- PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
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Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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Page/Page column 88
(2016/07/05)
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- SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3,4-B] PYRIDINE AND PYRAZOLO [3,4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3,4-b] pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo [3,4-b] pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson?s disease, Alzheimer?s disease, Down?s Syndrome, Huntington?s disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated there with using compounds and pharmaceutical compositions including the compounds.
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Page/Page column 21-22
(2012/10/18)
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- Synthesis of pyrimidine-modified NHC ruthenium-alkylidene catalysts and their application in RCM, CM, em and ROMP reactions
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A new type of N-heterocyclic carbene bearing ruthenium olefin metathesis catalyst was prepared through the incorporation of a chelated pyrimidinyl methylene subunit, in which electron-rich substituents were attached to stabilize the ruthenium complexes. These catalysts were successfully used in various types of olefin metathesis reactions, including ring-closing metathesis (RCM), cross-metathesis (CM), enyne metathesis (EM), and ring-opening metathesis polymerization (ROMP) reactions. The results therein showed that the presence of an electron-deficient pyrimidine structure greatly enhanced the new NHC ruthenium complexes' catalytic activities. New N-heterocyclic carbene bearing ruthenium olefin metathesis catalysts were synthesized and applied in various types of olefin metathesis reactions, including ring-closing metathesis, cross-metathesis, enyne metathesis, and ring-opening metathesis polymerization reactions. Copyright
- Wu, Guang-Long,Cao, Sheng-Li,Chen, Jian,Chen, Zili
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p. 6777 - 6784
(2013/01/15)
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- HETEROCYCLIC MODULATORS OF GPR119 FOR TREATMENT OF DISEASE
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Disclosed herein are compounds and methods which may be useful as inhibitors of GPRl 19 for the treatment or prevention of diseases including cardiovascular and metabolic diseases.
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Page/Page column 86-87
(2010/08/09)
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- Process chemistry related to the experimental rice herbicide 2,2-dimethyl-1-(4-methylthio-5-pyrimidinyl)indane
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Two concise syntheses of the experimental rice herbicide 2,2-dimethyl-1-(4-methylthio-5-pyrimidinyl)indane are reported. The initial synthesis relies on a low-temperature addition of 5-lithio-4-methylthiopyrimidine to 2,2-dimethyl-1-indanone to construct the pyrimidinylindane system. Process improvements to this route are described and resulted in the preparation of 90 kg of the title compound on pilot plant scale. Economics dictated the need to identify a new synthetic route which utilized inexpensive raw materials. Detailed herein is the initial discovery of a new route which features a novel combination of dissolving metal reduction/formylation/cyclization to construct the requisite pyrimidine ring. Process improvements to this chemistry have allowed us to deliver an appropriately substituted pyrimidinylindane in a minimal number of synthetic operations.
- Dietsche, Thomas J.,Gorman, David B.,Orvik, Jon A.,Roth, Gary A.,Shiang, William R.
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p. 275 - 285
(2013/09/07)
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