Abstract: The present application provides a novel set of compounds comprising a sPLA2 inhibitor conjugated to a niacin drug, as well as kits containing these compounds and methods of using the compounds to alter lipid levels and treat various cardiovascular diseases.

Abstract: Administration of sPLA2 inhibitors has been found to decrease cholesterol levels, atherosclerotic plaque formation and aortic aneurysm in mice, and to decrease cholesterol and triglyceride levels in humans. Interestingly, administration of sPLA2 inhibitors was found to decrease cholesterol levels even when the inhibitors were administered only once per day. Therefore, provided herein are methods of treating dyslipidemia, CVD, and conditions associated with CVD such as atherosclerosis and metabolic syndrome, by administering one or more sPLA2 inhibitors. Significantly, administration of sPLA2 inhibitors and various compounds used in the treatment of CVD, such as for example statins, resulted in greater decreases in LDL and LDL particle levels in a synergistic manner. In addition, administration of sPLA2 inhibitors and statins resulted in a synergistic decrease in plaque content.

Abstract: Administration of sPLA2 inhibitors has been found to decrease cholesterol levels, atherosclerotic plaque formation and aortic aneurysm in mice, and to decrease cholesterol and triglyceride levels in humans. Interestingly, administration of sPLA2 inhibitors was found to decrease cholesterol levels even when the inhibitors were administered only once per day. Therefore, provided herein are methods of treating dyslipidemia, CVD, and conditions associated with CVD such as atherosclerosis and metabolic syndrome, by administering one or more sPLA2 inhibitors. Significantly, administration of sPLA2 inhibitors and various compounds used in the treatment of CVD, such as for example statins, resulted in greater decreases in LDL and LDL particle levels in a synergistic manner. In addition, administration of sPLA2 inhibitors and statins resulted in a synergistic decrease in plaque content.

Abstract: Niacin drugs are frequently utilized as a therapeutic to treat CVD, increase HDL levels, and/or decrease TG levels. As disclosed herein, it has been found that administration of one or more sPLA2 inhibitors in combination with one or more niacin drugs unexpectedly results in a synergistic increase in HDL levels and a synergistic decrease in TG levels. Therefore, compositions, methods, and kits are provided for treating CVD, increasing HDL levels, decreasing TG levels, and improving HDL/LDL ratios.

Abstract: Administration of sPLA2 inhibitors has been found to decrease cholesterol levels, atherosclerotic plaque formation and aortic aneurysm in mice, and to decrease cholesterol and triglyceride levels in humans. Interestingly, administration of sPLA2 inhibitors was found to decrease cholesterol levels even when the inhibitors were administered only once per day. Therefore, provided herein are methods of treating dyslipidemia, CVD, and conditions associated with CVD such as atherosclerosis and metabolic syndrome, by administering one or more sPLA2 inhibitors. Significantly, administration of sPLA2 inhibitors and various compounds used in the treatment of CVD, such as for example statins, resulted in greater decreases in LDL and LDL particle levels in a synergistic manner. In addition, administration of sPLA2 inhibitors and statins resulted in a synergistic decrease in plaque content.

Abstract: The present invention provides novel methods for the synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (III) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

Abstract: A process is provided for preparing chloromethyl di-tert-butylphosphate (an intermediate for use in preparing water-soluble azole antifungal compounds), wherein potassium di-tert-butylphosphate is reacted with chloromethyl chlorosulfate under mild conditions (15 to 25° C.) in the presence of a base such as sodium carbonate or potassium carbonate, catalyst such as tetrabutylammonium sulfate or tetrabutylammonium chloride and an organic solvent such as dichloromethane or tetrahydrofuran. A process for preparing an azole antifungal agent employing the chloromethyl di-tert-butylphosphate (prepared in accordance with the present invention) is also provided.