8 results about "Erlotinib" patented technology

Olmsted syndrome (OS) is a rare genodermatosis classically characterized by the combination of bilateral mutilating transgredient palmoplantar keratoderma (PPK) and periorificial keratotic plaques. The inventors obtained remarkable results with a treatment with a EGFR inhibitor (e.g. erlotinib) in 3 patients with Olmsted Syndrome and erythemalgia linked to different TRPV3 mutations. In less than 3 months, the drug induced a complete disappearance of the hyperkeratosis and the pain. Anorexia and insomnia disappeared with an improvement of the growth. Accordingly, the present invention relates to the use of EGFR inhibitors for the keratodermas.

The invention relates to the technical field of chemical synthesis of medicines, and particularly discloses a production and preparation method of an erlotinib intermediate. The method comprises the following steps: taking 3, 4-dihydroxy benzaldehyde as an initial raw material, sequentially carrying out etherification, oxidation and nitration reactions to prepare 2-nitro-4, 5-bis (2-methoxyethoxy) benzoic acid, finally dissolving the 2-nitro-4, 5-bis (2-methoxyethoxy) benzoic acid, formamide, formic acid and triethylamine in gamma-valerolactone to form two material flows, and carrying out heat treatment to obtain the 2-nitro-4, 5-bis (2-methoxyethoxy) benzoic acid. And carrying out continuous cyclization reaction in a fixed bed reactor filled with a specific composite catalyst, and carrying out post-treatment to obtain the target product 6, 7-bis (2-methoxyethoxy)-4-quinazolinone. According to the method, the raw materials are easy to obtain, the reaction efficiency and the product purity are remarkably improved by optimizing the synthesis route and the reaction conditions, and a novel efficient, environment-friendly and stable method is provided for large-scale production of the erlotinib key intermediate.

This invention discloses a bio-preparation method for a key chiral intermediate of erlotinib ethyl ester. The method utilizes resting cells of *Saccharomyces cerevisiae* ZJPH1807 as a catalyst to prepare (R)-1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethanol via biocatalysis of 1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethanol. The product obtained using this strain exhibits high optical purity (ee value > 99.9%) and a reaction yield of 86.4%. The process is simple, environmentally friendly, and uses microbial cells as the biocatalyst, resulting in low cost.

This invention, entitled "Combined Application and Product of BAM-15 and Erlotinib," belongs to the field of combined antitumor drug application technology. The technical problem it aims to solve is the low response and limited efficacy of existing erlotinib monotherapy to EGFR wild-type lung adenocarcinoma, and the lack of effective targeted intervention options in clinical practice. The key points of the technical solution are: combining BAM-15 and erlotinib for the interventional treatment of EGFR wild-type lung adenocarcinoma; the combination produces a significant synergistic effect, with tumor suppression superior to the additive effect of using either drug alone, without antagonistic effects, effectively enhancing the inhibitory effect on EGFR wild-type lung adenocarcinoma and enriching clinical treatment options for tumors.

The present application relates to the field of pharmaceutical analysis, in particular to a method for detecting erlotinib related impurities and application thereof. The method adopts high performance liquid chromatography-mass spectrometry, the chromatographic column of the high performance liquid chromatography uses high-purity silica gel as the filler, and the mass spectrometry ion source is ESI source. The method provided by the present application realizes effective separation and detection of extremely low content of erlotinib related impurities. The method has the advantages of good specificity, high sensitivity and the like, realizes simultaneous detection of multiple erlotinib impurities, and has extremely low detection limit.

The present application relates to the technical field of animal model construction method, and particularly relates to a kind of construction method of small molecule drug induced peritoneal malignant mesothelioma animal model.The method uses epidermal growth factor receptor tyrosine kinase inhibitor (Erlotinib or its salt, Erlotinib) to be injected into abdominal cavity to mammal, and peritoneal malignant mesothelioma animal model is induced to form.The technical scheme can solve the technical problem that the construction process of peritoneal malignant mesothelioma animal model in prior art is too long or needs special equipment and conditions.The method of peritoneal malignant mesothelioma animal model constructed by the technical scheme is short in time consumption, high in efficiency, and does not need asbestos exposure and virus gene operation, greatly saves time cost and economic cost, is simple and easy to operate, and is easy to popularize, and the animal model is expected to be used for further revealing malignant mesothelioma mechanism of occurrence and development and screening new therapeutic drugs, and has ideal application prospect.

The present invention is directed to a protein kinase inhibitor for use in the treatment of tuberculosis, by direct inhibition of the growth of a Mycobacterium tuberculosis complex species, and to corresponding methods of treating tuberculosis. More specifically, the invention relates to the use of protein tyrosine kinase inhibitors such as gefitinib, erlotinib, or imatinib for use in the treatment of tuberculosis, by direct inhibition of the growth of a Mycobacterium tuberculosis complex species, rather than through use in host-directed therapy. Also provided are methods of determining the ability of a protein tyrosine kinase inhibitor to inhibit the growth of a Mycobacterium tuberculosis complex species and methods of identifying a protein tyrosine kinase inhibitor as being potentially effective in the treatment of tuberculosis by direct inhibition of a Mycobacterium tuberculosis complex species.