Patent classifications
A61K31/4706
Substituted crotonamide pharmaceutical composition and preparation method therefor
A composition of substituted crotonamide pharmaceutical and a preparation method therefor. The pharmaceutical composition comprises 5-50 parts of (E)-N-(3-cyano-7-ethoxy-4-(3-ethynylphenylamino)quinolin-6-yl)-4-(dimethylamino)but-2-enamide maleate, 40-120 parts of a filler, 2-20 parts of a disintegrant, 0-6 parts of an adhesive, and 0.5-5 parts of a lubricant. The filler is selected from carbohydrates.
Application of substituted crotonamide
An application of a substituted crotonamide, in particular being an application of (E)-N-(3-cyano-7-ethoxyl-4-(3-ethynylphenylamino)quinoline-6-yl)-4-(dimethylamino)but-2-enamide and a pharmaceutically acceptable salt and solvate thereof in the preparation of a drug for treating cancer mediated by a rare EGFR mutation.
Application of substituted crotonamide
An application of a substituted crotonamide, in particular being an application of (E)-N-(3-cyano-7-ethoxyl-4-(3-ethynylphenylamino)quinoline-6-yl)-4-(dimethylamino)but-2-enamide and a pharmaceutically acceptable salt and solvate thereof in the preparation of a drug for treating cancer mediated by a rare EGFR mutation.
Chloroquine gel and preparation method and application thereof
A product for preventing and treating external genitalia infection and/or flat warts is provided, wherein the product comprises a chloroquine nanosphere. The chloroquine nanosphere comprises a water-soluble nanosphere carrier, and chloroquine or a chloroquine derivative. A mass ratio of the chloroquine or the chloroquine derivative to the water-soluble nanosphere carrier during preparation ranges from 1:3 to 1:5. A loading rate of the chloroquine or the chloroquine derivative in the prepared chloroquine nanosphere ranges from 3.0% to 21.6%. The water-soluble nanosphere carrier is water-soluble chitosan; a deacetylation degree of the water-soluble chitosan ranges from 80% to 95%, and a viscosity-average molecular weight thereof ranges from 3000 to 5000 g/mol. The chloroquine derivative is selected from one or more of hydroxychloroquine, chloroquine phosphate or chloroquine sulfate.
Chloroquine gel and preparation method and application thereof
A product for preventing and treating external genitalia infection and/or flat warts is provided, wherein the product comprises a chloroquine nanosphere. The chloroquine nanosphere comprises a water-soluble nanosphere carrier, and chloroquine or a chloroquine derivative. A mass ratio of the chloroquine or the chloroquine derivative to the water-soluble nanosphere carrier during preparation ranges from 1:3 to 1:5. A loading rate of the chloroquine or the chloroquine derivative in the prepared chloroquine nanosphere ranges from 3.0% to 21.6%. The water-soluble nanosphere carrier is water-soluble chitosan; a deacetylation degree of the water-soluble chitosan ranges from 80% to 95%, and a viscosity-average molecular weight thereof ranges from 3000 to 5000 g/mol. The chloroquine derivative is selected from one or more of hydroxychloroquine, chloroquine phosphate or chloroquine sulfate.
SMALL MOLECULE INHIBITORS OF AUTOPHAGY AND HISTONE DEACTYLASES AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinoline or thioxanthenone (or similar) structure which function as autophagy inhibitors and/or histone deactylase inhibitors, and their use as therapeutics for the treatment of conditions characterized with aberrant autophagy activity and/or aberrant HDAC activity (e.g., cancer, pulmonary hypertension, diabetes, neurodegenerative disorders, aging, heart disease, rheumatoid arthritis, infectious diseases, conditions and symptoms caused by a viral infection (e.g., COVID-19)).
SMALL MOLECULE INHIBITORS OF AUTOPHAGY AND HISTONE DEACTYLASES AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinoline or thioxanthenone (or similar) structure which function as autophagy inhibitors and/or histone deactylase inhibitors, and their use as therapeutics for the treatment of conditions characterized with aberrant autophagy activity and/or aberrant HDAC activity (e.g., cancer, pulmonary hypertension, diabetes, neurodegenerative disorders, aging, heart disease, rheumatoid arthritis, infectious diseases, conditions and symptoms caused by a viral infection (e.g., COVID-19)).
METHOD FOR TREATING GEFITINIB RESISTANT CANCER
The present invention is directed to methods for the treatment of gefitinib and/or erlotinib resistant cancer. An individual with cancer is monitored for cancer progression following treatment with gefitinib and/or erlotinib. Progression of the cancer is indicative that the cancer is resistant to gefitinib and/ or erlotinib. Once progression of cancer is noted, the subject is administered a pharmaceutical composition comprising an irreversible epidermal growth factor receptor (EGFR) inhibitor. In preferred embodiments, the irreversible EGFR inhibitor is EKB-569, HKI-272 and HKI-357.
METHOD FOR TREATING GEFITINIB RESISTANT CANCER
The present invention is directed to methods for the treatment of gefitinib and/or erlotinib resistant cancer. An individual with cancer is monitored for cancer progression following treatment with gefitinib and/or erlotinib. Progression of the cancer is indicative that the cancer is resistant to gefitinib and/ or erlotinib. Once progression of cancer is noted, the subject is administered a pharmaceutical composition comprising an irreversible epidermal growth factor receptor (EGFR) inhibitor. In preferred embodiments, the irreversible EGFR inhibitor is EKB-569, HKI-272 and HKI-357.
MODIFIED CAVEOLIN-1 PEPTIDES FOR THE TREATMENT OF PATHOGEN-INDUCED LUNG INJURY
Provided herein are methods of using modified caveolin-1 (Cav-1) peptides to treat or prevent pathogen-induced lung injury and disrepair. In particular, provided are methods of using the modified Cav-1 peptides for the treatment of pathogen-induced lung injury and disrepair caused by a coronavirus, such as, for example, SARS-CoV-2.