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US 5,330,973 AGranted
Lipopeptide derivatives
AssigneeMerck & Co., Inc.
InventorsMilton L. Hammond, Robert E. Schwartz, James M. Balkovec
Life of this patent
Estimating the term…
Abstract
The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
Claims12
A compound having the formula:
- ##STR23## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H or OH;
- R' is C.sub.5 -C.sub.23 alkyl, C.sub.5 -C.sub.23 alkenyl, C.sub.5 -C.sub.23 alkynyl or aryl;
- and
- R is an acyl, phosphono or sulfo radical which possesses a charged group at a neutral pH.
1 more element
A compound having the formula ##STR24## wherein U, V and W are independently H or OH, selected from those in which (1) U, V and W are all OH;
- (2) U and W are H and V is OH;
- (3) U and V are H and W is OH;
- R' is C.sub.5 -C.sub.23 alkyl, C.sub.5 -C.sub.23 alkenyl, C.sub.5 -C.sub.23 alkynyl or aryl;
- and
- R is
- (1) PO.sub.3 AH wherein A is H, C.sub.1 -C.sub.6 alkyl, phenyl or substituted phenyl wherein the substituent may be alkyl, alkyloxy, alkylthio, or alkylamino or a Li, Na, K, Mg and Ca cation salt thereof;
- (2) SO.sub.3 H or cation salt thereof as defined in (1)
- (3) COC.sub.n H.sub.2n CO.sub.2 H wherein n is 1 to 6 or a cation salt thereof as defined in (1)
- (4) CONAC.sub.n H.sub.2n CO.sub.2 H wherein A is as defined in (1), n is 1 to 6, or a cation salt thereof as defined in (1)
- (5) COOC.sub.n H.sub.2n CO.sub.2 H wherein n is 1 to 6, or a cation salt thereof as defined in (1)
- (6) CONA(CHB)CO.sub.2 H wherein B is a residue of an amino acid, or a cation salt thereof;
- as defined in (1)
- (7) COCHBNR.sub.1 R.sub.2 wherein B is a residue of an amino acid, R.sub.1 and R.sub.2 independently are H, C.sub.1 -C.sub.6 alkyl, and phenyl, and acid addition salts thereof;
- (8) CONAC.sub.n H.sub.2n NR.sub.1 R.sub.2 wherein A is as defined in (1), R.sub.1 and R.sub.2 independently are as defined in (7), n is 2 to 6, and acid addition salts thereof;
- (9) COOC.sub.n H.sub.2n NR.sub.1 R.sub.2 wherein R.sub.1 and R.sub.2 independently are as defined in (7), n is 2 to 6, and acid addition salts thereof;
- and
- (10) COC.sub.n H.sub.2n NR.sub.1 R.sub.2 wherein R.sub.1 and R.sub.2 independently are as defined in (7), n is 1 to 6 and acid addition salts thereof.
14 more elements
Dependencies are inferred from the claim text.