancer (e.g., pancreatic cancer).

Substituted amides for treating and preventing cancer

Compounds and methods for treating diseases or conditions affected by the activity or expression of genes/proteins related to human GH, GHR, STAT5, SOCS, IGF-1, insulin are provided. Monoclonal antibodies for treating diseases or conditions related to growth hormone and growth hormone receptor activity are also provided.

Blockers of the growth hormone receptor in disease prevention and treatment

This disclosure provides methods and compositions to inhibit or suppress tumor growth or to treat cancer by inhibiting VprBP kinase activity. Also provided are methods of determining the effectiveness of the methods and compositions to inhibit or suppress tumor growth or to treat cancer by inhibiting VprBP kinase activity, methods for detecting a cancer, and methods for screening potential agents that inhibit VprBP kinase activity.

Compositions and methods for the treatment of VprBP-related cancers

Disclosed are pyrimidyl guanidine derivatives having anticancer activity. The pyimidyl guanidine derivatives have the structure: 

Substituted pyrimidyl guanidine derivatives having anticancer activity

Pharmacophore models to be used in drug design and discovery are provided. An in silico protocol and in vitro assays are presented. Compounds and their pharmaceutically acceptable salts with HIV-1 integrase inhibitory and anti-HIV activity and use thereof in the treatment of HIV/AIDS and related infections either alone or in combination with all the known antiretroviral therapeutics are described.

Compounds with HIV-1 integrase inhibitory activity and use thereof as anti-HIV/AIDS therapeutics

Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Such compounds include a compound of Formula II,  Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating gene expression.

Substituted N'-pyrrolo[1,2-a]quinoxalin-4-yl-hydrazides as anti-cancer agents

The present invention relates to compositions containing integrin-binding small molecules. Also disclosed are methods of binding integrins to these small molecules and methods of identifying small molecules binding to integrins.

Integrin-binding small molecules

The present invention discloses non-catechol compounds, such as thiazolothiazepines, and analogs and derivatives thereof, which are anti-integrase inhibitors. The compounds, which are useful as treatments for HIV disease, include compounds (I), (II), (III), or pharmaceutically acceptable salts thereof wherein A is thiazole, benzene, naphthalene, pyridine, pyrimidine, pyrazine, or quinoline; R is one or more of H, halogen, lower alkyl, lower alkoxy, NO, lower ester or carboxylic acid; X&#x2014;Y is CH&#x2014;S, S&#x2014;CH, CH&#x2014;O, CH&#x2014;S(O). S(O)&#x2014;CH, CH&#x2014;CH, CH&#x2014;CH&#x2014;CH, or CH&#x2014;CH&#x2014;CH&#x2014;CH; Ris H or hydroxy; Ris H, phenyl, or alkylamine; W is S or O; and Ris H, substituted or unsubstituted alkyl or amine; and Z is S, O, CH, CHCH, or C&#x2550;O.

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Ann Arbor, MI, United States of America

Nouri Neamati