213744-81-1Relevant academic research and scientific papers
SUBSTITUTED PYRROLO[2,3-D]PYRIMIDINES COMPOUNDS AS RET KINASE INHIBITORS
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Paragraph 00783; 00786, (2019/08/08)
Provided herein are compounds of the Formula I: [INSERT FORMULA I] and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2 and Ry have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
Enantioselective Synthesis of Pyrrolopyrimidine Scaffolds through Cation-Directed Nucleophilic Aromatic Substitution
Cardenas, Mariel M.,Toenjes, Sean T.,Nalbandian, Christopher J.,Gustafson, Jeffrey L.
, p. 2037 - 2041 (2018/04/12)
The catalytic enantioselective synthesis of 3-aryl-substituted pyrrolopyrimidines (PPYs), a common motif in drug discovery, is achieved through a kinetic resolution via quaternary ammonium salt-catalyzed nucleophilic aromatic substitution (SNAr). Both enantioenriched products and starting materials can be functionalized with no observed racemization to give enantiodivergent access to diverse chiral analogues of an important class of kinase inhibitor. One of the compounds was found to be a potent and selective inhibitor of breast tumor kinase.
FUSED PYRIMIDINE COMPOUND OR SALT THEREOF
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Paragraph 1526; 1527, (2018/02/06)
The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malign
NOVEL FUSED PYRIMIDINE COMPOUND OR SALT THEREOF
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Paragraph 1287-1289, (2018/02/28)
The problem to be solved by the present invention is to provide a novel compound having RET inhibitory activity. The present invention also provides a pharmaceutical preparation that is useful for the prevention and/or treatment of RET-related diseases, p
N-(SUBSTITUTED-PHENYL)-SULFONAMIDE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 24, (2018/04/11)
The invention relates to N-(substituted-phenyl)-sulfonamide compounds, which are extremely useful as inhibitors of protein kinases (e.g. PERK kinase) and accordingly can be used for the treatment of cell proliferative disorders, such as cancer, or diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.
Benzothiazole Kinase Inhibitors and Methods of Use
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, (2015/09/22)
The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PI3 kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.
Novel pyrazolo- and pyrrolo-pyrimidines and uses thereof
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, (2008/06/13)
The invention relates to compounds of the general formula: in which RA-RC and W are as defined herein, and to their preparation and use.
PYRROLO 2,3D]PYRIMIDINES AND THEIR USE AS TYROSINE KINASE INHIBITORS
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, (2008/06/13)
Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl gr
