ANTITUMOR EFFECT STRENGTHENING AGENT USING PYRAZOLO[3,4-d]PYRIMIDINE COMPOUND Russian patent published in 2023 - IPC A61K31/519 A61K33/24 A61K45/00 A61P35/00 A61P43/00 C07D487/04 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to an antitumor agent and a combination effective against a malignant tumor including (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof and other antitumor agent, the use of (R)-1-(1-acryloylpiperidin-3-yl) -4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof for enhancing another antitumor agent in the treatment of a malignant tumor, or for the treatment of such a tumor in a patient administering another antitumor agent, or by combined administration with another antitumor agent, the use of (R)-1-(1-acryloylpiperidin-3-yl)-4 -amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof in combination with another antitumor agent to obtain an antitumor agent effective against a malignant tumor, the use of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl )-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof, for the preparation of an antitumor enhancing agent of another antitumor agent, or for the preparation of an antitumor agent for treating a patient with malignant tumor receiving another antitumor agent, the use of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3- dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof for the production of an anticancer agent, comprising another antitumor agent, a method of treating cancer, comprising combined administration (R) -1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d ]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof and another antitumor agent, a method for enhancing the antitumor effect of another antitumor agent in the treatment of cancer, wherein the cancer is associated with HER2 activity and the other antitumor agent is selected from the group consisting of 5-fluorouracil (5-FU), 5-fluoro-2'-deoxyuridine (FdUrd), trifluridine, gemcitabine, capecitabine, trastuzumab, trastuzumab emtansine, AZD8055, everolimus, dactolizib, buparlisib, taselizib, palbociclib, cisplatin and paclitaxel, and where (R)-1 -(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine -3-carboxamide or its pharmaceutically acceptable salt is contained in an amount of from 0.001 to 100 mol per 1 mol of another antitumor agent.

EFFECT: treatment of a malignant tumor associated with HER2 activity using the compound (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof in combination with other antitumor agents mentioned above.

12 cl, 4 dwg, 34 tbl, 4 ex