7 results about "Dabigatran" patented technology

The invention provides application of an SNP (Single Nucleotide Polymorphism) marker of MIA2 in predicting the curative effect of an antithrombotic drug on thrombus, and belongs to the fields of molecular biology and cardiovascular medicine. According to the application disclosed by the invention, one or more of rs11845046 and rs10134365 of the MIA2 gene is found to be related to the prediction of the curative effect of dabigatran on thrombus for the first time. Gene polymorphism analysis and an ROC curve verify that the curative effect of an NVAF patient after the NVAF patient is treated by using the antithrombotic drug is related to the genotypes of rs11845046 and rs10134365 of the MIA2 gene in a patient sample, and when the genotype of the rs11845046 is GG or the genotype of the rs10134365 is CC, the drug effect of the subject taking the antithrombotic drug is good but the probability of bleeding events is increased.

The application discloses a kind of dabigatran bleeding risk prediction methods based on machine learning, it is related to computer-aided drug risk management technical field, the method is by obtaining patient baseline and follow-up data, multiple imputation method is handled missing value;With HAS-BLED score as the basis, candidate variables are screened from potential risk factors using LassoCV algorithm, and anemia, insulin use and antifungal agent use are determined as new prediction variables through clinical correlation analysis to construct a set of prediction variables;Finally, a random forest or gradient boosting algorithm is used to train the model to output the bleeding risk assessment results of the individual to be tested.The application combines machine learning algorithm, improves the prediction accuracy of dabigatran bleeding risk in Chinese non-valvular atrial fibrillation patients, solves the problem of insufficient prediction accuracy of traditional HAS-BLED score, and provides a more reliable basis for clinical individualized anticoagulant therapy decision.

The application discloses application of a dabigatran chlorine-containing derivative in preparation of a medicine for inhibiting and treating colon cancer, and a structure of the compound is: the compound is an artificial synthetic compound, and experiments by MTT colorimetry prove that the compound with an amount greater than 12.5 mu g / mL can effectively inhibit HCT116 colon cancer cell activity, and the greater the amount of the compound, the more significant the inhibiting effect on HCT116 cells is, and the compound can be used for research on human colon cancer as a medicine for inhibiting proliferation of human colon cancer cells or an antitumor medicine.

According to the preparation method of the key intermediate N-(4-cyanophenyl) glycine of dabigatran etexilate, p-chlorobenzonitrile and glycine serve as raw materials, a target compound (I) is obtained through one step, the raw materials are easy to obtain and low in price, reaction conditions are mild, the yield is high, water serves as a reaction solvent, emission of three wastes is remarkably reduced, and the method is environmentally friendly and more friendly, and has good industrial application prospects. The method is suitable for large-scale commercial production.

This invention relates to the field of pharmaceutical intermediates, and in particular to a microchannel method for preparing dabigatran ester intermediates. The synthetic route of this invention utilizes a continuous flow microchannel reactor in the preparation of dabigatran ester intermediates, thereby significantly shortening the reaction time to within a few hundred seconds. Simultaneously, the target product obtained through this continuous flow reaction process exhibits high yield and high purity; testing shows that the purity of the target product can reach over 99%, and the yield can reach over 90%. The preparation method of this invention produces few byproducts, can be continuously produced, and has a high degree of automation, showing promising prospects for industrial application.

The invention discloses a preparation method of a dabigatran nitroso impurity, which comprises the following steps: (1) dissolving a raw material (A) in a solvent, adding alkali, then adding an amino protecting group raw material and a catalyst, and reacting to obtain an intermediate product (B); (2) dissolving (B) in a solvent, then adding a nitrosation reagent, and carrying out nitrosation reaction to obtain an intermediate product (C); (3) dissolving (C) in a solvent, and removing a terminal amino protecting group R to obtain an intermediate product (D); and (4) dissolving (D) in a solvent, adding alkali, and carrying out ester hydrolysis reaction to obtain a target product (E). The target product is obtained through four-step reaction, the reaction condition is mild, the chemical purity of the product can reach 98% or above, a reference substance is provided for qualitative and quantitative analysis of dabigatran drugs, meanwhile, an important basis is provided for scientific evaluation of quality, safety and efficiency of dabigatran, and important application value is achieved.