DrugPatentWatch Database Preview
« Back to Dashboard
Summary for Patent: 5,198,533
|Abstract:||The present invention deals with LHRH antagonists which possess improved water solubility and while having the high antagonist potency of the basic peptides, are free of the edematogenic effects. These compounds are highly potent in inhibiting the release of gonadotropins from the pituitary gland in mammals, including humans. The compounds of this invention are represented by the formula wherein X is an acyl group derived from straight or branched chain aliphatic or alicyclic carboxylic acids having from 1 to 7 carbon atoms, or H.sub.2 N--CO, R.sup.1 is D-- or L--Pro, D-- or L--.DELTA..sup.3 --Pro, D--Phe, D--Phe(4--H1), D--Ser, D--Thr, D--Ala, D--Nal(1) or D--Nal (2), R.sup.2 is D--Phe or D--Phe(4--C1) R.sup.3 is D--Trp, D--Phe, D--Pal(3), D--Nal(1) or D--Nal(2), R.sup.6 is D--Cit, D--Hci, D--Cit(Q) or D--Hci(Q) and R.sup.10 is Gly or D--Ala where Q is lower alkyl of 1-3 carbon atoms and H1 is fluoro, chloro or bromo, and the pharmaceutically acceptable acid addition salts thereof and methods of use pertaining to these compounds.|
|Inventor(s):||Schally; Andrew V. (Metarie, LA), Bajusz; Sandor (New Orleans, LA)|
|Assignee:||The Administrators of the Tulane Educational Fund (New Orleans, LA)|
1. A peptide having the formula:
X is acetyl,
R.sup.1 is D-Nal(2),
R.sup.2 is D-Phe(4Cl),
R.sup.3 is D-Trp or D-Pal(3),
R.sup.6 is D-Cit or D-Hci, and
R.sup.10 is D-Ala
and the pharmaceutically acceptable acid addition salts thereof.
2. A peptide of claim 1 wherein R.sup.3 is D-Pal(3).
For more information try a trial or see the plans and pricing
Serving hundreds of leading biopharmaceutical companies globally:
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.