64 results about "Indacaterol" patented technology

The invention relates to new and improved processes for the preparation of Indacaterol and pharmaceutically acceptable salts thereof as well as intermediates for the preparation of Indacaterol. The new process avoids the use of the epoxide compound known in the art and the impurities associated therewith and results in a higher yield.

The invention discloses a synthesizing method of an indacaterol amino fragment 5,6-diethyl-2,3-dihydro-1H-inden-2-amine hydrochloride. According to the invention, ethylbenzene I is adopted as a raw material, and a Friedel-Crafts reaction is carried out, such that a compound II is obtained; the compound II is subjected to cyclization, such that ethylindene III is obtained; ethylindene III is subjected to alpha-site oximation reaction, such that a compound IV is obtained; the compound IV is subjected to RaneyNi reduction, such that a compound V is obtained; the compound V is processed with a Tf-protection and sodium borohydride reduction one-pot method, such that a compound VI is obtained; the compound VI is subjected to a Friedel-Crafts reaction, such that a compound VII is obtained; the compound VII is reduced, such that a compound VIII is obtained; and the compound VIII is subjected to protection removing and hydrochloride salt formation, such that a final product compound IX is obtained, and the 5,6-diethyl-2,3-dihydro-1H-inden-2-amine hydrochloride is obtained. The method provided by the invention is simple and convenient, and has low cost. The content of the product is higher than 99%. The method also has the advantages of low environmental pollution and suitability for industrialized production.

A novel process the for preparation of Indacaterol or its pharmaceutically acceptable salts and novel intermediates employed in the preparation thereof that is economically significant for large scale.

The invention discloses an application of indacaterol in the treatment of colorectal cancer, and belongs to the field of molecular biology, in particular, tumor treatment. Specifically, indacaterol selected from disclosed drugs can treat colorectal cancer. The results of cell experiments and animal experiments show that indacaterol can inhibit the proliferation, invasion and migration of colorectal tumor cell lines, and can obviously reduce the size of colorectal tumors of a mouse model. At the same time, for the first time, people find that indacaterol corrects the alternative splicing of tumor cells to achieve the effects mentioned above.

The present invention discloses a liquid, propellant-free pharmaceutical formulation and a method of administering the pharmaceutical formulation by nebulizing the pharmaceutical formulation in an inhaler. The liquid, propellant-free pharmaceutical preparation includes: (a) an active substance selected from glycopyrronium bromide and indacaterol maleate; (b) a solvent; (c) a pharmaceutically acceptable preservative, any Optionally include a pharmaceutically acceptable stabilizer, a pharmaceutically acceptable solubilizer, a pharmaceutically acceptable co-solvent or other pharmaceutically acceptable additives.