12 results about "Cinacalcet" patented technology

The invention discloses a preparation method of cinacalcet hydrochloride. The preparation method comprises the following steps: 1) carrying out a reaction on 3-(3-trifluoromethylphenyl) propanol and phosphorus oxychloride; first post-treatment: extracting the product obtained in the step 1) by using an organic solvent, drying and concentrating to obtain 1-(3-chloropropyl)-3-trifluoromethyl benzene; (2) carrying out substitution reaction on the 1-(3-chloropropyl)-3-trifluoromethyl benzene obtained by the first post-treatment and (R)-1-(1-naphthyl) ethylamine; the product obtained in the second step is subjected to extraction, drying and concentration through an organic solvent and then subjected to a salt forming reaction with hydrochloric acid, and cinacalcet hydrochloride is obtained.According to the method, it is guaranteed that the product has the good yield and high purity, meanwhile, the impurity content, especially oxidation impurities, is remarkably reduced, and the appearance color and luster of cinacalcet hydrochloride are effectively improved.

The invention discloses application of a calcimimetic agent in preparation of a medicine for treating autosomal dominant polycystic kidney disease. Pax8rtTA is adopted; tetOCre is taken as a starting material; after a Pkd1fl / fl mouse model is treated by a calcimimetic cinacalcet, by inhibiting secretion of parathyroid hormone, abnormal activation of ciliary positioning Pth1r is reduced, the progress of the polycystic kidney disease is delayed, and the medicine can remarkably delay cyst growth, improve related indexes of renal functions and has a significant clinical application prospect. The abnormal proliferation of cyst epithelial cells and the interstitial fibrosis process of the kidney are effectively inhibited.

The invention discloses a preparation method of cilnipride tartrate, which is characterized in that YT2303S-01 is used as a starting material, an intermediate 1 and an intermediate 2 are prepared in sequence, and finally the preparation of the cilnipride tartrate is completed. The raw materials adopted by the invention are commercially available products, the raw material sources are stable, and large-scale and industrial production can be conveniently carried out.

The invention belongs to the technical field of medicine synthesis, and discloses a preparation method of cinacalcet hydrochloride impurities. According to the preparation method, the safety of the operation process is high, risks caused by raney nickel use and high-pressure hydrogenation in the prior art route are effectively avoided, meanwhile, the yield and purity of the product both reach the high level, and the dual requirements for process safety and product quality are met.

The invention discloses a cinacalcet-containing transdermal patch as well as a preparation method and application thereof. The transdermal patch comprises a high-molecular matrix layer, wherein the high-molecular matrix layer comprises cinacalcet, a silicone pressure-sensitive adhesive and one or more high-molecular polymers selected from a water-insoluble cellulose derivative, polyvinylpyrrolidone and a polyethylene caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. The transdermal patch disclosed by the invention is good in drug permeability and colloid application performance, high in safety, free of skin irritation, high in stability and good in uniformity, and can meet the requirements of clinically treating hyperparathyroidism or hypercalcemia.

This invention relates to the field of pharmaceutical biotechnology, providing the application of aminoquinoline compounds (such as hydroxychloroquine and chloroquine) in the preparation of drugs for treating hyperparathyroidism. These compounds restore the expression of calcium-sensitive receptors (CaSRs) on the cell membrane surface by inhibiting the lysosomal degradation pathway of CaSRs in parathyroid cells. Experiments have confirmed that 4-aminoquinoline compounds, used alone or in combination with calcimimetics (such as cinacalcet), significantly reduce serum PTH and calcium levels in a model of refractory secondary hyperparathyroidism (SHPT) and inhibit glandular hyperplasia. In particular, the combination therapy regimen exhibits a significant synergistic effect, effectively reversing calcimimetics resistance. This invention is the first to discover a novel use for the antimalarial / antirheumatic drug hydroxychloroquine in the treatment of hyperparathyroidism, realizing a new use for an existing drug; and providing a safe and effective new drug treatment strategy for clinically refractory SHPT.

The present invention relates to a particle size reduction process using inert gas for preparation of nitrosamine free Cinacalcet salt. Wherein, Cinacalcet salt is substantially free of nitrosamine impurities.

The invention discloses a cinacalcet salt of diclofenac as well as a pharmaceutical composition and medical application of the cinacalcet salt, provides the cinacalcet salt of the diclofenac as shown in a formula (I), and further provides a pharmaceutical composition containing the cinacalcet salt of the diclofenac and a PD-1 / PD-L1 inhibitor. The diclofenac cinacalcet salt and the pharmaceutical composition of the diclofenac cinacalcet salt can be used for preparing drugs for preventing and / or treating cancers, infectious diseases, fibrosis diseases, autoimmune diseases and painful diseases.

This invention relates to cinacalcet hydrochloride, specifically to its application in the preparation of drugs for treating allergic rhinitis. This invention is the first to discover that cinacalcet hydrochloride has a therapeutic effect on allergic rhinitis. Specifically, drugs that effectively inhibit NO release from RAW264.7 cells (an in vitro inflammation model was established using LPS stimulation of RAW264.7 cells) were screened from 1430 FDA-approved small molecule compounds, and cinacalcet hydrochloride was discovered for the first time to dose-dependently inhibit NO release in the in vitro inflammation model. Furthermore, in vivo therapeutic experiments also showed that cinacalcet hydrochloride effectively inhibits the release of allergic mediators in vivo without affecting the body weight of mice, demonstrating good safety.

The invention discloses an application of cinacalcet hydrochloride in preparation of drugs for resisting drug-resistant bacteria. The invention finds that the cinacalcet hydrochloride (CC) has dual effects, on one hand, the sensitivity of a strain carrying a tmexCD-toprJ gene cluster to tigecycline can be recovered, and on the other hand, the conjugational metastasis of antibiotic resistance genes can be inhibited by reducing over 99% of plasmid propagation. The synergistic effect of the CC and the tigecycline is that the minimum inhibitory concentration of the tigecycline is reduced by at least 8 times by dissipating proton dynamic potential and inducing active oxygen to damage an excretion function. Besides, the CC also reduces propagation of various drug-resistant plasmids by synergistically inhibiting expression of an Mpf and Dtr conjugation system and inhibiting SOS response, so that plasmid transfer and stable colonization of exogenous DNA (Deoxyribose Nucleic Acid) are blocked. The CC overcomes the tigecycline drug resistance mediated by tmexCD-topJ by destroying energy metabolism and oxidative stress, and meanwhile, limits horizontal transfer of other drug-resistant genes.

The invention provides application of cinacalcet and pharmaceutically acceptable salts thereof in preparation of antifungal drugs, discovers that the clinically marketed drug cinacalcet has a new antifungal application, realizes effective redevelopment of existing drugs, expands treatment indications of the drugs, and provides a new technical path and a potential chemical entity for drug reutilization. Experimental results show that cinacalcet has a good inhibition effect on various pathogenic fungi and has certain broad-spectrum antifungal activity. As the medicine is clinically applied for a long time, the safety is definite, the toxic and side effects are controllable, the safety evaluation and preparation development risks in the new medicine research and development process are remarkably reduced, and the feasibility and popularization value of industrial application are improved.

The application discloses a synthesis method of cinacalcet hydrochloride, and comprises the following steps: mixing 3-trifluoromethyl phenylpropanol, (R)-1-(1-naphthyl)ethylamine, a catalyst and diphenyl phosphate, stirring under the protection of nitrogen or inert gas at 120-130 DEG C for 15-25 hours, cooling to room temperature, adding n-hexane to obtain a mixed solution, pouring the mixed solution into hydrochloric acid, standing until white solids are precipitated, filtering and drying to obtain the cinacalcet hydrochloride, wherein the catalyst is 1-hydroxytetraphenylcyclopentadienyl(tetraphenyl-2,4-cyclopentadienyl-1-ketone)-mu-hydroxytetracarbonyl diruthenium (II), the synthesis method is simple in steps, the cinacalcet hydrochloride is synthesized in one step, the catalyst used is cheap, the yield is high, the cost is obviously reduced, and the method is suitable for large-scale production.