918523-46-3Relevant academic research and scientific papers
COMPOUNDS FOR THE TREATMENT OF BRAF-ASSOCIATED DISEASES AND DISORDERS
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Paragraph 0720; 0721, (2021/01/20)
Provided herein are compounds of the Formula I: and pharmaceutically acceptable salts, solvates and polymorphs thereof, wherein L, X1, R1, R2, R3, R4, R5 and R6 are as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors, including malignant and benign BRAF-associated tumors of the CNS and malignant extracranial BRAF-associated tumors.
Protein kinase inhibitor and its composition and use thereof
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Paragraph 0270-0272, (2017/08/02)
The invention relates to compounds as shown in the general formula (I), pharmaceutical compositions containing the compounds, a method for treating diseases and disease symptoms related to abnormal activity of protein kinase by using the compounds, and medicinal use of the compounds.
KINASE MODULATING COMPOUNDS, COMPOSITIONS CONTAINING THE SAME AND USE THEREOF
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Page/Page column 37, (2013/06/05)
The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties
Mathieu, Simon,Gradl, Stefan N.,Ren, Li,Wen, Zhaoyang,Aliagas, Ignacio,Gunzner-Toste, Janet,Lee, Wendy,Pulk, Rebecca,Zhao, Guiling,Alicke, Bruno,Boggs, Jason W.,Buckmelter, Alex J.,Choo, Edna F.,Dinkel, Victoria,Gloor, Susan L.,Gould, Stephen E.,Hansen, Joshua D.,Hastings, Gregg,Hatzivassiliou, Georgia,Laird, Ellen R.,Moreno, David,Ran, Yingqing,Voegtli, Walter C.,Wenglowsky, Steve,Grina, Jonas,Rudolph, Joachim
experimental part, p. 2869 - 2881 (2012/06/01)
Recent clinical data provided proof-of-concept for selective B-Raf inhibitors in treatment of B-RafV600E mutant melanoma. Pyrazolopyridine-type B-Raf inhibitors previously described by the authors are potent and selective but exhibit low solubility requiring the use of amorphous dispersion-based formulation for achieving efficacious drug exposures. Through structure-based design, we discovered a new class of highly potent aminopyrimidine-based B-Raf inhibitors with improved solubility and pharmacokinetic profiles. The hinge binding moiety possesses a basic center imparting high solubility at gastric pH, addressing the dissolution limitation observed with our previous series. In our search for an optimal linker-hinge binding moiety system, amide-linked thieno[3,2-d]pyrimidine analogues 32 and 35 (G945), molecules with desirable physicochemical properties, emerged as lead compounds with strong efficacy in a B-RafV600E mutant mouse xenograft model. Synthesis, SAR, lead selection, and evaluation of key compounds in animal studies will be described.
HETEROCYCLIC SULFONAMIDES AS RAF INHIBITORS
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Page/Page column 50, (2012/09/21)
Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I), stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 55, (2011/04/14)
Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 60, (2011/04/14)
Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or trea
RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 42-43, (2011/04/14)
Compounds of Formula II are useful for inhibition of Raf kinases. Methods of using compounds of Formula II and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or tr
RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 41, (2011/04/14)
Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or trea
RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 35, (2011/04/14)
Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment
