Patent classifications
C07D211/90
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.
Prodrugs of glutamine analogs
The disclosure provides compounds having formula (I): ##STR00001##
and the pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.2, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.
Prodrugs of glutamine analogs
The disclosure provides compounds having formula (I): ##STR00001##
and the pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.2, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.
POTENT AND SELECTIVE INHIBITORS OF THE CALCIUM-ACTIVATED POTASSIUM CHANNEL, KCA3.1, FOR USE AS PLATFORM THERAPEUTICS
Provided is the use of compounds of Formula I, as well as certain specific compounds, or a pharmaceutically acceptable salt, solvate or derivative thereof, in the preparation of a medicament to treat or prevent a disease condition that is associated with increased K.sub.Ca3.1 or altered activity, such as stroke.
POTENT AND SELECTIVE INHIBITORS OF THE CALCIUM-ACTIVATED POTASSIUM CHANNEL, KCA3.1, FOR USE AS PLATFORM THERAPEUTICS
Provided is the use of compounds of Formula I, as well as certain specific compounds, or a pharmaceutically acceptable salt, solvate or derivative thereof, in the preparation of a medicament to treat or prevent a disease condition that is associated with increased K.sub.Ca3.1 or altered activity, such as stroke.
KETAMINE DERIVATIVES AND COMPOSITIONS THEREOF
Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.
Quaternary heteroatom containing compounds
The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): ##STR00001##
comprising treating a compound of Formula (I): ##STR00002##
with a transition metal catalyst and under alkylation conditions as valence and stability permit.
Quaternary heteroatom containing compounds
The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): ##STR00001##
comprising treating a compound of Formula (I): ##STR00002##
with a transition metal catalyst and under alkylation conditions as valence and stability permit.
COMPOUNDS HAVING INHIBITORY EFFECT ON MITOCHONDRIAL HYPERFISSION
The present invention provides a compound for treating or preventing diseases caused by mitochondrial hyperfission.
The present invention provides a compound represented by formula (1):
##STR00001## wherein R.sub.1 and R.sub.1 are each independently hydrogen, an optionally substituted lower alkyl, an optionally substituted lower cycloalkyl, and the like; R.sub.2 is an optionally substituted lower alkyl, an optionally substituted lower cycloalkyl, and the like; R.sub.3 and R.sub.4 are each independently hydrogen, halogen, hydroxy, nitro, cyano, an optionally substituted lower alkyl, and the like; R.sub.5 and R.sub.6 are each independently an optionally substituted lower alkyl; an optionally substituted lower cycloalkyl, and the like; X is nitrogen or oxygen; Y is carbon, nitrogen or oxygen; and a broken line represents the presence or absence of a bond; or a pharmaceutically acceptable salt, a solvate, or a prodrug thereof.