50 results about "Raf Kinase Inhibitor" patented technology

This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II):or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.

This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

The invention relates to the use of a group of aryl ureas in treating raf mediated diseases and pharmaceutical compositions for use in such therapy of the formulawherein,Y is NHRHal is chlorine or bromine,R is H, CH3 or CH2OH, andX1 to X7 are each, independently, H, OH or —OC(O)C1-C4 alkyl, or a salt purified stereoisomer thereof,wherein at least one of X1 to X7 is OH or —OC(O)C1-C4 alkyl.

The present invention provides diagnostic and prognostic methods for predicting the effectiveness of treatment of a cancer patient with inhibitors of EGFR kinase, PDGFR kinase, or FGFR kinase. Based on the surprising discovery that tumors cells after having undergone an EMT, while being mesenchymal-like, still express characteristics of both epithelial and mesenchymal cells, and that such cells have altered sensitivity to inhibition by receptor protein-tyrosine kinase inhibitors, in that they have become relatively insensitive to EGFR kinase inhibitors, but have frequently acquired sensitivity to inhibitors of other receptor protein-tyrosine kinases such as PDGFR or FGFR, methods have been devised for determining levels of specific epithelial and mesenchymal biomarkers that identify such “hybrid” tumor cells (e.g. determination of co-expression of vimentin and epithelial keratins), and thus predict the tumor's likely sensitivity to inhibitors of EGFR kinase, PDGFR kinase, or FGFR kinase. Improved methods for treating cancer patients with EGFR, PDGFR or FGFR kinase inhibitors that incorporate such methodology are also provided.

The present invention relates to Raf kinase inhibitors containing zinc-binding and their use in the treatment of Raf related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.

This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and / or inhibit abnormal cell proliferation.

The invention is based upon the discovery that the mitogen-activated protein kinase (MAPK) pathway can increase CA9 expression independently of HIF-1, as well as increasing CA9 expression under HIF-1-dependent pathways initiated by hypoxia or high cell density. Disclosed herein are novel therapeutic methods for treating preneoplastic / neoplastic diseases associated with abnormal MN / CA IX expression, using MAPK pathway inhibitors. Preferably, the MAPK pathway inhibitors are raf kinase inhibitors, particularly the raf kinase inhibitor Sorafenib. Further disclosed are methods for patient therapy selection for MAPK pathway inhibitors, preferably in combination with other cancer therapies, based on detection of abnormal MN / CA9 gene expression in preneoplastic / neoplastic tissues.

The invention relates to a kind of new aramide compounds based on a purine structure, a preparation method thereof, a medicinal composition containing the compounds and a medical application thereof, and particularly relates to an application of the compounds serving as a Raf kinase inhibitor. The composition of the new compounds can be independently used or can be used together with at least one of other medicines for treating the diseases regulated by protein kinase such as cancers.

New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

The invention relates to Raf kinase inhibitor pentafluoride sulfur-based aryl urea, and a preparation method and applications thereof. The structure of pentafluoride sulfur-based aryl urea is represented by formula I, wherein Z, R1, R3, R2, m, and n are defined by the patent claims and the patent specification. Pntafluoride sulfur-based aryl urea can be used as a Raf kinase inhibitor, possesses excellent stability, and can be used for preparing medicines used for preventing and / or treating Raf kinase induced diseases.

A combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis is disclosed. The patient is treated with a camptothecin derivative and one or more chemotherapeutic agents selected from a microtubule active agent; an alkylating agent; an anti-neoplastic anti-metabolite; a platin compound; a topoisomerase II inhibitor; a VEGF inhibitor; a tyrosine kinase inhibitor; an EGFR kinase inhibitor; an mTOR kinase inhibitor; an insulin-like growth factor I inhibitor; a Raf kinase inhibitor; a monoclonal antibody; a proteasome inhibitor; a HDAC inhibitor; and ionizing radiation.

New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

The present invention relates to Raf kinase inhibitors containing zinc-binding and their use in the treatment of Raf related diseases and disorders such as cancer. The said derivatives may further actas HDAC inhibitors.

The invention relates to the field of pharmaceutical chemistry, in particular to N,N'-bis-substituted urea compounds, a preparation method thereof, a medicinal composition containing the compounds and medical application of the N,N'-bis-substituted urea compounds, particularly application of the N,N'-bis-substituted urea compounds used as a Raf kinase inhibitor.

The invention belongs to the field of pharmaceutic preparations, and relates to an RAF kinase inhibitor particle composition. The composition comprises the following components: (1) 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropal[b]benzofuran-5-yl)oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one or a pharmaceutically acceptable salt as an active component,(2) silicified microcrystalline cellulose and (3) an optionally selected other pharmaceutically acceptable excipient. The particle composition is prepared by using a rolling granulation technology. The method adopts the rolling granulation technology to solve the problems of easy agglomeration and poor fluidity of materials, obtains the particle composition with better fluidity, stability and dissolution for preparing a corresponding formulation dosage form, and is suitable for commercial production.

The invention relates to 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo [d] imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa [b] benzofuran-5-yl) oxy)-3,4-dihydro-1,8-naphthyridin-2 (1H)-one (Compound 1) maleate salts, in particular the sesqui-maleate salt and its crystalline forms, methods of preparation, pharmaceutical compositions, and therapeutic uses for treatment of diseases or disorders mediated by BRAF or other kinases.

The invention relates to novel aromatic amide compounds and a preparation method thereof, a medical composition containing the compounds and medical application of the compounds and the composition, and particularly application of the compounds and composition in serving as Raf kinase inhibitors. The novel compound composition can be used independently or used by combining at least one other drug for treating diseases such as cancers which are regulated by protein kinase. Please see the formula in the description.

The invention relates to the field of pharmaceutical chemistry, in particular to a diaryl urea compound (A), wherein the definitions of R1-R13, Ar and X are shown in the specification. The invention also discloses a preparation method of the compounds of the general formula (A), medicinal compositions containing the compounds and medical application thereof, particularly application as the Raf kinase inhibitor.

The invention relates to the fields of medicinal chemistry and chemical treatment. Specifically, the invention provides a 2-substituted-5-phenyl furan compound represented by the following general formula I, or a cis-trans isomer or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof, and a preparation method, a pharmaceutical composition and an application thereof in preparation of a B-Raf kinase inhibitor. The compound or the pharmaceutical composition thereof can be used as the high-efficiency B-Raf kinase inhibitor used for treating tumor diseases.

The invention relates to 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo [d] imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa [b] benzofuran-5-yl) oxy)-3,4-dihydro-1, 8-naphthyridin-2 (1H)-one (Compound 1) maleate salts, in particular the sesqui-maleate salt and its crystalline forms, methods of preparation, pharmaceutical compositions, and therapeutic uses for treatment of diseases or disorders mediated by BRAF or other kinases.

A combination therapy for treating patients suffering from proliferative diseases or diseases associated with persistent angiogenesis is disclosed. The patient is treated with a camptothecin derivative and one or more chemotherapeutic agents selected from a microtubule active agent; an alkylating agent; an anti-neoplastic anti-metabolite; a platin compound; a topoisomerase II inhibitor; a VEGF inhibitor; a tyrosine kinase inhibitor; an EGFR kinase inhibitor; an mTOR kinase inhibitor; an insulin-like growth factor I inhibitor; a Raf kinase inhibitor; a monoclonal antibody; a proteasome inhibitor; a HDAC inhibitor; and ionizing radiation.

The invention relates to a pharmaceutical composition comprising Compound 1 or a pharmaceutically acceptable salt thereof for the treatment of cancer and a process for its preparation. The invention also relates to administering the pharmaceutical composition to a patient according to an intermittent dosing regimen.

The present disclosure relates to methods for the treatment of cancers. In particular, the disclosure provides methods for treatment of cancer by administering Raf inhibitors in combination with Aurora kinase inhibitors. The present disclosure relates to methods of treating subject suffering from cancer, comprising administering to the subject a Raf kinase inhibitor or a pharmaceutically acceptable salt thereof; and an Aurora kinase inhibitor or a pharmaceutically acceptable salt thereof; the amount of said Raf kinase inhibitor or a pharmaceutically acceptable salt thereof being such that the combination thereof is therapeutically effective in the treatment of the cancer. In some [embodiments, the cancer is a solid tumor cancer.