Patent classifications
C07D211/86
METHODS FOR ENANTIOSELECTIVE ALLYLIC ALKYLATION OF ESTERS, LACTONES, AND LACTAMS WITH UNACTIVATED ALLYLIC ALCOHOLS
The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic -quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation.
1',3'-Disubstituted-4-Phenyl-3,4,5,6-Tetrahydro-2H,1'H-[1,4']Bipyridinyl-2'-Ones
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I)
##STR00001##
wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptorssubtype 2 (mGluR2) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
1',3'-Disubstituted-4-Phenyl-3,4,5,6-Tetrahydro-2H,1'H-[1,4']Bipyridinyl-2'-Ones
The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I)
##STR00001##
wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptorssubtype 2 (mGluR2) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
NOVEL SUBSTITUTED GLYCINE DERIVED FXIA INHIBITORS
The present invention provides compounds of Formula (I): (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
##STR00001##
NOVEL SUBSTITUTED GLYCINE DERIVED FXIA INHIBITORS
The present invention provides compounds of Formula (I): (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
##STR00001##
PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING VIRAL INFECTIONS CONTAINING PIPERLONGUMINE-BASED COMPOUND AS ACTIVE INGREDIENT
The present disclosure relates to a pharmaceutical composition for preventing or treating viral infections, containing a piperlongumine-based compound as an active ingredient. Specifically, the piperlongumine-based compound according to the present disclosure inhibits SARS-CoV-2 infection, and thus can be useful for treating viral infections, particularly RNA viral infections.
INHIBITORS OF THE WNT/BETA-CATENIN PATHWAY
The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.
INHIBITORS OF THE WNT/BETA-CATENIN PATHWAY
The present disclosure relates to compounds that are capable of modulating the WNT/Beta-Catenin pathway. The disclosure further relates to methods of treating colorectal cancer and other WNT/Beta-Catenin mediated cancers.
Enhancer of Zeste Homolog 2 inhibitors
This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. ##STR00001##
Enhancer of Zeste Homolog 2 inhibitors
This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. ##STR00001##