University of Illinois

G1 Therapeutics, Inc.

Chicago Biosolutions, Inc.

Thatcher, Gregory R.

Molloy, Mary Ellen

Tonetti, Debra

Qin, Zihui

Michalsen, Bradley

Xiong, Rui

Siklos, Marton

Thatcher, Greg, R.

Gregory R Thatcher

Rui Xiong

Jiong Zhao

Debra A Tonetti

Yangfeng Li

Yunlong Lu

Zihui Qin

Bradley Michalsen

Mary Ellen Molloy

Marton Siklos

Lauren Gutgesell

Carlo Ivan Rosales

Jay Copeland Strum

Irina Gaisina

Norton Peet

Lijun Rong

Debra Tonetti

In one aspect, the disclosure relates to relates to substituted benzothiophene analogs which are useful as selective degraders of estrogen receptor, methods of making same, pharmaceutical compositions comprising same, and methods of treating one or more clinical conditions associated with estrogen receptor, such as a cancer, including breast cancer, or osteoporosis. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

Substituted benzothiophene analogs as selective estrogen receptor degraders

This invention is benzothiophene-based estrogen receptor downregulators and their compositions and uses to treat estrogen-related medical disorders.

Benzothiophene-based selective estrogen receptor downregulator compounds

Described herein are pyridinone-based compounds, derivatives thereof, and pharmaceutical formulations thereof. In some aspects, the pyridinone-based compounds, derivatives thereof, and/or pharmaceutical formulations thereof can be administered to a subject in need thereof. In some aspects, pyridinone-based compounds, derivatives thereof, and/or pharmaceutical formulations thereof can modulate an activity and/or a function of a BRD protein and/or BET protein.

Pyridinone-based epigenetic modifiers and uses thereof

Vaccination is the most prevalent prophylactic means for controlling seasonal influenza infections. However, an effective vaccine usually takes at least 6 months to develop for the circulating strains. Therefore, new therapeutic options are needed for acute treatment of influenza infections to control this virus and prevent epidemic/pandemic situations from developing. Described herein are fast-acting, orally active acylated amino-substituted heterocyclyl compounds effective to control this virus. In one aspect, described herein is a method of treating an influenza infection in a subject comprising administering to the subject the compounds described herein.

Inhibitors of influenza viral entry

Benzothiophene-based selective estrogen receptor downregulators

Compositions, combinations and methods comprising a CDK4/6 inhibitor of Formula D with a selective estrogen receptor downregulator of Formula A, B or C that are advantageous for the treatment of abnormal cellular proliferation, including a cancer or a tumor.

Combination therapy for treatment of cancer

Disclosed herein are methods for treatment of estrogen-related medical disorders. The methods of treatment may comprise administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of at least one compound of formula (I) or a pharmaceutically acceptable salt thereof.

Compositions and methods for treating estrogen-related medical disorders

This invention is benzothiophene-based selective mixed estrogen receptor downregulators and their compositions and uses to treat estrogen-related disorders.

Benzothiophene-based selective mixed estrogen receptor downregulators

Disclosed is a compound of formula (I). or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions including the compound of formula (I) and methods of using the compound of formula (I). 

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Chicago, IL, United States of America

Gregory R Thatcher