A61K31/4748

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

Bupropion as a modulator of drug activity
11590124 · 2023-02-28 · ·

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Bupropion as a modulator of drug activity
11590124 · 2023-02-28 · ·

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

TETRAHYDROISOQUINOLINES AS SELECTIVE NADPH OXIDASE 2 INHIBITORS

Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein “custom-character” represents a single or double bond, R.sup.1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.a is hydrogen, —CH.sub.2R.sup.2, R.sup.3, or —SO.sub.2R.sup.4; R.sup.2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.4 is lower aliphatic, or substituted or unsubstituted aryl; and R.sup.5 is hydrogen, halogen, or lower aliphatic.

TETRAHYDROISOQUINOLINES AS SELECTIVE NADPH OXIDASE 2 INHIBITORS

Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein “custom-character” represents a single or double bond, R.sup.1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.a is hydrogen, —CH.sub.2R.sup.2, R.sup.3, or —SO.sub.2R.sup.4; R.sup.2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.4 is lower aliphatic, or substituted or unsubstituted aryl; and R.sup.5 is hydrogen, halogen, or lower aliphatic.

Theacrine-based supplement and method of use thereof in a synergistic combination with caffeine

A human dietary supplement comprises theacrine and optionally other compounds that modulate the effects of theacrine. Uses for the theacrine-containing supplement include improvement of at least one of mood, energy, focus, concentration or sexual desire or a reduction of at least one of anxiety or fatigue. A synergistic composition comprises co-administration of theacrine and caffeine, wherein the co-administered caffeine reduces theacrine oral clearance (CL/F) and oral volume of distribution (Vd/F). In addition, the co-administered caffeine increases area under the plasma concentration time curve (AUC) of theacrine, and increases theacrine maximum plasma concentration (C.sub.max) in comparison with the corresponding pharmacokinetic parameters when theacrine is administered alone.

Theacrine-based supplement and method of use thereof in a synergistic combination with caffeine

A human dietary supplement comprises theacrine and optionally other compounds that modulate the effects of theacrine. Uses for the theacrine-containing supplement include improvement of at least one of mood, energy, focus, concentration or sexual desire or a reduction of at least one of anxiety or fatigue. A synergistic composition comprises co-administration of theacrine and caffeine, wherein the co-administered caffeine reduces theacrine oral clearance (CL/F) and oral volume of distribution (Vd/F). In addition, the co-administered caffeine increases area under the plasma concentration time curve (AUC) of theacrine, and increases theacrine maximum plasma concentration (C.sub.max) in comparison with the corresponding pharmacokinetic parameters when theacrine is administered alone.

Theacrine-based supplement and method of use thereof in a synergistic combination with caffeine

A human dietary supplement comprises theacrine and optionally other compounds that modulate the effects of theacrine. Uses for the theacrine-containing supplement include improvement of at least one of mood, energy, focus, concentration or sexual desire or a reduction of at least one of anxiety or fatigue. A synergistic composition comprises co-administration of theacrine and caffeine, wherein the co-administered caffeine reduces theacrine oral clearance (CL/F) and oral volume of distribution (Vd/F). In addition, the co-administered caffeine increases area under the plasma concentration time curve (AUC) of theacrine, and increases theacrine maximum plasma concentration (C.sub.max) in comparison with the corresponding pharmacokinetic parameters when theacrine is administered alone.

Method for increasing the lifespan and motility of animal sperm using an inhibitor of Slo3 potassium channel

The invention relates to a method for increasing the lifespan of animal sperm comprising contacting said sperm with an inhibitor of Slo3 potassium channel. The invention also relates to a use of an inhibitor of Slo3 potassium channel, for increasing the lifespan of animal sperm or motility of capacitated animal sperm, comprising contacting an inhibitor of Slo3 potassium channel with said sperm. Moreover, the invention relates to an artificial insemination instrument for use in artificial insemination of an animal, comprising animal sperm in contact with an inhibitor of Slo3 potassium channel. The invention also relates to a method for artificially inseminating an animal using said artificial insemination instrument. Eventually, the invention relates to a method for increasing the fertility of an animal, comprising contacting sperm of said animal with an inhibitor of Slo3 potassium channel; then artificially inseminating said animal with said sperm.