Patent ID: 6313143
Filing Date: 2001-11-06
Classification: A61P,C07D,C07F

Abstract:
A compound having the formula ##STR22##and pharmaceutically active salts of said compounds, wherein:R is selected from the group consisting of --PO.sub.3 R.sup.1 R.sup.2, --CHR.sup.3 OCOR.sup.4, --CHR.sup.3 OCO.sub.2 R.sup.4, --CHR.sup.3 OCONHR.sup.4 and --COR.sup.4 ;R.sup.1 and R.sup.2 are selected from the group consisting of H, Na and NH.sub.4, and are the same unless either R.sup.1 or R.sup.2 is H, in which case the other can be different, or alternatively, R.sup.1 and R.sup.2 together represent Ca;R.sup.3 is selected from the group consisting of H or methyl;R.sup.4 is selected from a group consisting of lower alkyl, which may be optionally substituted by one or more substituents selected from the group consisting of --CO.sub.2 R.sup.5, --NR.sup.6 R.sup.7, polyethylene glycol, --OPO.sub.3 R.sup.1 R.sup.2, hydroxy, alkoxy, and aryl, provided that when R is --COR.sup.4, R.sup.4 is not unsubstituted lower alkyl,alkenyl, which may be optionally substituted by one or more substituents selected from the group consisting of --CO.sub.2 R.sup.5, --NR.sup.6 R.sup.7, polyethylene glycol, --OPO.sub.3 R.sup.1 R.sup.2, hydroxy, alkoxy, and aryl,cycloalkyl, which may be optionally substituted by one or more substituents selected from the group consisting of --CO.sub.2 R.sup.5, --NR.sup.6 R.sup.7, polyethylene glycol, --OPO.sub.3 R.sup.1 R.sup.2, hydroxy, alkoxy, and aryl,heterocycle, which when including N as a heteroatom the N optionally may be substituted with --COR.sup.8, andaryl which optionally may be substituted by one or more substituents selected from the group consisting of --CO.sub.2 R.sup.5, hydroxy, alkoxy, polyethylene glycol, --OPO.sub.3 R.sup.1 R.sup.2, and alkyl which itself may be substituted with hydroxy, carboxy, and substituted amino;R.sup.5 is selected from the group consisting of H, Na, or lower alkyl;R.sup.6 and R.sup.7 are each independently selected from H, lower alkyl, and --COR.sup.8, or alternatively, the group --NR.sup.6 R.sup.7 forms a 5 or 6 membered heterocyclic ring; andR.sup.8 is lower alkyl that optionally may be substituted with a polyethylene glycol.