Abstract: The present invention is directed to novel antibiotic A 40926 derivatives characterized by having a carboxy, (C.sub.1 -C.sub.4) alkoxy-carbonyl, aminocarbonyl, (C.sub.1 -C.sub.4) alkylaminocarbonyl, di (C.sub.4 -C.sub.4)alkylaminocarbonyl or hydroxymethyl substituent on the N-acylaminoglucuronyl moiety and a hydroxy or a polyamine substituent in position 63 of the molecule. The compounds of the invention show high in vitro activity against glycopeptide resistant Enterococci and Staphylococci.
Type:
Grant
Filed:
April 30, 1996
Date of Patent:
May 12, 1998
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Adriano Malabarba, Romeo Ciabatti, Gianbattista Panzone, Alessandra Maria Marazzi
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 formulaX--R.sup.1 --R.sup.2 --R.sup.3 --Ser--Tyr--R.sup.6 --Leu--Arg--Pro--R.sup.10 --NH.sub.2whereinX 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) andR.sup.
Type:
Grant
Filed:
May 23, 1988
Date of Patent:
March 30, 1993
Assignee:
The Administrators of the Tulane Educational Fund