Patent classifications
A61K38/06
SMALL MOLECULE INHIBITORS OF SARS-CoV-2 VIRAL REPLICATION AND USES THEREOF
This invention is in the field of medicinal pharmacology. In particular, the present invention relates to pharmaceutical agents which function as inhibitors of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral replication and/or SARS-CoV-2 related viral 3CL protease (M.sup.pro) activity. The invention further relates to methods of treating and/or ameliorating symptoms related to conditions caused by the SARS-CoV-2 virus (e.g., COVID-19), comprising administering to a subject (e.g., a human patient) a composition comprising one or more pharmaceutical agents which function as inhibitors of SARS-CoV-2 viral replication and/or inhibitors of SARS-CoV-2 related M.sup.pro activity.
COMPOSITIONS AND METHODS FOR THE TREATMENT AND PREVENTION OF VASCULAR MALFORMATIONS
Provided herein are methods and compositions for treating and preventing vascular malformations including lymphatic, venous, capillary, arteriovenous, and combinations thereof. Methods of treatment and prevention include the administration of proteasome inhibitors, omipalisib, disulfiram, and agents which target genes in the PI3K/AKT/mTOR or RAS/RAF/MAPK pathways, including but not limited to Pik3ca, Pik3r3, Tsc2, Rasa1, Map2k2, and Glmn.
COMPOSITIONS AND METHODS FOR THE TREATMENT AND PREVENTION OF VASCULAR MALFORMATIONS
Provided herein are methods and compositions for treating and preventing vascular malformations including lymphatic, venous, capillary, arteriovenous, and combinations thereof. Methods of treatment and prevention include the administration of proteasome inhibitors, omipalisib, disulfiram, and agents which target genes in the PI3K/AKT/mTOR or RAS/RAF/MAPK pathways, including but not limited to Pik3ca, Pik3r3, Tsc2, Rasa1, Map2k2, and Glmn.
NUTRITIONAL HEALTH SUPPLEMENTS
A nutritional health supplement is provided for the brain. In one exemplary embodiment, a nutritional health supplement comprises a first neuroprotective agent having antioxidant, anti-inflammatory, anti-apoptic, anti-autophagic, and anti-cerebral edema properties, and having calcium-induced apoptotic signaling-inhibiting properties; a second neuroprotective agent having glutamate-mediated excitotoxicity-mitigating and calcium influx-mitigating properties and having antioxidant and blood-brain barrier protecting properties; a third neuroprotective agent that is a precursor for glutathione synthesis and has calcium influx-mitigating and anti-oxidative stress mediating properties and that augments the first neuroprotective agent's calcium-induced apoptotic signaling-inhibiting properties and anti-cerebral edema properties and the second neuroprotective agent's antioxidant properties; a NAD+ precursor that augments the first neuroprotective agent's anti-apoptotic properties, the second neuroprotective agent's glutamate-mediated excitotoxicity-mitigating and blood-brain barrier protecting properties, and the third neuroprotective agent's calcium influx-mitigating and anti-oxidative stress mediating properties. The second neuroprotective agent augments the third neuroprotective agent's calcium influx-reducing property.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
Tripeptide Propylene Oxide Derivative and Preparation Method and Application thereof
The present invention discloses a tripeptide propylene oxide derivative or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The structure of the tripeptide propylene oxide derivative is shown in formula I. Compared with the prior art, the present invention provides tripeptide epoxy ketone compounds with a novel structure and a function of inhibiting proteasome. As 20S proteasome inhibitors, the tripeptide epoxy ketone compounds can block tumor cell proliferation and induce tumor cell apoptosis, so the tripeptide epoxy ketone compounds can be used for the treatment and prevention of a plurality of human and animal diseases such as malignant tumors, and the effect is significantly better.
Tripeptide Propylene Oxide Derivative and Preparation Method and Application thereof
The present invention discloses a tripeptide propylene oxide derivative or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The structure of the tripeptide propylene oxide derivative is shown in formula I. Compared with the prior art, the present invention provides tripeptide epoxy ketone compounds with a novel structure and a function of inhibiting proteasome. As 20S proteasome inhibitors, the tripeptide epoxy ketone compounds can block tumor cell proliferation and induce tumor cell apoptosis, so the tripeptide epoxy ketone compounds can be used for the treatment and prevention of a plurality of human and animal diseases such as malignant tumors, and the effect is significantly better.