Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.

Novel inhibitors of DXP synthase and methods of use thereof are disclosed.

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I); wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is W.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or ##STR00001##
R.sup.1 and R.sup.2 are each independently H, alkyl optionally substituted with phenyl, or cycloalkyl, m is 0, 1, 2 or 3, A is a pharmaceutically acceptable acid, W.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.2/t; M is a metal ion, an ammonium ion or a basic amino acid cation which can form a salt with an acid radical; t is the charge number of M. ##STR00002##

The present invention relates to novel compounds and probes which have a common chemical structure necessary to obtain potent inhibitory activity against KLK4 and/or may be used for the detection of KLK4 peptides and their activity. It further relates to the use of these compounds and methods for inhibiting and/or detecting KLK4 activity in vitro and in vivo by making use of said probes or inhibitors. The compounds of the invention differ from prior art compounds at least in the presence of phenyl guanidine (instead of e.g. benzyl guanidine) and/or the presence of a heteroatom in the tail group, their combined presence unexpectedly leading to potent and selective KLK4 inhibitory activity.

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I); wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is W.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or

##STR00001##

R.sup.1 and R.sup.2 are each independently H, alkyl optionally substituted with phenyl, or cycloalkyl, m is 0, 1, 2 or 3, A is a pharmaceutically acceptable acid, W.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.2/t; M is a metal ion, an ammonium ion or a basic amino acid cation which can form a salt with an acid radical; t is the charge number of M.

##STR00002##