16279-73-5Relevant academic research and scientific papers
ARYL-BIPYRIDINE AMINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
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, (2019/07/13)
The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I): wherein A, X, Y, Z, Q, R1, R2, R3, R4, R5, and n are described herein.
Copper mediated C-H amination with oximes: En route to primary anilines
Xu, Lin-Lin,Wang, Xing,Ma, Biao,Yin, Ming-Xing,Lin, Hai-Xia,Dai, Hui-Xiong,Yu, Jin-Quan
, p. 5160 - 5164 (2018/06/21)
Here we report an efficient Cu(i)-mediated C-H amination reaction with oximes as amino donors to introduce NH2 groups directly. Various strongly coordinating heterocycles including quinoline, pyrimidine, pyrazine, pyrazole and triazole were tolerated well. The potential utility was further demonstrated in a late-stage modification of telmisartan (an antagonist for the angiotensin II receptor).
CYCLOHEXANEDIAMINE COMPOUNDS AND METHODS FOR THEIR PREPARATION
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Paragraph 0124, (2014/10/04)
The present invention provides processes for the preparation of cyclohexanediamine compounds of formula Ia and intermediates thereof. The compounds are useful as Syk kinase inhibitors and in various pharmaceutical compositions, and particularly useful for treating conditions mediated at least in part by Syk kinase activity.
SELECTIVE KINASE INHIBITORS
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Paragraph 0314; 0315, (2013/06/06)
Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
Facile one-pot synthesis of monosubstituted 1-aryl-1h-1,2,3-triazoles from arylboronic acids and prop-2-ynoic acid (=propiolic acid) or calcium acetylide (=calcium carbide) as acetylene source
Yang, Qing,Jiang, Yubo,Kuang, Chunxiang
experimental part, p. 448 - 454 (2012/05/04)
The synthesis of monosubstituted 1-aryl-1H-1,2,3-triazoles was achieved in a one-pot reaction from arylboronic acids and prop-2-ynoic acid or calcium acetylide (=calcium carbide), respectively, as a source of acetylene, with yields ranging from moderate to excellent (Scheme 1, Table 2). The reaction conditions were successfully applied to arylboronic acids, including analogs with various functionalities. Unexpectedly, the 1,2,3-triazole moiety promoted a regioselective hydrodebromination (Scheme 2). Copyright
Facile and quick synthesis of 1-monosubstituted aryl 1,2,3-triazoles: A copper-free [3+2] cycloaddition
Jiang, Yubo,Kuang, Chunxiang,Yang, Qing
experimental part, p. 289 - 292 (2011/02/28)
An efficient copper-free synthesis of 1-monosubstituted aryl 1,2,3-triazoles from sodium acetylide and aryl azides was developed, which was found suitable for various aryl azides and completed within 15 min at room temperature with moderate to excellent y
3-AZABICYCLO [3.1.0] HEXANE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 68, (2009/08/16)
The present invention relates to 3-azabicyclo[3.1.0]hexane derivatives, which are useful as vanilloid receptor (VR) ligands, methods of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.
Thiazole-4-carboxyamide derivatives
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Page/Page column 56, (2008/06/13)
The present invention is concerned with novel thiazole 4-carboxyamide derivatives of the general formula (I) and with methods for the preparation thereof, which compounds are useful as metabotropic glutamate receptor antagonists: wherein R1 to R4 are as defined in the specification.
