A method for the synthesis of an aminoalkylenephosphonic acid or its phosphonate esters including the following steps: a) forming, in the presence of an aldehyde or ketone and an acid catalyst, a reaction mixture by mixing a compound having at least one HNR.sup.1R.sup.2 moiety or a salt thereof, with a compound having one or more POP anhydride moieties, the moieties having one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V), wherein the ratio of moles of aldehyde or ketone to NH moieties is 1 or more and wherein the ratio of NH moieties to POP anhydride moieties is 0.3 or more, and b) recovering the resulting aminoalkylenephosphonic acid having compound or its phosphonate esters.

The invention provides a newly discovered oxadiazole class of antibiotics. The oxadiazoles impair cell-wall biosynthesis and exhibit activities against the Gram-positive bacteria such as the bacterium Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA) and vancomycin-resistant and linezolid-resistant S. aureus. For example, 5-(1H-indol-5-yl)-3-(4-(4-(trifluoromethyl)phenoxy)phenyl)-1,2,4-oxadiazole (antibiotic 75b) was efficacious in a mouse model of MRSA infection, exhibiting a long half-life, a high volume of distribution, and low clearance. Antibiotic 75b antibiotic is bactericidal and is orally bioavailable. This class of antibiotics can be used as a therapeutic agent against infections by Gram-positive bacteria such as MRSA.

A composition comprising a perfluoro-N.sup.2-phosphinylamidine chromium salt complex having Structure PFAHNPACr I:

##STR00001##

wherein R.sup.f1 is a substituted phenyl group comprising alkyl groups at the 2 and 6 positions and at least one fluoro group or perfluoroalkyl group at the 3, 4, and/or 5 positions, R.sup.2 is a C.sub.1 to C.sub.30 organyl group, R.sup.4 and R.sup.5 are each independently a C.sub.1 to C.sub.30 organyl group, and CrX.sub.p is a chromium salt where X is a monoanion, and p is an integer from 2 to 6.

A catalyst system comprising an N.sup.2-phosphinylamidine chromium salt complex having Structure PFHNPACr I: ##STR00001##
wherein Rf.sup.1, Rf.sup.2, Rf.sup.4, and Rf.sup.5 are independently selected from a perfluorohydrocarbyl group; and CrX.sub.p is a chromium salt; X is a monoanion, and p is an integer from 2 to 6. A process comprising a) contacting i) ethylene, ii) a catalyst system comprising an N.sup.2-phosphinylamidine chromium salt complex having Structure PFHNPACr I: ##STR00002##
wherein each Rf.sup.1, Rf.sup.2, Rf.sup.4, and Rf.sup.5 are independently selected from a perfluorohydrocarbyl group and CrX.sub.p is a chromium salt; X is a monoanion and p is an integer from 2 to 6, and iii) optionally an organic reaction medium; and b) forming an oligomer product in a reaction zone.

The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

A compound of formula (I) for use in the prevention or treatment of a bacterial infection wherein: P.sup.X is selected from the group consisting of (P1), (P2) and (P3).

##STR00001##

A compound of Formula (II): for use in the prevention or treatment of a bacterial infection.

##STR00001##

The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.