876322-58-6Relevant academic research and scientific papers
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors
Smith, Aaron,Ni, Zhi-Jie,Poon, Daniel,Huang, Zilin,Chen, Zheng,Zhang, Qiong,Tandeske, Laura,Merritt, Hanne,Shoemaker, Kevin,Chan, John,Kaufman, Susan,Huh, Kay,Murray, Jeremy,Appleton, Brent A.,Cowan-Jacob, Sandra W.,Scheufler, Clemens,Kanazawa, Takanori,Jansen, Johanna M.,Stuart, Darrin,Shafer, Cynthia M.
supporting information, p. 5221 - 5224 (2017/11/01)
A series of imidazo[1,2-a]pyridin-6-yl-benzamide analogs was designed as inhibitors of B-RAFV600E. Medicinal chemistry techniques were employed to explore the SAR for this series and improve selectivity versus P38 and VEGFR2.
Design and Discovery of N-(2-Methyl-5′-morpholino-6′-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers
Nishiguchi, Gisele A.,Rico, Alice,Tanner, Huw,Aversa, Robert J.,Taft, Benjamin R.,Subramanian, Sharadha,Setti, Lina,Burger, Matthew T.,Wan, Lifeng,Tamez, Victoriano,Smith, Aaron,Lou, Yan,Barsanti, Paul A.,Appleton, Brent A.,Mamo, Mulugeta,Tandeske, Laura,Dix, Ina,Tellew, John E.,Huang, Shenlin,Mathews Griner, Lesley A.,Cooke, Vesselina G.,Van Abbema, Anne,Merritt, Hanne,Ma, Sylvia,Gampa, Kalyani,Feng, Fei,Yuan, Jing,Wang, Yingyun,Haling, Jacob R.,Vaziri, Sepideh,Hekmat-Nejad, Mohammad,Jansen, Johanna M.,Polyakov, Valery,Zang, Richard,Sethuraman, Vijay,Amiri, Payman,Singh, Mallika,Lees, Emma,Shao, Wenlin,Stuart, Darrin D.,Dillon, Michael P.,Ramurthy, Savithri
, p. 4869 - 4881 (2017/06/28)
RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant tumors has been established in genetically engineered mouse models and human tumor cells. To date
DERIVATIVES OF 1 H-PYRAZOLO[3,4-B]PYRIDINE AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
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Paragraph 00222-00223; 00347-00348, (2015/03/13)
The present invention discloses compounds according to Formula (I): wherein R1, R2, R3, R4, L, and X are as defined herein. The present invention relates to compounds,methods for their production, pharmaceutical
NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
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Paragraph 0450; 0451; 0452; 0658; 0659; 0660, (2015/03/28)
The present invention discloses compounds according to Formula I: wherein R1, R2, R3, R4, L, and X are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical
BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS
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Paragraph 0156; 0157, (2014/09/29)
The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
2-AMINOQUINAZOLINE DERIVATIVE
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, (2011/01/12)
A 2-aminoquinazoline derivative represented by formula (I) {wherein R1 represents a hydrogen atom, or the like, R2 represents a hydrogen atom, R3 represents formula (II) [wherein A1 represents formula (III), or the like, R8 represents lower alkyl, or the like, and R9 represents optionally substituted aryl, or the like], R4 represents hydroxy, or the like, and R5 represents optionally substituted aryl, or the like}, or a pharmaceutically acceptable salt thereof is provided.
EPHA4 RTK INHIBITORS FOR TREATMENT OF NEUROLOGICAL AND NEURODEGENERATIVE DISORDERS AND CANCER
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Page/Page column 17, (2010/08/08)
The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.
USE OF TRIFLUOROMETHYL SUBSTITUTED BENZAMIDES IN THE TREATMENT OF NEUROLOGICAL DISORDERS
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Page/Page column 34, (2008/06/13)
The invention relates to methods of using the compounds of the invention, including trifluoromethyl substituted benzamide compounds and salts thereof, as well as pharmaceutical compositions comprising the same, in the treatment of Eph receptor-related (e.g., neurological) injuries and disorders. The invention also relates to modulating the activity of an Eph receptor in a cell, stimulating neural regeneration, and reversing neuronal degeneration, by administering a compound of the invention to a cell or subject in an effective amount.
Trifluoromethyl substituted benzamides as kinase inhibitors
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Page/Page column 19, (2008/06/13)
The invention relates to trifluoromethyl substituted benzamide compounds of the formula I, pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases, especially of ephrin receptor kinases, and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.
