Duke University

American Home Products Corporation

Eli Lilly and Company

Ohio State Innovation Foundation

Other

Icagen, Inc.

Esanex, Inc.

Philip Floyd Hughes

Timothy Haystead

Timothy A J Haystead

John H Musser

Leslie G Humber

Dominick Mobilio

Sean Patrick Hollinshead

Jose Serafin Mendoza

Joseph Wendell Wilson

Emily Derbyshire

Charles Howard Mitch

John S Ward

Bret E Huff

Michael A Staszak

Yazan Alwarawrah

Jesse Kwiek

Michael F Gross

Serge Beaudoin

Grant Andrew McNaughton-Smith

George Salvatore Amato

Christopher David Lascola

Dennis J Thiele

Jiyong Hong

Michael Terman

Neil Alexander Castle

Bushu Dong

Alexander M Jaeger

Khaldon Bodoor

This disclosure relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating diseases related to Heat Shock Transcription Factor 1 (HSF1) activity and/or function. More particularly, this disclosure relates to methods of inhibiting HSF1 activity with these compounds and pharmaceutical compositions thereof, and methods of treating diseases associated with HSF1 activity and/or function, such as cancer.

Compositions and methods for the treatment of cancer

The present invention provides inhibitors of TAK1 having formula (I) and methods of using such compounds to treat various diseases.

Substituted benzimidazoles as inhibitors of transforming growth factor-&#x3b2; kinase

The present disclosure relates to a method for inhibiting Fatty Acid Synthase (FASN) with a FASN inhibitor, methods for treating cancer and viral infections with a FASN inhibitor, and compounds and compositions inhibiting FASN.

Fatty acid synthase inhibitors

Described herein are compounds that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may allow for selective detection of Hsp90 in a sample.

Compounds and methods for targeting HSP90

The present invention provides inhibitors of TAK1 having formula (II), affinity resins, and fluorescent dyes and methods of using such compounds to treat various diseases or in protein isolation or purification. 

Substituted indazoles linked to a substituted adenine with a polyethylene glycol moiety selectively bind to Hsp90. The compounds include detection moieties such as fluorophores and are useful in methods and kits for selective detection of Hsp90 in a sample. 

Substituted heterocycles for targeting Hsp90

Described herein are substituted indazoles comprising formula (II) that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. Formula (II) may link to detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample. 

Substituted heterocycles for targeting HSP90

The invention relates to indazolylbenzamide, indolylbenzamide, benzo[d]imidazolyl-benzamide, and benzo[d]triazolylbenzamide derivatives of formula useful in the treatment and/or prevention of diseases and/or conditions related to cell proliferation, such as cancer, infection, inflammation and inflammation-associated disorders, and conditions associated with angiogenesis.

Indazolyl- and indolyl-benzamide derivatives

The present invention provides novel inhibitors of TAK1 having formula (I) and methods of using such compounds to treat various diseases. 

Substituted benzimidazole and substituted benzothiazole inhibitors of transforming growth factor-&#x3b2; kinase and methods of use thereof

Described herein are 6-aminopurine compounds comprising formula (III) that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. Formula (III) may link to detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample. 

Substituted 6-aminopurines for targeting HSP90

Inducible HSP70 is overexpressed in a wide spectrum of human tumors and its expression correlates with metastasis and poor outcomes to radiation and chemotherapy in patients. Identification of small molecule inhibitors of HSP70 pose a new therapy to cancer treatment. HS72, a benzimidazole piperidinyl carboxamide has been identified as an allosteric inhibitor for HSP70 and has demonstrated good tumor growth inhibition in vivo.

Heat shock protein 70 (hsp-70) receptor ligands

Described herein are substituted indazoles that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. The compounds may include detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample. Suitable compounds include those of formula (II): 

Substituted indazoles for targeting Hsp90

The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.

Growing community of inventors

Chapel Hill, NC, United States of America

Philip Floyd Hughes