6 results about "Exemestane" patented technology

The method comprises the following steps: taking androstane-3-ketone-4-ene-17beta-carboxylic acid shown in a formula II as a raw material, carrying out decarboxylation hydroxylation, sulfonylation, elimination and double-bond oxidative cracking to prepare the exemestane intermediate shown in a formula VI, and then sequentially carrying out allylic oxidation, wittig reaction and 1, 2, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3-trimethyl-1, 3, 4-trimethyl-1, 3 the exemestane shown in the formula I is prepared through the step of 1, 2-site dehydrogenation. The method has the characteristics of simple process operation, mild conditions, high reaction yield and the like, and is suitable for industrial production.

The invention belongs to the field of bioengineering pharmacy, and particularly relates to a method for preparing high-standard exemestane through microbial conversion. According to the method, Nocardia simplex Noc (PN)-TS001 is adopted as a fermentation strain, methylenide is efficiently converted by microorganisms to prepare high-standard exemestane, and through optimization and combination of processes of all stages such as methylenide pretreatment, microorganism fermentation conversion and extraction refining, the substrate feeding concentration is increased to 1%-8%, the conversion rate reaches 88%-95%, the total yield reaches 88%-90%, and the yield of exemestane is increased to 90%. The detection content of the prepared exemestane refined product is more than 99.5%, the impurity content is less than 0.1%, and each index meets the USP standard. The method is simple and feasible in process, environment-friendly, low in cost, high in conversion efficiency, high in yield and high in product quality, and has a very good industrial application prospect.

The present patent application discloses a new use of exemestane, and specifically discloses the use of exemestane in treating diseases with reduced nerve function, including cerebral ischemia-reperfusion injury, cerebral infarction, Parkinson's disease, etc. In long-term research, it is found that exemestane has a neuroprotective effect, can prevent or delay the death of nerve cells, and has a therapeutic effect on diseases with reduced nerve function, such as cerebral ischemia-reperfusion injury and cerebral infarction.

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 discloses application of exemestane in preparation of a medicine for treating spontaneous cerebral hemorrhage. The invention proposes and verifies that exemestane can effectively reduce the hematoma area after spontaneous cerebral hemorrhage, maintain the brain tissue structure, relieve immune cell infiltration, avoid brain cell apoptosis, promote motor function recovery and improve anxiety behaviors for the first time, and provides a new direction for treatment of spontaneous cerebral hemorrhage.

The invention relates to the technical field of drug detection, and discloses a method for detecting beta-lactam compound residues in a drug, which comprises the following steps of: extracting and diluting beta-lactam compounds in the drug through a uniform pretreatment process (adopting 50% acetonitrile) in combination with optimized LC-MS / MS conditions (including specific chromatographic columns, gradient elution procedures and mass spectrum parameters); synchronous quantitative detection of eight beta-lactam compounds (covering cephalosporin and penem) in five raw material medicines (exemestane, etoposide, abiraterone acetate, emtricitinib and cilnimod) with remarkable structural difference is realized, and the limit of quantitation is as low as 0.008 ppm. According to the method, the detection sensitivity is remarkably improved, the trace residue monitoring requirement is met, pretreatment steps are simple and universal, conditions do not need to be adjusted according to different raw material medicines, the detection efficiency and the method applicability are greatly improved, and the problems that the sensitivity is insufficient and the universality is poor in the prior art are effectively solved.