Xavier University of Louisiana

The Administrators of the Tulane Educational Fund

United States of America, As Represented by the Secretary of Agriculture

United States Department of Agriculture

Xavier University

Xavier University of Lousiana

Endotarget Inc.

Guangdi Wang

Shilong Zheng

Qiu Zhong

Quan Jiang

Matthew E Burow

Stephen M Boue

Qiang Zhang

Thomas E Wiese

Jiawang Liu

Shanchun Guo

Bruce Alan Bunnell

Galina Goloverda

Igor Kolesnichenko

Amy Strong

Vladimir Kolesnichenko

Hongjoong Kim

Xianyou Peng

Borui Kang

Matthew Burow

Stephen Boue

Bruce Bunnell

Madhusoodanan Mottamal

The present disclosure relates to compounds having the structure of Formula (I) that serve as degraders (and/or inhibitors) of Bruton's tyrosine kinase (BTK). In the present disclosure, the said compounds, which contain a target protein (BTK) binding moiety and a E3 ubiquitin ligase (CRBN) binding moiety, are directed to bind to both the BTK and CRBN, such that the BTK is placed in close proximity to the E3 ligase to mediate ubiquitylation of the target protein followed by degradation of the target protein by the proteasome. The present disclosure provides methods for synthesizing the herein disclosed said compounds, and their pharmacological activities associated with degradation or inhibition of the target protein. Further, the present disclosure teaches the utilization of such compounds in a treatment for proliferative diseases and autoimmune disorders, including hematological cancers and rheumatoid arthritis, particularly non-Hodgkin lymphoma, and especially chronic lymphocytic leukemia (CLL) and mantle cell lymphoma.

Substituted pyrimidines for the targeted degradation of Bruton's tyrosine kinase

Disclosed are methods of solvent removal in an evacuated, closed system at ambient or low (spontaneously dropped due to evaporation endothermicity) temperature. The methods disclosed are suitable for removing the solvents with a broad range of volatility, having normal (STP) boiling points from 30 up to at least 202° C. (vapor pressures at least of 0.1 to 500 torr; higher boiling point solvents are possible to remove with longer experimental times) and is only limited from a volume standpoint by the size of the apparatus used.

Methods of solvent removal at ambient temperatures—cryovap

The present disclosure relates to androgen receptor signaling inhibitors and the synthesis of the same. Further, the present disclosure teaches the utilization of the androgen receptor signaling inhibitors in a treatment for proliferative diseases, including cancer, particularly prostate cancer, and especially castration-resistant prostate cancer.

Inhibitors of androgen receptor signaling

Disclosed are daidzein analogs having the formula (I). Also disclosed are compositions, include a disclosed daidzein analogs, methods of preventing or treating bone disease or bone injury and/or stimulating bone growth, in a subject that include administering to the subject an effective amount of disclosed daidzein analog. Disclosed are isolated mesenchymal stem cell that has been altered by treatment a disclosed daidzein analog, daidzein, glycinol, glyceollin I, or glyceollin II, to increase the osteogenic potential of the mesenchymal stem cells.

Enhanced osteogenic activity of daidzein analogs on human mesenchymal stem cells

The present disclosure relates to boronic derivatives of hydroxamate compounds, methods for making the same, methods for use as a monotherapy or in combination with one or more other therapeutic agents, for treatment of proliferative diseases such as cancer. The present disclosure also teaches the utilization of said boronic derivatives of hydroxamates as epigenetic therapy medications with enhanced bioavailability, lower-toxicity, and longer-lasting efficacy.

Boronic derivatives of hydroxamates as anticancer agents

Boron-based prodrugs of phenol- or aromatic hydroxyl group-containing therapeutic molecules ('original drugs'), uses thereof, and methods of making the same, are provided for achieving, for example, improved bioavailability, prolonged retention (e.g., in a circulatory system) and, in particular, significantly lowered therapeutically effective dosage in order to reduce adverse effects while maintaining the desired therapeutic effects of the original drugs.

Boron-based prodrug strategy for increased bioavailability and lower-dosage requirements for drug molecules containing at least one phenol (or aromatic hydroxyl) group

Combretastatins analog compounds and their pharmaceutically acceptable salts are presented, as well as pharmaceutical compositions comprising the combretastatin analog compounds and uses of the combretastatin analog compounds, either alone or in combination with at least one additional therapeutic agent, in the treatment of cancer, and in particular cancer presenting as metastatic tumors.

Anti-vasculature and anti-tubulin combretastatin analogs for treatment of cancer

Provided are compositions for treatment of cancers, including breast cancer, comprising at least one novel daidzein analog, as well as methods of using the same for preventing or treating cancer or tumor growth.

Daidzein analogs as treatment for cancer

Thiazole analog compounds and their pharmaceutically acceptable salts are disclosed, including pharmaceutical compositions comprising the thiazole analog compounds, either alone or in combination with at least one additional therapeutic agent, and/or with a pharmaceutically acceptable carrier. Methods of using the thiazole analog compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative diseases, such as cancer, are also disclosed.

Anti-migration and anti-invasion thiazole analogs for treatment of cellular proliferative disease

The present disclosure relates to boron-based 4-hydroxytamoxifen and endoxifen prodrugs and the synthesis of the same. Further, the present disclosure teaches the utilization of the boron-based 4-hydroxytamoxifen and endoxifen prodrugs in a treatment for breast cancer.

Growing community of inventors

New Orleans, LA, United States of America

Guangdi Wang