The Johns Hopkins University

Institute of Organic Chemistry and Biochemistry Ascr, V.v.i.

ÚStav Organické Chemie A Biochemie Av {Hacek Over (c)}r, V.v.i.

Ustav Organicke Chemie a Biochemie Av Cr, V.v.i.

Institute of Organic Chemistry & Biochemistry

Inst of Organic Chem. and Biochemistry As Cr V.v.i

Adarga Limited

Rana Rais

Barbara S Slusher

Pavel Majer

Andrej Jancarik

Lukas Tenora

Tomas Tichy

Marcela Krecmerova

Jan Vavra

Xuhang Li

Gregory J Riggins

James Vornov

Ivan Snajdr

Katerina Novotna

Jesse Alt

Clemens Kratochwil

Michael Nedelcovych

Diane E Peters

Glutamine antagonists and their use for treating oncological, immunological, and neurological diseases are disclosed. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder, the method comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof. Also disclosed are methods of enhancing the effects of an immune checkpoint inhibitor, enabling a subject to respond to an immune checkpoint inhibitor, or enabling the toxicity or the dose or number of treatments with an immune checkpoint inhibitor to be reduced, comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof, and an immune checkpoint inhibitor. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder that is refractory to checkpoint inhibitor therapy, the method comprising administering to a subject in need thereof, and having the refractory disease or disorder, a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof.

Glutamine antagonists and uses thereof

Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.

Prodrugs of prostate specific membrane antigen (PSMA) inhibitor

The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R, R, R′, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

Prodrugs of glutamine analogs

Prodrugs of hydroxamate-based GCPII inhibitors and methods of their use for treating a disease or condition are disclosed.

Prodrugs of hydroxamate-based GCPII inhibitors

Prodrugs of mebendazole and methods for their use in treating a disease, disorder, or disorder, including cancer, are disclosed.

Mebendazole prodrugs with enhanced solubility and oral bioavailability

Methods for buccally, sublingually, or intranasally administering a prodrug of propofol to a subject in need of treatment thereof in an amount sufficient to deliver a therapeutically effective amount of propofol to the subject are disclosed.

Buccal, sublingual and intranasal delivery of fospropofol

Prodrug compositions and utility of hydroxamate-based GCPII inhibitors

The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R, R, R', and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

Methods and compounds are disclosed for treating inflammatory bowel disease (IBD) by using Prostate Specific Membrane Antigen (PSMA) inhibitors.

Methods for treating inflammatory bowel disease using prostate specific membrane antigen (PSMA) inhibitors

Growing community of inventors

West Friendship, MD, United States of America

Rana Rais