Johns Hopkins University

Ústav Organické Chemie a Biochemie Av {hacek Over (c)}r, V.v.i.

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

Institute of Organic Chemistry & Biochemistry

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

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

Andrej Jancarik

Barbara S Slusher

Pavel Majer

Rana Rais

Lukas Tenora

Tomas Tichy

Marcela Krecmerova

Jan Vavra

Gregory J Riggins

Jonathan David Powell

Robert Leone

Judson Englert

Jonathan Powell

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

The disclosure provides methods of treating cancer in a subject or preventing a relapse or reducing the incidence of relapse of cancer in a subject in remission, comprising administering to the subject: (a) a therapeutically effective amount of an immunotherapeutic agent, e.g., an immune checkpoint blockade therapy, an adoptive cellular therapy, a marrow-infiltrating lymphocytes, an adenosine A2aR inhibitor, or an antibody; and (b) a compound 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).

Methods for cancer and immunotherapy using prodrugs of glutamine analogs

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

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.

Growing community of inventors

Koprivnice, Czechia

Andrej Jancarik