- AMINOPYRAZINE COMPOUNDS AS HPK1 INHIBITOR AND THE USE THEREOF
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Disclosed herein is an aminopyrazine compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating HPK1 related disorders or diseases by using the compound disclosed herein.
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Page/Page column 94-95
(2021/02/26)
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- Cu(I)/sucrose-catalyzed hydroxylation of arenes in water: The dual role of sucrose
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A protocol for the hydroxylation of aryl halides catalyzed by copper(I) and sucrose in neat water has been developed. The dual role of sucrose, the reaction pathway, and the high selectivity for hydroxylation were investigated using a combination of experimental and theoretical techniques. This journal is
- Murata, Shigeo,Takagi, Mio,Takita, Ryo,Watanabe, Ayako,Watanabe, Kohei
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supporting information
p. 7827 - 7831
(2020/11/02)
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- MACROCYCLIC AZOLOPYRIDINE DERIVATIVES AS EED AND PRC2 MODULATORS
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The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula (I), or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.
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Paragraph 1259
(2020/10/09)
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- PYRROLIDINE DERIVATIVES AS PPAR AGONISTS
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The present invention discloses a class of pyrrolidine derivatives as PPAR agonist, and their use for the treatment of some diseases of PPAR receptor-associated pathways (such as nonalcoholic steatohepatitis and concurrent fibrosis, insulin resistance, primary biliary cholgangitis, dyslipidenmia, hyperlipidemia, hypercholesterolemia, atherosclerosis, hypertriglyceridemia, cardiovascular disease, obesity or the like). In particular, the present invention discloses a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof.
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Paragraph 0596-0598
(2019/08/02)
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- Regioselective palladium-catalyzed C–H arylation of 4-alkoxy and 4-thioalkyl pyrazoles
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A methodology for the palladium-catalyzed regioselective C–H arylation of electron rich pyrazoles has been developed. New ligands and mild conditions (70–90 °C) have been identified for this transformation. An intramolecular application of the methodology provided a novel synthetic route for the regioselective synthesis of 1,5-dihydroisochromeno[4,3-c]pyrazoles and 1,5-dihydroisothiochromeno[4,3-c]pyrazoles.
- Vernier, William F.,Gomez, Laurent
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supporting information
p. 4587 - 4590
(2017/11/15)
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- COMPOUNDS
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The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example Alzheimer's disease.
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Page/Page column 138
(2016/02/12)
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- Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives
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Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4 (JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (e.g., 1), further optimization led to the identification of non-carboxylate inhibitors derived from pyrido[3,4-d]pyrimidin-4(3H)-one. A number of exemplars such as compound 41 possess interesting activity profiles in KDM4C and KDM5C biochemical and target-specific, cellular mechanistic assays.
- Westaway, Susan M.,Preston, Alex G. S.,Barker, Michael D.,Brown, Fiona,Brown, Jack A.,Campbell, Matthew,Chung, Chun-Wa,Drewes, Gerard,Eagle, Robert,Garton, Neil,Gordon, Laurie,Haslam, Carl,Hayhow, Thomas G.,Humphreys, Philip G.,Joberty, Gerard,Katso, Roy,Kruidenier, Laurens,Leveridge, Melanie,Pemberton, Michelle,Rioja, Inma,Seal, Gail A.,Shipley, Tracy,Singh, Onkar,Suckling, Colin J.,Taylor, Joanna,Thomas, Pamela,Wilson, David M.,Lee, Kevin,Prinjha, Rab K.
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p. 1370 - 1387
(2016/03/05)
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- QUINAZOLINE DERIVATIVES AS ERBB RECEPTOR TYROSINE KINASES
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The invention concerns quinazoline derivatives of the formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, X1, Q1, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.
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Page/Page column 225-226
(2010/02/15)
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