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Prodrugs of prostate specific membrane antigen (PSMA) inhibitor
- 1.0501191 - ÚOCHB 2019 RIV eng P - Patent Document
Slusher, B. - Rais, R. - Krečmerová, Marcela - Tichý, Tomáš - Majer, Pavel - Jančařík, Andrej
Prodrugs of prostate specific membrane antigen (PSMA) inhibitor.
2018. Owner: The Johns Hopkins University - Ústav organické chemie a biochemie AV ČR, v. v. i. Date of the patent acceptance: 05.06.2018. Patent Number: US9988407
Institutional support: RVO:61388963
Keywords : 2-Phosphonomethylpentanedioic acid (2-PMPA) * glutamate carboxypeptidase II * GCPII * PSMA * pivaloyloxymethyl * isopropyloxycarbonyloxymethyl * POM * POC * prodrug
OECD category: 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.
Permanent Link: http://hdl.handle.net/11104/0293187
File Download Size Commentary Version Access 0501191.pdf 7 5.3 MB Other open-access
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