18 results about "Raf kinase" patented technology

Provided herein are inhibitors of receptor tyrosine kinase effector, RAF, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.

The present invention concerns pharmaceutically acceptable salts of ((2,3- dichlorophenyl)sulfonyl)(2,4-difluoro-3-((6-(4-(4-hydroxy-4-(trifluoromethyl)piperidin-1-yl)- 1H-benzo[d]imidazol-1-yl)pyrido[3,2-d]pyrimidin-4-yl)amino)phenyl)amide of the formula (I) below: (I) wherein said salt is selected from a sodium salt, a choline salt, a potassium salt, and a calcium salt.

The present disclosure relates to compounds and compositions for inhibiting RAF serine / threonine protein kinase, methods of making the compounds and compositions, and their use in the treatment of various cancers.

The disclosure provides compounds of Formula I (Formula I) (c) And the pharmaceutically acceptable salts thereof. The A, B, C, and D rings and the variables, RA, RB, RC, RD, L0, L1, L2, and L2, are defined herein. Compounds and salts of Formula I are useful as inhibitors of RAF kinase dimerization, including dimerization of wild type and mutant BRAF kinases. The disclosure includes pharmaceutical compositions comprising a compound or salt of Formula I. The disclosure also includes methods of treating a cancer susceptible to treatment with an inhibitor of BRAF dimers or BRAF dimerization, comprising administering a therapeutically effective amount of a compound or salt of Formula I to a patient in need of such treatment. These cancers susceptible to treatment with an inhibitor of BRAF dimers or BRAF dimerization include melanoma, thyroid cancer, hairy cell leukemia, ovarian cancer, lung cancer, and colorectal cancer.

The invention provides the use of kinase inhibitors and derivatives of staurosporine, such as PKC412, to treat patients having epidermis bullosa simplex (BBS), epidermolytic hyperkeratosis, epidermolytic palmoplantar keratoderma, palmoplantar keratoderma, nonepidermolytic, pachyonychia congenita type 1, pachyonychia congenita type 2, or other intermediate filament associated diseases using oral or topical cream or ointment formulations of the same. The invention also provides the use of SRC and RAF kinase inhibitors, alone or in combination with PKC412, to treat intermediate filament associated diseases.

# imgabs0 # Described herein are compounds (I) as RAF inhibitors and their use in the treatment of conditions such as cancer.

Disclosed herein is a physically stable solid dispersion comprising Compound 1, i.e., the B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-naphthyridin-4-yl)oxy)-1a,6b-dihydro-1H-cyclopropa [b] benzofuran-1-yl)-3-(2, 4, 5-trifluorophenyl) urea and a specific stabilizing polymer, the method for preparing the same, and the uses of the solid dispersion. Also disclosed herein is the crystalline form of Compound 1.

To provide, e.g., a new form of a particularly poorly water-insoluble compound, i.e., Compound 1, which shows better bioavailability and has chemical and physical stability during formulation and storage of this drug.SOLUTION: Disclosed herein are: a physically stable solid dispersion comprising Compound 1, i.e., the B-RAF kinase dimer inhibitor 1-((1S,1aS,6bS)-5-((7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-4-yl)oxy)-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-1-yl)-3-(2,4,5-trifluorophenyl)urea and a specific stabilizing polymer; a method of preparing the same; uses of the solid dispersion; and a crystalline form of Compound 1.SELECTED DRAWING: None

The invention discloses an insect Raf kinase inhibition factor, which is a protein coded by a CvBV28-5 gene of polydDNA (deoxyribonucleic acid) virus of cotesia vestalis, and the amino acid sequence is shown as SEQ ID No.22 or SEQ ID No.8. The invention further discloses a preparation method of the insect Raf kinase inhibition factor. The nucleotide sequence of the gene for coding the inhibition factor of the insect Raf kinase is as shown in SEQ ID NO. 21 or SEQ ID NO. 7. The invention proves that CvBV28-5 interacts with Raf protein of plutella xylostella for the first time, so that the peak value of 20E titer in hemolymph of larvae of plutella xylostella is influenced, the ecdysis process of the larvae of plutella xylostella is prolonged, and a new gene resource is provided for improving the biological control efficiency of parasitic wasps and developing novel transgenic insect-resistant crops.

Provided herein are solid forms, methods of use, and processes relating to 1-((1S,1aS,6bS)-5-((7- oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-4-yl)oxy)-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-1-yl)-3- (2,4,5-trifluorophenyl) urea.

The present invention relates to crystalline salts of the RAF kinase inhibitor N-(3-(5-((1-ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide, which are useful in the treatment of cancer and other diseases.

Provided herein are inhibitors of receptor tyrosine kinase effector, RAF, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.

Compounds of formula I as RAF inhibitors and their use in treatment of conditions such as cancer # imgabs0 #

Inhibitory peptides for modifying RAF kinase protein dimerization are described. The peptides display a binding affinity for the dimer interface of a B-Raf, allowing for modification of RAF kinase dimerization, and inhibition of tumor growth. An embodiment of the disclosure is a peptide generated by modifying SEQ ID NO: 1, which corresponds to amino acids 503-521 of B-Raf kinase, e.g., cyclization, N-terminal capping, C-terminal capping, substitution of one or more amino acid residues, etc. The peptides disclosed herein include a modification to SEQ ID NO: 1 that can improve or otherwise alter binding affinity of the peptide to the dimer interface.

Disclosed herein are solid dispersions of a pan-RAF kinase inhibitor. In particular, provided herein is a pharmaceutical composition comprising a solid dispersion having a mass median diameter of about 75 µm to about 400 µm and one or more pharmaceutically acceptable excipients, wherein the solid dispersion comprises (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridine-2-yl)thiazole-5-carboxamide or a pharmaceutically acceptable salt thereof and a vinylpyrrolidone-vinyl acetate copolymer.

Provided herein are inhibitors of receptor tyrosine kinase effector (RAF), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of disease.