Patent classifications
C07D207/26
DEUTERATED PROTEASE INHIBITORS
Compounds and treatment methods with compounds exhibiting antiviral activity and/or inhibition of viral replication against viruses, particularly those belonging to the picornavirus-like supercluster, including coronavirus having a formula:
##STR00001##
or a prodrug or pharmaceutically-acceptable salt thereof, where: each X comprises at least one cyclic moiety directly attached to the oxygen or connected via an alkyl linkage, where at least one of the linkage and/or the X moiety comprises a deuterium substitution; and Z is selected from the group consisting of aldehydes and bisulfite salts, or the ester or carbamate prodrugs thereof.
METHOD FOR PURIFYING WASTE N-METHYL-2-PYRROLIDONE MIXTURE SOLUTION
A method for purifying a waste N-methyl-2-pyrrolidone (NMP) mixed solution according to an embodiment of the present disclosure includes using a base. The base according to an embodiment may be NaBH.sub.4. N-methylsuccinimide and γ-butyrolactone are simultaneously removed, and high-purity NMP can be recovered by applying a base to the waste NMP mixed solution.
METHOD FOR PURIFYING WASTE N-METHYL-2-PYRROLIDONE MIXTURE SOLUTION
A method for purifying a waste N-methyl-2-pyrrolidone (NMP) mixed solution according to an embodiment of the present disclosure includes using a base. The base according to an embodiment may be NaBH.sub.4. N-methylsuccinimide and γ-butyrolactone are simultaneously removed, and high-purity NMP can be recovered by applying a base to the waste NMP mixed solution.
PHARMACEUTICAL COMPOSITIONS COMPRISING POH DERIVATIVES
The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
PHARMACEUTICAL COMPOSITIONS COMPRISING POH DERIVATIVES
The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
Inhibitors of cysteine proteases and methods of use thereof
The disclosure provides compounds, such as compounds of Formula II, with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease. ##STR00001##
Inhibitors of cysteine proteases and methods of use thereof
The disclosure provides compounds, such as compounds of Formula II, with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease. ##STR00001##
GEM-DISUBSTITUTED PYRROLIDINES, PIPERAZINES, AND DIAZEPANES, AND COMPOSITIONS AND METHODS OF MAKING THE SAME
Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).
GEM-DISUBSTITUTED PYRROLIDINES, PIPERAZINES, AND DIAZEPANES, AND COMPOSITIONS AND METHODS OF MAKING THE SAME
Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).
Activation of carbonyl beta-carbons for chemical transformations
The present invention relates to a method for synthesizing a compound of Formula (I) ##STR00001## as defined herein, comprising: (i) activating a compound of Formula (II) ##STR00002## as defined herein, by reacting said compound of Formula (II) with a compound of Formula (III) ##STR00003## as defined herein, in the presence of a base, to obtain a compound of Formula (IV) ##STR00004## as defined herein; and (ii) reacting the compound of Formula (IV) with an electrophile to obtain the compound of Formula (I). The present invention further relates to the organocatalysts used in the described methods and their respective uses.