- FUSED RING HETEROARYL COMPOUNDS AND THEIR USE AS TRK INHIBITORS
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The disclosure provides novel chemical compounds represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof. The compounds can be used as an inhibitor of Trk and are useful in the treatment of pain, cancer, inflammation, neurodegenerative disease and certain infectious diseases. In some compounds of Formula I, Q is —CH═CR3C(O)NR4R5, —C≡CC(O)NR4R5, or
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- Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9
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The serine-threonine kinase CDK9 is a target of emerging interest for the development of anti-cancer drugs. There are multiple lines of evidence linking CDK9 activity to cancer, including the essential role this kinase plays in transcriptional regulation
- Phillipson, Louisa J.,Segal, David H.,Nero, Tracy L.,Parker, Michael W.,Wan, Soo San,De Silva, Melanie,Guthridge, Mark A.,Wei, Andrew H.,Burns, Christopher J.
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p. 6280 - 6296
(2015/09/28)
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- HETEROAROMATIC COMPOUNDS AS PI3 KINASE MODULATORS AND METHODS OF USE
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The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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Paragraph 0308; 0309; 0310
(2014/09/03)
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- FUSED HETEROCYCLES AS LCK INHIBITORS
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There is provided fused heterocycles of imidazopyridazine or pyrazolopyrimidine derivative represented by the formula (I), which have excellent Lck inhibitory activity and are useful for a medicament particularly an immunosuppressive agent. [wherein one of Y and Z is C atom, and the other is N atom; -X-10 is -N (R1) - or the like, -R1 is hydrogen or the like, -A- is bond or the like, is cycloalkyl, aryl or the like, -E- is bond or the like, -R3 is aryl, aromatic heterocycle or the like, -R4, -R5 and -R6 are the same or different, each being hydrogen or the like.]
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Page/Page column 31
(2010/11/25)
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