63 results about "Indacaterol" patented technology

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.

The invention relates to an indacaterol intermediate salt and a preparation method thereof, and the preparation method of the indacaterol intermediate salt has the advantages of simple operation, low cost, good reproducibility and easy realization, and is suitable for industrial production.

The invention relates to liquor containing indacaterol maleate. The content of the indacaterol maleate is 2.0 mug/ml-15 mug/ml; while being used, content can be released in the forms of mists by virtue of pressure of a manual pump, ultrasonic spraying, an air compressor, and the like, and can be used for lung inhalation administration. The invention specifically relates to inhalation spray containing the indacaterol maleate.

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 relates to a preparation process of a compound dry powder inhaler for glucocorticoids and beta2 receptor agonists. The process comprises the following steps: (a) performing micronizationon glucocorticoids and beta2 receptor agonists; (b) mixing the micronized product in the step (a) with a drug carrier, or mixing the micronized product in the step (a) with a drug carrier and an additive; and (c) adding the composition in the step (b) into a sample handling room for handling, thereby obtaining the pharmaceutical composition of the dry powder inhaler. The sample handling room is an environment of which the humidity is 45-75% or an environment of which the pressure is not higher than 500Pa; the handling time is 2-72 hours; the glucocorticoids are mometasone furoate or pharmaceutically acceptable salts thereof; and the beta2 receptor agonists are indacaterol or pharmaceutically acceptable salts thereof. The process disclosed by the invention is simple, convenient to operateand low in production cost.

The invention relates to a preparation method of indacaterol maleate, in particular, the indacaterol maleate is prepared from 8-benzyloxy-5-(2-bromoacetyl)-2-hydroxyquinoline, (R)-2-methyl-CBS-oxazolidine borane, tert-butyldimethylsilyl trifluoromethanesulfonate, 5,6-diethyl-2,3-dihydro-1H-2-amine hydrochloride, palladium/carbon and maleic acid as raw materials through four-step reaction of chiralreduction reaction, TBS hydroxyl protection reaction, condensation reaction and hydrogenation reduction reaction, and the preparation method of the indacaterol maleate provided by the invention is high in yield, low in cost, environmentally friendly, easy to operate, and suitable for industrial 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 provides an indacaterol tablet and a preparation method thereof. According to the method, the indacaterol tablet is prepared in a manner that the powder is directly pressed to form the tablet. Thus, the production process is simple; the production cycle is shortened; and the equipment cost and the operating cost are lowered. The prepared indacaterol tablet is good in appearance, smooth in technological process, good in operability as well as high in dissolubility and has the qualified content uniformity; and the good bioavailability of the indacaterol tablet in a human body is realized. Thus, a good treatment effect is obtained.

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 invention specifically relates to a preparation method for indacaterol maleate, belonging to the field of drug synthesis. The preparation method is simple and short in steps, easy to operate, safe, friendly to environment and fee of an alkaline solution; after a heating reaction, a coupled product in the step 1) can be obtained, and the amount of produced regioisomers, dimers and other by-products is small; the yield of the product indacaterol maleate is high, as high as 93%, and the HPLC purity of the product indacaterol maleate is more than 97.8%; post-treatment is simple, and industrialproduction of indacaterol maleate is facilitated; and the product indacaterol maleate is high in optical purity.

The invention relates to a combination of inhaled / oral roflumilast or its pharmaceutically acceptable salt combined with inhaled indacaterol or its pharmaceutically acceptable salt, and the pharmaceutical combined product is used for simultaneous, successive or respective drug administration, is used for treatment or prevention of respiratory tract disease or its symptoms, and is especially used for treatment of obstruction or inflammation-accompanying diseases such as chronic obstructive pulmonary disease (COPD) or asthma.

The invention relates to a novel salt form of an indacaterol maleate intermediate namely (R)-8-(benzyloxy)-5-[2-[(5,6-diethyl-2,3-dihydro-1H-indene-2-yl)amino]-1-hydroxyethyl]quinoline-2(1H)-one and acrystal form thereof. The salt form and the crystal form thereof provided by the invention have good impurity removal effect and thermodynamic stability and simple and convenient preparation method,facilitate operation and storage, and are applicable to industrial application. The invention also relates to preparation methods for the salt form and the crystal form of the salt form, and an application of the salt form and the crystal form of the salt form in preparation of indacaterol maleate.

The invention discloses application of indacaterol maleate as a cGAS-STING pathway targeted agonist. In-vitro level verification, biotin photoaffinity labeling, conjugated protein omics, bioinformatics and molecular biology results show that the indacaterol maleate can activate a cGAS-STING pathway in a targeted manner and inhibit cancer cell proliferation and has a good treatment prospect in adjuvant therapy of colorectal cancer related diseases.

The invention provides a method for determining salmeterol, indacaterol and olodaterol in pork. The method includes the following steps: step 1, preparing samples; step 2, extracting to-be-detected samples; step 3, determining detection conditions of a liquid chromatography-tandem mass spectrometer and performing detection; step 4, drawing standard working curves; step 5, according to liquid chromatograms of to-be-detected solutions in the S2, calculating the contents of the olodaterol, the indacaterol and the salmeterol in the pork. The method has the advantages that the salmeterol, the indacaterol and the olodaterol in the pork are simultaneously determined for the first time, and the blank in current detection of the salmeterol, the indacaterol and the olodaterol in the pork is filled up; ion response values are high, sensitivity is high, detection limits are low, qualitativeness, quantitativeness, accuracy, rapidness, high efficiency and sensitivity are truly realized, and the method can serve as a reliable measure to detect the three drugs in the pork.

The invention provides a preparation method of an indacaterol intermediate. According to the preparation method provided by the invention, low-price raw materials are adopted, the operation is simpleand feasible, the reaction selectivity is good, complicated operations such as column chromatography are not required, the yield of a final prepared product is as high as 92.6%, and the total yield ofa whole route is as high as 71.2%, so that the preparation method is very suitable for industrial production.

The invention provides a preparation method of an intermediate diethylbenzene. The preparation method comprises the steps: reacting diethyl acetophenone and hydrazine hydrate, and making a compound react with alkaline to obtain the diethylbenzene. The preparation method provided by the invention has the advantages of availability of raw materials, simplicity and convenience in operation, good quality, high yield and low cost, and is suitable for large-scale industrialized production.

The invention relates to a preparation method of indacaterol and a salt thereof. The preparation method comprises the following steps: in a solvent, reacting a mixture containing a compound as shown in a formula I with m-chlorobenzoic acid to obtain a compound as shown in a formula II-1; and subjecting the obtained compound as shown in the formula II-1 to reacting and conversion to obtain indacaterol and the salt thereof. The preparation method of indacaterol and the salt thereof has the advantages of higher yield, high purity, easiness in refining, simple and convenient operation and suitability for industrialization.

The present invention relates to a process for preparing indacaterol or salts thereof. The process comprises of forming compound of Formula 1 by reacting compound of Formula 2 and compound of Formula 3 in the presence of a solvent to Form compound of Formula 4, which on removal of the protecting groups forms compound of Formula 1.