- HETEROARYL COMPOUNDS AS INHIBITORS OF PROGRAMMED NECROSIS PATHWAY, COMPOSITION AND METHOD USING THE SAME
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The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to the programmed necrosis pathway.
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Paragraph 00231; 00234-00235
(2021/07/10)
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- SALT OF PYRAZOLOQUINOLINE DERIVATIVE, AND CRYSTAL THEREOF
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The present invention provides a salt of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric
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Paragraph 0166-0168
(2016/05/02)
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- HETEROCYCLIC KINASE INHIBITORS
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Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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- Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors
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The synthesis and biological evaluation of two novel series of potent and selective FTase inhibitors are described. Two novel series of potent and selective FTase inhibitors have been synthesized using structure-based design. Medicinal chemistry efforts led to the discovery of compound 4e with potent cellular activity and good oral bioavailability in dog. A synthetic route toward novel heterocycles 1,5-dimethyl-6-oxo-4-aryl-1,6-dihydro-pyridine-2- carbonitrile was established. The structure of compound 5c was confirmed by X-ray crystallography.
- Wang, Le,Lin, Nan-Horng,Li, Qun,Henry, Rodger F.,Zhang, Haiying,Cohen, Jerome,Gu, Wen-Zhen,Marsh, Kennan C.,Bauch, Joy L.,Rosenberg, Saul H.,Sham, Hing L.
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p. 4603 - 4606
(2007/10/03)
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- Farnesyltransferase inhibitors
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Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.
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- Farnesyltransferase inhibitors
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Substituted imidazoles and thiazoles having the formula are useful for inhibiting farnesyltransferase. Also disclosed are farnesyltransferase-inhibiting compositions and methods of inhibiting farnesyltransferase in a patient.
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- First Metalation of Aryl Iodides: Directed Ortho-Lithiation of Iodopyridines, Halogen-Dance, and Application to Synthesis
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Metalation of iodopyridines was succesfully achieved by LDA at low temperature.In many cases, lithiation is ortho directed by the iodo group which subsequently ortho-migrates very fast to give stabilized iodolithiopyridines.This procedure was applied to 2
- Rocca, P.,Cochennec, C.,Marsais, F.,Thomas-dit-Dumont, L.,Mallet, M.,et al.
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p. 7832 - 7838
(2007/10/02)
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