Patent classifications
C07C233/66
Process for deoxyfluorination of phenols
The present invention refers to a process for transition-metal-assisted .sup.18F-deoxyfluorination of phenols. The transformation benefits from readily available phenols as starting materials, tolerance of moisture and ambient atmosphere, large substrate scope, and translatability to generate doses appropriate for positron emission tomography (PET) imaging.
HEPATITIS B CAPSID ASSEMBLY MODULATORS
Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.
COMPOUNDS AND METHODS FOR HEMATOPOIETIC REGENERATION
The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention.
COMPOUNDS AND METHODS FOR HEMATOPOIETIC REGENERATION
The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention.
PREPARATION METHOD FOR M-DIAMIDE COMPOUNDS
The present disclosure provides a preparation method for m-diamide compounds. The method includes the following steps: 2-fluoro-3-nitrobenzoyl chloride and 4-(perfluoropropane-2-yl)-2-(trifluoromethyl)aniline are subjected to a condensation reaction, followed by a reduction reaction and an alkylation reaction to give 2-fluoro-3-(alkylamino)-N-(4-(perfluoropropane-2-yl)-2-(trifluoromethyl)phenyl)benzamide, which reacts with an acyl chloride compound to give 2-fluoro-3-(alkylbenzamido)-N-(4-(perfluoropropane-2-yl)-2-(trifluoromethyl)phenyl)benzamide, which is finally brominated to obtain the m-diamide compound. The reactions are almost quantitative with few by-products. Cryogenic and high-temperature reactions are not used. The introduction of bromine atoms at specific sites can be achieved in the final step. The preparation method has high yield and is more suitable for industrial production.
PREPARATION METHOD FOR M-DIAMIDE COMPOUNDS
The present disclosure provides a preparation method for m-diamide compounds. The method includes the following steps: 2-fluoro-3-nitrobenzoyl chloride and 4-(perfluoropropane-2-yl)-2-(trifluoromethyl)aniline are subjected to a condensation reaction, followed by a reduction reaction and an alkylation reaction to give 2-fluoro-3-(alkylamino)-N-(4-(perfluoropropane-2-yl)-2-(trifluoromethyl)phenyl)benzamide, which reacts with an acyl chloride compound to give 2-fluoro-3-(alkylbenzamido)-N-(4-(perfluoropropane-2-yl)-2-(trifluoromethyl)phenyl)benzamide, which is finally brominated to obtain the m-diamide compound. The reactions are almost quantitative with few by-products. Cryogenic and high-temperature reactions are not used. The introduction of bromine atoms at specific sites can be achieved in the final step. The preparation method has high yield and is more suitable for industrial production.
INHIBITORS OF THE RAS ONCOPROTEIN, METHODS OF MAKING AND METHODS OF USE THEREOF
A compound for use in treating a disease associated with activating mutations in RAS, or for use in treating a disease treatable by a reduction in RAS activity, is selected from a compound of Formula (I), salts and esters thereof. The compounds are particularly useful in treating cancer.
##STR00001##
Diabetes and metabolic syndrome treatment with a novel dual modulator of soluble epoxide hydrolase and peroxisome proliferator-activated receptors
N-benzylbenzamides that act as dual soluble soluble epoxide hydrolase (sEH)/peroxisome proliferator-activated receptor (PPAR) modulators and are useful as medications in the treatment of Metabolic Syndrome (MetS) cluster diseases, including diabetes. Methods of making and using the same are further provided.
Diabetes and metabolic syndrome treatment with a novel dual modulator of soluble epoxide hydrolase and peroxisome proliferator-activated receptors
N-benzylbenzamides that act as dual soluble soluble epoxide hydrolase (sEH)/peroxisome proliferator-activated receptor (PPAR) modulators and are useful as medications in the treatment of Metabolic Syndrome (MetS) cluster diseases, including diabetes. Methods of making and using the same are further provided.
MCT4 inhibitors and uses thereof
Presented herein are MCT4 inhibitors and uses thereof for treating cancer.