6-POSITION MODIFIED DECAPEPTIDE LHRH ANTAGONISTS

The present invention provides a class of decapeptide compounds which are potent antagonists of LHRH activity and which have the structure A -D -E -G -J -L -M -Q -R -T . The compounds of the percent invention are characterized by having an OMEGA -amino-functionalized side chain on the D-aminoacyl re...

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Main Authors SWENSON, ROLF, E, FITZPATRICK, TIMOTHY, D, GREER, JONATHAN, HAVIV, FORTUNA, NICHOLS, CHARLES, J, MORT, NICHOLAS, A
Format Patent
LanguageEnglish
French
Published 23.06.1994
Edition5
Subjects
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present invention provides a class of decapeptide compounds which are potent antagonists of LHRH activity and which have the structure A -D -E -G -J -L -M -Q -R -T . The compounds of the percent invention are characterized by having an OMEGA -amino-functionalized side chain on the D-aminoacyl residue at position 6. The OMEGA -amino group of this side chain is further derivatized by the attachment of an extending group which likewise has a terminal amino group which is capped by an acyl group. La présente invention concerne une classe de composés décapeptidiques qui sont de puissants antagonistes de l'activité de LHRH et qui ont la structure A1-D2-E3-G4-J5-L6-M7-Q8-R9-T10. Les composés de la présente invention se caractérisent en ce qu'ils possèdent une chaîne latérale fonctionnalisée OMEGA-amino sur le reste D-aminoacyle en position 6. Le groupe OMEGA-amino de cette chaîne latérale est ensuite dérivé en y attachant un groupe élargi qui possède également un groupe amino terminal coiffé par un groupe acyle.
Bibliography:Application Number: WO1993US11628