32 results about "Ponatinib" patented technology

The present disclosure relates to polymorphic forms of the hydrochloride salt of ponatinib (“compound 1”) and to processes for the preparation of these polymorphic forms. The present disclosure also generally relates to a pharmaceutical composition comprising the forms, as well of methods of using the form(s) in the treatment of disorders associated with pathological cellular proliferation, such as neoplasms, and cancer.

The invention relates to a preparation method of a drug for treating chronic granulocytic leukemia, belonging to the field of medical chemistry, and specifically relates to a preparation method of 3-[2-(imidazo[1,2-b] pyridazine-3-yl) acetenyl]-4-methyl-N-{4-[4-methyl piperazine-1-yl] methyl}-3- trifluoromethyl phenyl} benzoyl amide (ponatinib). The method comprises the following steps: adding a phosphine ligand and cesium carbonate at the same time by taking Pd(PPh3)2Cl2 as a catalyst; adding strong base DBU or adding CuI as a cocatalyst to carry out sonagashira reaction, wherein the phosphine ligand is selected from tricyclohexyl phosphine (PCy3), tri-tert-butyl phosphine (PtBu3) or tri(funan-2-yl) phosphine (P(2-furyl)3). The method disclosed by the invention is complete in reaction, does not have or has extremely few diyne byproduct of alkyne coupling, and is easy to separate and purity.

Methods and compositions for treating cancer are disclosed. The compositions comprise immune cells pretreated with ponatinib, or immune cells co-administered with ponatinib, where ponatinib promotes survival and anti-cancer cytotoxicity of the immune cells.

The invention discloses a preparing method of ponatinib. The preparing method of ponatinib comprises the steps of building a reaction system in copper salt and alkaline organic solvent with 3-halogen-parazole [1,5-a]pyrimidine being the starting point, with trimethylsilylacetylene, tetrabutylammonium fluoride and the like being raw materials in sequence and with acridine salt being a photocatalyst, and thus indirectly building a synthesizing path of ponatinib. The synthesis conditions are mild, the cost is low, and the yield of ponatinib is high.

The invention discloses a preparation method for Ponatinib (I). The preparation method comprises the following steps: imidazo [1, 2-b] pyridazine-3-formyl chloride (II) is used as a raw material and subjected to the Friedel-Crafts acylation reaction with 4-methyl benzoic acid (III) to generate an intermediate (IV) being 3-(imidazo[1, 2-b] pyridazine-3-yl)-(4-methyl benzoic acid-3-yl) ketone, the intermediate (IV) is subjected to the Omair-Amos reaction with a Wittig reagent under alkaline condition to obtain an intermediate (V) being 3-(imidazo[1, 2-b] pyridazine-3-ethynyl)-4-methyl benzoic acid, the intermediate (V) is subjected to the amidation reaction with side chain (VI) being 4-((4-methyl piperazine-1-yl)-methyl)-3-(trifluoromethyl) aniline to obtain the Ponatinib (I). According to the preparation method provided by the invention, the raw materials are easy to obtain, the process is concise, and the method is economical and environment-friendly and is suitable for industrial production.

The subject matter described herein is directed to compositions comprising a MEK inhibitor, or a pharmaceutically acceptable salt thereof, and a multi-kinase inhibitor that targets PDGFRα, S6 and STAT3 or a pharmaceutically acceptable salt thereof, and their use in treating pancreatic cancer. In another aspect, disclosed herein are methods of treating pancreatic cancer by administering a MEK inhibitor, or a pharmaceutically acceptable salt thereof, and a multi-kinase inhibitor, or a pharmaceutically acceptable salt thereof. In another aspect, the combination of cobimetinib, or a pharmaceutically acceptable salt thereof, and ponatinib or a pharmaceutically acceptable salt thereof is administered in a composition or the combination is administered separately to treat pancreatic cancer.