37 results about "Toremifene" patented technology

Novel methods for treating or reducing the likelihood of acquiring vaginal dysfunctions, more particularly vaginal dryness and dyspareunia, leading to sexual dysfunction and low sexual desire and performance, in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor. Further administration of estrogen or selective estrogen receptor modulator, particularly those selected from the group consisting of Raloxifene, Arzoxifene, Tamoxifen, Droloxifene, Toremifene, Iodoxifene, GW 5638, TSE-424, ERA-923, and lasofoxifene, and more particularly compounds having the general structure:is specifically disclosed for the medical treatment and / or inhibition of development of some of these above-mentioned diseases. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

The invention provides a synthetic method of toremifene. The synthesis method comprises: step S1, making a MacMurray reaction between compound B having structural formula II and compound C having structural formula III to obtain compound D having structural formula IV; step S2, making compound D react with compound E having structural formula V or The hydrochloride of compound E undergoes a selective alkylation reaction on the phenolic hydroxyl group to obtain compound F with structural formula VI; step S3, reacting compound F with thionyl chloride to obtain toremifene, wherein structural formula II is : Structural formula III is: Structural formula IV is Structural formula Ⅴ is ClCH 2 CH 2 N(CH 3 ) 2 ; Structural formula Ⅵ is The stereoselectivity of the obtained compound D is higher, so when using it as an intermediate to synthesize toremifene, the reaction yield of the toremifene of the Z configuration can be increased, and the toremifene of the Z configuration can be improved. purity; and the process is stable, the reaction conditions are mild, the intermediates are easy to separate, and can be used for large-scale production.

This invention relates to the treatment of breast cancer in a subject, for example a 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 SERM (tamoxifen, toremifene), aromatase inhibitor, palbociclib (Ibrance), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and / or fulvestrant treatments; metastasis in a subject suffering from breast cancer; and / or HER2-positive; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

The invention relates to a preparation method of citric acid toremifene intermediates 4-[2-(N,N-dimethylamino)ethyoxyl diphenylketone and 1,2-diphenyl-1-[4[2-[2-N,N- dimethylamino]ethoxyl]-1,4-butanediol. The preparation method of the 4-[2-(N,N-dimethylamino)ethyoxyl diphenylketone comprises the steps that 4-hydroxy diphenyl ketone, inorganic alkali, a first solvent and a second solvent are mixed and are stirred at the temperature of 53-58 DEG C for 0.8-2 hours, then cooling is performed to 40 DEG C or below, N,N-dimethylamino chloroethane hydrochloride is added, heating is performed to reach 80-85 DEG C, and stirring reaction is performed for 2-5 hours; cooling is performed to 40 DEG C or below, drinking water is added, stirring is performed to make the mixture layered, and an upper-layer oil phase is taken; the oil phase is washed with 4% sodium hydroxide solution till it is detected through TLC that the 4-hydroxy diphenyl ketone disappears, then washing is performed with drinking water till pH is 8-9; the obtained product is subjected to decompression at the temperature of 55-60 DEG C to evaporate out the solvent, and the citric acid toremifene intermediates 4-[2-(N,N-dimethylamino)ethyoxyl diphenylketone is obtained after cooling.

This invention relates to the treatment of androgen receptor-positive breast cancer in a subject, for example a female subject. Accordingly, this invention provides methods of: a) treating a subject suffering from breast cancer; b) treating a subject suffering from metastatic breast cancer; c) treating a subject suffering from refractory breast cancer; d) treating a subject suffering from AR-positive breast cancer; e) treating a subject suffering from AR-positive refractory breast cancer; f) treating a subject suffering from AR-positive metastatic breast cancer; g) treating a subject suffering from AR-positive and ER-positive breast cancer; h) treating a subject suffering from triple negative breast cancer; i) treating a subject suffering from advanced breast cancer; j) treating a subject suffering from breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and / or fulvestrant treatments; k) treating, preventing, suppressing or inhibiting metastasis in a subject suffering from breast cancer; l) prolonging survival of a subject with breast cancer, and / or m) prolonging the progression-free survival of a subject with breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound, comprising administering to the subject a therapeutically effective amount of a SARM compound of this invention.

Novel methods for treating or reducing the likelihood of acquiring vaginal dysfunctions, more particularly vaginal dryness and dyspareunia, leading to sexual dysfunction and low sexual desire and performance , in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor. Further administration of estrogen or selective estrogen receptor modulator, particularly those selected from the group consisting of Raloxifene, Arzoxifene, Tamoxifen, Droloxifene, Toremifene, Iodoxifene, GW 5638, TSE-424, ERA-923, and lasofoxifene, and more particularly compounds having the general structure:is specifically disclosed for the medical treatment and / or inhibition of development of some of these above-mentioned diseases. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

This invention relates to the treatment of breast cancer in a subject, for example a 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 SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and / or fulvestrant treatments; metastasis in a subject suffering from breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

This invention relates to the treatment of breast cancer in a subject, for example a female subject. The breast cancer includes 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 SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and / or fulvestrant treatments, and metastasis in a subject suffering from breast cancer. The method comprises administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

This invention relates to the treatment of breast cancer in a subject, for example a 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 SERM (tamoxifen, toremifene), aromatase inhibitor, palbociclib (Ibrance), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and / or fulvestrant treatments; metastasis in a subject suffering from breast cancer; and / or HER2-positive; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.

The present invention provides methods for reducing the incidence of, inhibiting, suppressing, and treating androgen-deprivation induced osteoporosis, bone fractures and / or loss of bone mineral density (BMD) in men having prostate cancer, comprising administering to a male human subject having prostate cancer a toremifene and / or its analog, derivative, isomer, metabolite. pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide. or any combination thereof. The present invention also provides methods of treating, preventing, suppressing, inhibiting, or reducing the incidence of hot flashes, gynecomastia, and / or hair loss in a subject, comprising same.

This invention relates to the treatment of breast cancer in a subject, for example a 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), abemaciclib (Vorzenio)), mTOR inhibitor (everolimus), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), 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; and / or treating a subject suffering from ER mutant expressing breast cancer, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.