Patent classifications
C07D239/36
Pyrimidinone derivatives as SHP2 antagonists
The invention relates to pyrimidinone derivatives of the general Formula I, ##STR00001## or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
Pyrimidinone derivatives as SHP2 antagonists
The invention relates to pyrimidinone derivatives of the general Formula I, ##STR00001## or a pharmaceutically acceptable salt thereof, and the use of the compounds of the present invention for the treatment of hyperproliferative diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.
COMPOUNDS AND THEIR USE FOR THE TREATMENT OF ALPHA1-ANTITRYPSIN DEFICIENCY
The invention relates to specified benzamide compounds of formula (1), and pharmaceutical compositions containing the compounds. The compounds may be inducers of α.sub.1-antitrypsin (A1AT), and may be used in the treatment of a disease or disorder such as α.sub.1-antitrypsin deficiency (A1AD or AATD).
MODULATORS OF HSD17B13 AND METHODS OF USE THEREOF
The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.
MODULATORS OF HSD17B13 AND METHODS OF USE THEREOF
The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.
METHOD FOR THE SYNTHESIS OF 2,4-DIMETHYLPYRIMIDIN-5-OL, INTERMEDIATES, AND METHOD FOR THE SYNTHESIS OF LEMBOREXANT USING THE INTERMEDIATES
A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.
METHOD FOR THE SYNTHESIS OF 2,4-DIMETHYLPYRIMIDIN-5-OL, INTERMEDIATES, AND METHOD FOR THE SYNTHESIS OF LEMBOREXANT USING THE INTERMEDIATES
A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
Compounds which are inhibitors of Notum
A compound for use in the treatment of a disease ameliorated by the inhibition of Notum of formula (I): (I) ##STR00001##