Patent classifications
C07D211/90
Arylhydrazides containing a 2-pyridone moiety as selective antibacterial agents
The present invention belongs to the field of antibacterial agents, more specifically to antibacterials for treating Acinetobacter baumannii infections. The invention provides arylhydrazides containing a 2-pyridone moiety, according to formula (I), which show selective antibacterial activity against A. baumannii. The invention also relates to their use as medicaments and specifically as antibacterials for the treatment of A. baumannii infections, as well as to a process for their preparation and to pharmaceutical compositions containing them. ##STR00001##
Dihydropyridinone MGAT2 inhibitors
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.
Dihydropyridinone MGAT2 inhibitors
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.
SMALL MOLECULE INHIBITORS OF NECROPTOSIS
The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF- induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
SMALL MOLECULE INHIBITORS OF NECROPTOSIS
The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF- induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
ARYL DIHYDROPYRIDINONES AND PIPERIDINONE MGAT2 INHIBITORS
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.
ARYL DIHYDROPYRIDINONES AND PIPERIDINONE MGAT2 INHIBITORS
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.
2-OXO-3,4-DIHYDROPYRIDINE-5-CARBOXYLATES AND THEIR USE
The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.
##STR00001##
2-OXO-3,4-DIHYDROPYRIDINE-5-CARBOXYLATES AND THEIR USE
The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.
##STR00001##
NOVEL COMPOUNDS AND METHODS OF TREATING OR AMELIORATING AN IL-1R-MEDIATED DISEASE OR DISORDER USING SAME
The present invention provides compounds useful for treating or preventing an IL-1R-mediated disease or disorder. In certain embodiments, the disease or disorder comprises scleroderma.