Processes for the preparation of dolutegravir and pharmaceutically acceptable salts utilizing alkenylamine are disclosed. Intermediates in those synthetic schemes are also disclosed.

The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

The present invention provides compounds of Formula (I): ##STR00001##
or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

The present invention relates to novel derivatives of cystobactamides of formula (Ib) and the use thereof for the treatment or prophylaxis of bacterial infections.

##STR00001##

The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R.sup.1 is optionally substituted C.sub.6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1-6alkyl group; R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-6alkyl group optionally substituted with amino, mono- or di(C.sub.1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C.sub.1-6alkyl group or C.sub.1-6 alkoxy group; R.sup.6 is C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.3-7cycloalkylC.sub.1-6alkyl or arylC.sub.1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder mediated by heat shock proteins. ##STR00001##

Disclosed are a novel piperlongumine-based compound, an immuno regulator containing as an active ingredient the compound, or a pharmaceutically acceptable salt or solvate thereof, and a health functional food for immune regulation.

Disclosed are a novel piperlongumine-based compound, an immuno regulator containing as an active ingredient the compound, or a pharmaceutically acceptable salt or solvate thereof, and a health functional food for immune regulation.

Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.

Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.

The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic -quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation.