Prodrugs of prostate specific membrane antigen (PSMA) inhibitor

0501191 - ÚOCHB 2019 RIV eng P - Patentový dokument
Slusher, B. - Rais, R. - Krečmerová, Marcela - Tichý, Tomáš - Majer, Pavel - Jančařík, Andrej
Prodrugs of prostate specific membrane antigen (PSMA) inhibitor.
2018. Vlastník: The Johns Hopkins University - Ústav organické chemie a biochemie AV ČR, v. v. i. Datum udělení patentu: 05.06.2018. Číslo patentu: US9988407
Institucionální podpora: RVO:61388963
Klíčová slova: 2-Phosphonomethylpentanedioic acid (2-PMPA) * glutamate carboxypeptidase II * GCPII * PSMA * pivaloyloxymethyl * isopropyloxycarbonyloxymethyl * POM * POC * prodrug
Obor OECD: Organic chemistry
https://worldwide.espacenet.com/publicationDetails/originalDocument?CC=US&NR=9988407B2&KC=B2&FT=D&ND=4&date=20180605&DB=&locale=en_EP#

Various structural types of prodrugs of 2-phosphonomethylpentanedioic acid were synthesized as GCPII inhibitors. The prodrug with the optimal pharmacokinetic profile was obtained by introducing POC groups on both the phosphonate and α-carboxylate. Thus formed Tris-POC-2-PMPA afforded excellent release of parent 2-PMPA following oral administration in both mice and dog.
Trvalý link: http://hdl.handle.net/11104/0293187