PRODRUGS OF D-ISOGLUTAMYL-[D/L]- TRYPROPHAN

Provided are carboxylic ester derivatives of formula (I), methods of preparing them, and methods for using them. These compounds are prodrugs of D-isoglutamyl-[D/L]-tryptophan. The in vitro bioconversion of some of the prodrugs to the parent drug D-isoglutamyl-D-tryptophan (or thymodepressin) was te...

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Main Authors XIN TAO, LEUNG-TOUNG REGIS, LI WANREN, RABADIA VRAJILAL S, TAM TIM FAT, FEENEY CHRISTOPHER JOHN, ZHAO YANQING, WODZINSKA JOLANTA MARIA, WANG YINGSHENG
Format Patent
LanguageEnglish
Published 25.06.2014
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:Provided are carboxylic ester derivatives of formula (I), methods of preparing them, and methods for using them. These compounds are prodrugs of D-isoglutamyl-[D/L]-tryptophan. The in vitro bioconversion of some of the prodrugs to the parent drug D-isoglutamyl-D-tryptophan (or thymodepressin) was tested in human hepatocytes and in human blood. In vivo pharmacokinetic studies following oral administration of some of the prodrugs to rats are also reported.
Bibliography:Application Number: ZA20130007229