5 results about "Bosentan" patented technology

This invention provides a combination therapy method to increase the effectiveness of cancer immunotherapy. [Solution] The present invention provides a combination therapy using bosentan and a checkpoint inhibitor that is effective in treating cancer in a target or inhibiting the proliferation of tumor cells, and / or can induce, enhance, or prolong an immune response against tumor cells. The effectiveness of cancer immunotherapy depends on whether T cells can migrate to the tumor, travel to locations adjacent to malignant cells, recognize them, and kill them.

The application belongs to the technical field of medicines. A bexarotene pharmaceutical cocrystal, a preparation method and application thereof are provided. Specifically, the application discloses a method for forming a cocrystal of bexarotene and L-arginine in a molar ratio of 1:1 or 1:2 by using a grinding method in combination; the cocrystal reduces the melting point and improves the solubility of bexarotene on the basis of retaining the drug activity of bexarotene; and the application of the bexarotene and L-arginine cocrystal as a pharmaceutically active ingredient in the preparation of a drug for preventing and treating pulmonary arterial hypertension.

The application provides a preparation method of bosentan, which comprises the following steps: mixing phosphorus oxychloride and 5-(2-methoxyphenoxy)-[2,2'-bipyrimidine]-4,6(1H,5H)-dione, reacting to obtain 4,6-dichloro-5-(2-methoxyphenoxy)-2,2'-bipyrimidine; then mixing the 4,6-dichloro-5-(2-methoxyphenoxy)-2,2'-bipyrimidine with 4-tert-butylbenzenesulfonamide, an acid binding agent and a polar aprotic solvent, and reacting to obtain 4-tert-butyl-N-[6-chloro-5-(2-methoxyphenoxy)-4-pyrimidinyl]benzenesulfonamide potassium salt; then mixing the 4-tert-butyl-N-[6-chloro-5-(2-methoxyphenoxy)-4-pyrimidinyl]benzenesulfonamide potassium salt with ethylene glycol, an alkali metal hydroxide and tetrahydrofuran to obtain a bosentan precursor; and finally mixing the bosentan precursor with ethanol and water, reacting, cooling and crystallizing to obtain bosentan. The preparation method of bosentan can greatly save reaction time, improve reaction yield, reduce impurity content, simplify post-treatment operation, reduce preparation cost and be convenient for industrial large-scale production and application.

The present application belongs to the technical field of medicine, and particularly relates to a pharmaceutical composition and use thereof. The pharmaceutical composition composed of a PGI2 receptor agonist compound or a pharmaceutical salt thereof and bosentan has a synergistic effect on inhibiting K+ induced pulmonary artery ring tension increase and / or inhibiting PDGF induced human pulmonary artery smooth muscle cell proliferation. The combined pharmaceutical composition is more helpful for treating the disease of a patient with pulmonary arterial hypertension which cannot be controlled by a single drug. The combined pharmaceutical composition has a stronger synergistic effect on inhibiting K+ induced pulmonary artery ring tension increase and / or inhibiting PDG induced human pulmonary artery smooth muscle cell proliferation than the combined use of the existing drug selexipag and bosentan at a specific ratio and test concentration. Therefore, the combined pharmaceutical composition at a specific ratio and test concentration is more helpful for treating the disease of a patient with moderate to severe pulmonary arterial hypertension which cannot be controlled by the combined use of the existing drug selexipag and bosentan.

A Bosentan micro-tablet, comprising: a compound I having the following structural formula or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable excipient for preparing a dispersible micro-tablet. The micro-tablet can meet the medication requirements of children for Bosentan, achieve accurate administration, and minimize the side effects of drugs.