933791-33-4Relevant academic research and scientific papers
SOLID FORMS OF AN AZOLOPYRIMIDINE COMPOUND
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Paragraph 0207; 0211, (2020/02/14)
The present invention provides solid forms, solvates and hydrates of 3-[2-amino-6-(1-{[6-(2-hydroxypropan-2-yl)pyridine-2-yl]methyl}-1H-1,2,3-triazol-4-yl)pyrimidin-4-yl]-2-methylbenzonitrile, and methods of making and using the same.
ADENOSINE RECEPTOR BINDING COMPOUNDS
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Paragraph 00453; 00514-00515, (2020/02/06)
The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.
Development of a Scalable and Practical Synthesis of AB928, a Dual A2a/A2bReceptor Antagonist
Debien, Laurent P. P.,Jeffrey, Jenna L.,Leleti, Manmohan R.,Miles, Dillon H.,Powers, Jay P.,Rosen, Brandon R.,Sharif, Ehesan U.
, p. 1254 - 1261 (2020/08/14)
AB928 is a potent and selective dual antagonist of the A2a and A2b receptors, which is currently in clinical trials. Here, we report the development of two scalable and practical syntheses of AB928. The first-generation synthesis was used to successfully
DOSING WITH AN AZOLOPYRIMIDINE COMPOUND
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Paragraph 0205; 0209, (2019/09/04)
Provided herein are methods of treating a disease, disorder, or condition, mediated at least in part by the adenosine A2A receptor (A2AR) and/or the adenosine A2B receptor (A2BR) using Compound (I). In some embodiments, the disease or disorder is a cancer related disorder. Also provided herein are pharmaceutical compositions and single unit dosages of Compound (I).
AZOLOPYRIMIDINE FOR THE TREATMENT OF CANCER-RELATED DISORDERS
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Paragraph 0272, (2018/08/12)
Compound that is an inhibitor of at least one of the A2A and A2B adenosine receptors, and compositions containing the compound and methods for synthesizing the compound, are described herein. The use of such compound and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by the adenosine A2A receptor and/or the adenosine A2B receptor.
QUINAZOLINE-PYRIDINE DERIVATIVES FOR THE TREATMENT OF CANCER-RELATED DISORDERS
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Paragraph 0261, (2018/11/26)
Compounds that inhibit at least one of the A2A and A2B adenosine receptors, and compositions containing the compound and methods for synthesizing the compound, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by the adenosine A2A receptor and/or the adenosine A2B receptor.
A general synthesis of bis-α-acyloxy-1,4- and -1,5-diketones through catalytic oxidative opening of acylated THF and THP diols
Piccialli, Vincenzo,D'Errico, Stefano,Borbone, Nicola,Oliviero, Giorgia,Centore, Roberto,Zaccaria, Sabrina
, p. 1781 - 1789 (2013/04/10)
The first general synthesis of bis-α-acyloxy-1,4- and -1,5-diketones has been accomplished in a catalytic oxidative opening of bis-acylated THF and THP (tetrahydropyran) diols, which were synthesised by osmium- or ruthenium-catalysed oxidative cyclisation of 1,5- and 1,6-dienes. The overall sequence corresponds to the regioselective double ketoacyloxylation of the starting diene. The synthesised bis-α-acyloxy-1,5-dicarbonyl compounds have been transformed into pyridine-based oxido pincer ligands or pyrazinedimethanol substances, leading to the discovery of unprecedented aromatisation routes. The first general synthesis of bis-α-acyloxy-1,4- and -1,5-diketones is reported. The process features the catalytic oxidative opening of bis-acylated THF and THP diols, which were synthesised by the transition-metal-mediated oxidative cyclisation of 1,5- and 1,6-dienes. The 1,5-diketone products were cyclised to give pyridinedimethanol derivatives. New aromatisation modes have been disclosed. Copyright
TRIAZOLO [4, 5-D] PYRAMIDINE DERIVATIVES AND THEIR USE AS PURINE RECEPTOR ANTAGONISTS
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Page/Page column 56, (2010/01/30)
Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are. disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.
