264209-16-7Relevant academic research and scientific papers
Novel Phenylpyridine Derivative and Pharmaceutical Composition Comprising the Same
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Paragraph 0179; 0180, (2020/08/12)
The present disclosure relates to a novel phenylpyridine derivative represented by Chemical Formula 1 and a pharmaceutical composition comprising the same, and the compound according to the present disclosure can be usefully used for the prevention or treatment of autoimmune diseases or cancers.
MODULATORS OF MYC FAMILY PROTO-ONCOGENE PROTEIN
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Paragraph 00125, (2020/09/08)
Disclosed herein are compounds and compositions having potency in the modulation of Myc family proteins. Such compounds and compositions can be used in the treatment of proliferative diseases, such as cancer, or in the treatment of disease where modulation of Myc family proteins is desired. Also disclosed herein are methods of using said compounds and compositions.
Dual-inhibitors of N-Myc and AURKA as potential therapy for neuroendocrine prostate cancer
Ban, Fuqiang,Cherkasov, Artem,Lallous, Nada,Leblanc, Eric,Lee, Joseph,Morin, Hélène,Singh, Kriti,Ton, Anh-Tien
, p. 1 - 19 (2020/11/11)
Resistance to androgen-receptor (AR) directed therapies is, among other factors, associated with Myc transcription factors that are involved in development and progression of many cancers. Overexpression of N-Myc protein in prostate cancer (PCa) leads to its transformation to advanced neuroendocrine prostate cancer (NEPC) that currently has no approved treatments. N-Myc has a short half-life but acts as an NEPC stimulator when it is stabilized by forming a protective complex with Aurora A kinase (AURKA). Therefore, dual-inhibition of N-Myc and AURKA would be an attractive therapeutic avenue for NEPC. Following our computer-aided drug discovery approach, compounds exhibiting potent N-Myc specific inhibition and strong anti-proliferative activity against several N-Myc driven cell lines, were identified. Thereafter, we have developed dual inhibitors of N-Myc and AURKA through structure-based drug design approach by merging our novel N-Myc specific chemical scaffolds with fragments of known AURKA inhibitors. Favorable binding modes of the designed compounds to both N-Myc and AURKA target sites have been predicted by docking. A promising lead compound, 70812, demonstrated low-micromolar potency against both N-Myc and AURKA in vitro assays and effectively suppressed NEPC cell growth.
Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy
Rana, Sandeep,Sonawane, Yogesh A.,Taylor, Margaret A.,Kizhake, Smitha,Zahid, Muhammad,Natarajan, Amarnath
supporting information, p. 3736 - 3740 (2018/10/24)
We synthesized a library of aminopyrazole analogs to systematically explore the hydrophobic pocket adjacent to the hinge region and the solvent exposed region of cyclin dependent kinases. Structure-activity relationship studies identified an optimal substitution for the hydrophobic pocket and analog 24 as a potent and selective CDK2/5 inhibitor.
AURORA KINASE INHIBITORS
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Paragraph 0256, (2014/12/12)
Disclosed herein inter alia are compositions and methods useful in the treatment of cancer and for modulating the activity of Aurora A kinase and/or a Myc family protein.
HETEROCYCLIC PYRIMIDINE CARBONIC ACID DERIVATIVES WHICH ARE USEFUL IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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Paragraph 0545; 0548-0549, (2013/12/04)
The present invention relates to a compound having the general formula (C), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
7-OXO-THIAZOLOPYRIDINE CARBONIC ACID DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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Paragraph 0542-0543; 0544-0545, (2013/12/04)
The present invention relates to a compound having the general formula (A), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
5-SULFANYLMETHYL-PYRAZOLO [1,5-A] PYRIMIDIN-7-OL DERIVATIVES AS CXCR2 ANTAGONISTS
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Page/Page column 31, (2008/12/05)
The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease.
Novel Compounds
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Page/Page column 52-53, (2008/06/13)
There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.
