A61K31/4706

Substituted crotonamide pharmaceutical composition and preparation method therefor
20230000855 · 2023-01-05 ·

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
20230000854 · 2023-01-05 ·

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
20230000854 · 2023-01-05 ·

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
20230022696 · 2023-01-26 ·

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
20230022696 · 2023-01-26 ·

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
20230226149 · 2023-07-20 ·

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.