3 results about "Toremifene" patented technology

The application relates to the technical field of compound synthesis, and particularly discloses a preparation method of an intermediate of toripalimab citrate, which comprises the following steps: a first reaction of cinnamyl alcohol and diethyl phosphite in an organic solvent to obtain a first reactant; and a second reaction of the obtained first reactant, alkali and 4-[2-(N,N-dimethylamino)ethoxy]benzophenone to obtain a second reactant containing the intermediate I of toripalimab citrate. A brand-new process route is developed, raw materials used in the route are all easy to obtain, the whole reaction route is short, operation is simple, reaction conditions are mild and safe, the yield of the obtained intermediate I of toripalimab citrate is high, the purity is also high, the total yield is more than 80%, the purity is more than 99.9%, and industrialized production can be realized.

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 a toremifene citrate tablet and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The toremifene citrate tablet is prepared from a toremifene citrate solid dispersion, a filling agent, a disintegrating agent, a lubricating agent and a flow aid, wherein the toremifene citrate solid dispersion is prepared by compounding toremifene citrate, copovidone, quercetin and hydroxypropyl methylcellulose K100M in proportion. The preparation method comprises preparation of the toremifene citrate solid dispersion and preparation of the tablet. Compared with the prior art, the toremifene citrate tablet can play a slow release effect, is high in bioavailability and is suitable for industrial mass production.