6 results about "Neratinib" patented technology

The invention provides a pharmaceutical composition for treating non-small cell lung cancer and application of the pharmaceutical composition. The pharmaceutical composition comprises gefitinib, erlotinib, afatinib, neratinib, osimertinib and the like which serve as active ingredients. The pharmaceutical composition disclosed by the invention can simultaneously contain various EGFR inhibitors as active ingredients, and the active ingredients are controlled at ultra-low dosage, so that the pharmaceutical composition not only can ensure the treatment effect, even the drug effect of the pharmaceutical composition is obviously superior to that of a high-dosage EGFR inhibitor independent administration group, but also can ensure the safety, and the pharmaceutical composition is suitable for clinical application. And after the active components are combined, a good synergistic effect is achieved, and more importantly, the occurrence of drug resistance can be remarkably reduced or even resisted. In a lung cancer cell culture experiment, the EGFR inhibitor independent administration group has a drug resistance phenomenon at the earliest 20 days, but the pharmaceutical composition group still has no drug resistance phenomenon after 160 days of administration.

Disclosed in the present invention are a dimethylphosphoryl substituted compound, and a preparation method therefor, a pharmaceutical composition thereof and the use thereof. Provided in the present invention is a compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound of the present invention can target a host eIF2α kinase, eIF2α phosphorylation and protein synthesis. The compound of the present invention has great biological activity for treating breast cancer. Particularly, compound SIPI-27 and compound SIPI-28 of the present invention has inhibitory activity against breast cancer significantly superior to that of the control compounds BTdCPU and neratinib; and / or the compound of the present invention also has biological activity against coronaviruses and / or orthopoxviruses, in particular, compound SIPI-25 of the present invention has broad-spectrum anti-coronavirus activity against porcine epidemic diarrhea virus (PEDV), mouse hepatitis virus (MHV), infectious bronchitis virus (IBV) and porcine deltacoronavirus (PDCoV), and also has activity against the Taterapox virus (TTV) orthopoxvirus.

The invention belongs to the technical field of biological medicines, and particularly relates to application of neratinib in preparation of a medicine for preventing and treating noise-induced deafness. According to the specific technical scheme, the application of the neratinib in preparation of the medicine for preventing and treating hearing impairment / deafness is provided. According to the invention, the fact that neratinib can play a hearing protection role by specifically regulating and controlling cochlea immune microenvironment is found for the first time, and the hearing protection role is specifically realized by the following mechanisms: regulating and controlling biological effects such as cell signal channels, inflammatory response and cell stress response, protecting hair cell structures, and reducing cochlea basilar membrane outer hair cell loss caused by noise exposure. Based on the new discovery of the invention, the neratinib can be used for preparing medicines for preventing and treating hearing impairment and deafness caused by noise.

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 dimethyl phosphoryl substituted compound as well as a preparation method, a pharmaceutical composition and application thereof. The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof. The compound provided by the invention can target host eIF2alpha kinase, eIF2alpha phosphorylation and protein synthesis. The compound provided by the invention has excellent biological activity for treating breast cancer. Particularly, the inhibitory activity of the compound SIPI-27 and the compound SIPI-28 on the breast cancer is obviously superior to that of contrast compounds BTdCPU and neratinib; and / or the compound provided by the invention still has biological activity of resisting coronavirus and / or orthopoxvirus, and particularly, the compound SIPI-25 provided by the invention has broad-spectrum anti-coronavirus activity of resisting porcine epidemic diarrhea virus (PEDV), mouse hepatitis virus (MHV), infectious bronchitis virus (IBV) and porcine delta coronavirus (PDCoV), and also has anti-orthopoxvirus (TTV) activity.

This disclosure provides a pharmaceutical combination for treating non-small cell lung cancer, comprising a therapeutically effective amount of a PIN1 inhibitor and a therapeutically effective amount of neratinib.