4 results about "Anastrozole" patented technology

The present application provides a kind of bivalent platinum complex with anastrozole as ligand and its use, the structure of the bivalent platinum complex is as shown in (I).The bivalent platinum complex described in the present application has good antitumor activity.In the present method, anastrozole is reacted with potassium chloroplatinite in an organic solvent to obtain a bivalent platinum complex with anastrozole as ligand, and is applied to the antiproliferation of human breast cancer cells, showing excellent antitumor activity.

This invention relates to the treatment of breast cancer in a subject, and the subject can be either a male or female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed selective estrogen receptor modulator (SERM) (tamoxifen, toremifene, raloxifene), gonadotropin-releasing hormone (GnRH) agonist (goserelin), aromatase inhibitor (AI) (letrozole, anastrozole, exemestane), cyclin-dependent kinase 4 / 6 (CDK 4 / 6) inhibitor (palbociclib (Ibrance), ribociclib (Kisqali), lerociclib, abemaciclib (Vorzenio), trilaciclib, lerociclib), mTOR inhibitor (everolimus), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), alpelisib (Piqray) (an inhibitor of phosphatidylinositol-3-kinase subunit alpha (PI3Kα)), lapatinib, neratinib (Nerlynx), olaparib (Lynparza) (an inhibitor of the enzyme poly ADP ribose polymerase (PARP)), bevacizumab (Avastin), and / or fulvestrant treatments; metastasis in a subject suffering from breast cancer; HER2-positive; treating a subject suffering from ER mutant expressing breast cancer and / or treating breast cancer in a subject, by first determining the 18F-16β-fluoro-5α-dihydrotestosterone (18F-DHT) tumor uptake and identifying said subject as having AR-positive breast cancer based on 18F-DHT tumor uptake, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound and a cyclin-dependent kinase 4 / 6 (CDK 4 / 6) inhibitor.

The invention relates to a preparation method of anastrozole, which comprises the following steps: by taking methyl 3, 5-dibromobenzoate as a starting raw material, sequentially carrying out substitution, reduction, phosphorylation and N-alkylation to obtain anastrozole. The preparation method provided by the invention is a brand new technical route and is not reported in any literature and patent. According to the method, the yield of the product can be greatly improved, and the method is suitable for industrial production.

The invention relates to the technical field of medicine synthesis, in particular to a synthesis method of an anastrozole intermediate. The synthesis method comprises the following steps: S1, adding a first solvent into 3, 5-bis [(2, 2-dimethyl) ethyl cyano] toluene serving as a raw material, mixing, then adding N-bromo-butanediimine, and carrying out substitution reaction to obtain a reaction mixed solution; s2, adding diethyl phosphite and organic alkali into the reaction mixed solution at room temperature, and reacting to obtain a finished product reactant system; s3, carrying out post-treatment on the finished product reactant system to obtain a crude anastrozole intermediate; s4, mixing the anastrozole intermediate crude product with a refining solvent, and refining to obtain a refining system; sequentially carrying out crystallization and suction filtration on the refining system to obtain a filter cake; and sequentially washing and drying the filter cake to obtain a finished product anastrozole intermediate. The method has the advantages of easily available raw materials, low cost, efficient reaction, high conversion rate, high product purity and the like.