Patent classifications
C07F9/6571
A PRODRUG PLATFORM USEFUL TO DELIVER AMINES, AMIDES AND PHENOLS
A prodrug platform is useful to deliver pharmaceutically active amines, amides and phenols and their use in the diagnosis, prevention and/or treatment of various diseases. Compared with the parent drug (e.g., Gemcitabine), the prodrugs show a significant overall safety improvement (therapeutic index (TI) improvement), especially in liver. The prodrugs can treat several diseases, including, for example, cancer, metabolic disease, viral infection, immunological disease, neurologic disease, and blood disease.
CANNABINOID DERIVATIVES
This disclosure relates generally to cannabinoid derivatives, pharmaceutical compositions comprising them, and methods of using the cannabinoid derivatives.
CANNABINOID DERIVATIVES
This disclosure relates generally to cannabinoid derivatives, pharmaceutical compositions comprising them, and methods of using the cannabinoid derivatives.
3,3,3',3'-tetramethyl-1,1'-spirobiindane-based monophosphine ligand, intermediates thereof, preparation method and use of the same
Provided are a 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-based monophosphine ligand and intermediates thereof, and preparation methods and uses of the same. The monophosphine ligand is a compound represented by formula I or formula I′, or an enantiomer, a raceme or a diastereoisomer thereof, including phosphonite ligands, phosphite ligands, phosphoramidite ester ligands, phosphoric acid and phosphonic amide. The monophosphine ligand is prepared with a known 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-7,7′-diol derivative as a raw material through a scheme in which the compound presented by formula II acts as an intermediate. The present disclosure provides a novel monophosphine ligand, which can be used as a ligand in a metal-catalysed organic reactions or in directly catalyzing an organic reaction, especially as a chiral monophosphine ligand widely used in many chiral catalytic reactions such as asymmetric addition, asymmetric hydrogenation, asymmetric coupling, and asymmetric allyl alkylation, having economic practicality and industrial application prospects. ##STR00001##
AKR1C3 INHIBITOR AND MEDICAL USE
Described are compounds that act as AKR1C3 inhibitors or pharmaceutically acceptable salts or solvates or isotopically substituted compounds thereof and methods thereof.
AKR1C3 INHIBITOR AND MEDICAL USE
Described are compounds that act as AKR1C3 inhibitors or pharmaceutically acceptable salts or solvates or isotopically substituted compounds thereof and methods thereof.
Prodrug compounds and their uses
Provided herein are prodrug compounds, their preparation and their uses, such as treating liver diseases or nonliver diseases via intervening in molecular pathways in the liver.
INHIBITORS OF THE ENZYME ENOLASE FOR PRECISION ONCOLOGY
Provided herein are compounds of the formula: wherein the variables are defined herein. The present disclosure also provides pharmaceutical compositions comprising the compounds disclosed herein as well as methods of treatment using the compounds and/or compositions disclosed herein. Such compounds and compositions may be used, for example, for the inhibition of enolase enzymes.
Nucleotide Analogs
Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.
Nucleotide Analogs
Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.