130 results about "Lapatinib" patented technology

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.

The invention provides a method for the treatment of Ph+ leukemia in a patient comprising administering to the patient (i) a BCR-ABL tyrosine kinase inhibitor, and (ii) an agent which selectively binds to a cell surface receptor expressed on Ph+ leukemic stem cells. The invention further provides for the use of (i) and (ii) in, or in the manufacture of a medicament for, the treatment of Ph+ leukemia in a patient; and a composition for the treatment of Ph+ leukemia in a patient comprising (i) and (ii); and kits comprising (i) and (ii). In some embodiments, the tyrosine kinase inhibitor is or is not imatinib; or is selected from the group consisting of dasatinib, nilotinib, bosutinib, axitinib, cediranib, crizotinib, damnacanthal, gefitinib, lapatinib, lestaurtinib, neratinib, semaxanib, sunitinib, toceranib, tyrphostins, vandetanib, vatalanib, INNO-406, AP24534, XL228, PHA-739358, MK-0457, SGX393 and DC2036; or is selected from the group consisting of dasatinib and nilotinib. In some embodiments, the agent binds to a receptor involved in signalling by at least one of IL-3, G-CSF and GM-CSF. In some embodiments, the agent is a mutein selected from the group consisting of IL-3 muteins, G-CSF muteins and GM-CSF muteins. In some embodiments, the mutein is an IL-3 mutein. In some embodiments, the agent is a soluble receptor which is capable of binding to IL-3.

The invention relates to a process for preparing a lapatinib synthetic intermediate, which is characterized by comprising the following process steps: mixing 5-iodo-2-aminobenzonitrile and DMF-DMA; heating and refluxing the mixture at a temperature of between 90 and 100 DEG C for 1 to 2 hours, and performing reduced pressure distillation at a pressure of 0.1 MPa and at a temperature of between 70 and 80 DEG C for 10 to 30 minutes to remove excessive DMF-DMA; adding glacial acetic acid and 3-chloro-4-(3-fluorophenyl-methoxy) aniline; heating and refluxing the mixture at a temperature of between 90 and 100 DEG C for 1 hour, cooling the mixture to the room temperature, and pouring the mixture to ice water; performing vacuum filtration, and washing a filter cake with the ice water and then with methanol; and performing vacuum drying on the filter cake to obtain a faint yellow solid N-(3-chloro-4-(3-fluorophenylmethoxy)phenyl)-6-iodoquinazoline-4-amine. The route avoids the use of thionyl chloride or phosphorus oxychloride and reduces pollutions to the environment; besides, the process has high yield and simple operation and is suitable for industrial production.

The invention provides a synthetic method for lapatinib. The method comprises the following steps: (a) in an organic solvent, reacting a compound (6) with a compound (7) in the presence of alkali to obtain a compound (8); (b) in the organic solvent, reacting the compound (8) with a compound (9) in the presence of alkali, and after the reaction is ended, adding a reducing agent for producing a reductive amination reaction to obtain a compound (10); (c) in the organic solvent, reacting the compound (10) with BOC anhydride in the presence of alkali to obtain a compound (11); (d) in the organic solvent, fully reacting the compound (11) with N,N-dimethylformamide dimethyl acetal under the backflow condition, and after the reaction is ended, adding a compound (4) and reacting under the backflow condition to obtain a compound (12); (e) in the organic solvent, producing a deprotection reaction of the compound (12) to obtain lapatinib. The invention further provides two new key intermediates. The method has the characteristics of few steps, high yield and suitability for industrialized production.

Methods for the treatment of a cell proliferation disease or disorder in a subject, involving applying a psoralen derivative lacking a DNA cross-linking motif to cancer cells, applying a psoralen or a derivative thereof and lapatinib, or applying a psoralen or derivative thereof and neratinib, to a subject and further applying initiation radiation energy form an energy source.

The invention relates to a I-type crystal of dibenzenesulfonate of an inhibitor of protein tyrosine kinase. Specifically, the invention relates to a I-type crystal of lapatinib dibenzenesulfonate. The crystal, radiated by Cu-K<alpha>, has the following characteristic peaks, represented by a 2theta angle and an inter-planar distance in an X-ray powder diffraction pattern: 6.21(14.23), 10.02(8.82), 12.11(7.30), 13.26(6.67), 13.55(6.53), 13.79(6.42), 14.88(5.95), 6.70(5.31), 17.59(5.04), 18.26(4.86), 18.93(4.68), 19.61(4.52), 20.71(4.29), 21.06(4.21), 22.19(4.00), 23.60(3.77), 24.20(3.68), 24.58(3.62), 25.10(3.55), 25.85(3.44), 26.75(3.33), 30.83(2.90), and 32.89(2.72). According to the invention, the I-type crystal of lapatinib dibenzenesulfonate has better stability, and can be preferably used for clinic treatment.

Cell-targeted serine protease constructs are provided. Such constructs can be used in methods for targeted cell killing such as for treatment cell of proliferative diseases (e.g., cancer). In some aspects, recombinant serine proteases, such as Granzyme B polypeptides, are provided that exhibit improved stability and cell toxicity. Methods and compositions for treating lapatinib or trastuzumab-resistant cancers are also provided.