301221-57-8Relevant academic research and scientific papers
Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques
Di Lello, Paola,Pastor, Richard,Murray, Jeremy M.,Blake, Robert A.,Cohen, Frederick,Crawford, Terry D.,Drobnick, Joy,Drummond, Jason,Kategaya, Lorna,Kleinheinz, Tracy,Maurer, Till,Rougé, Lionel,Zhao, Xianrui,Wertz, Ingrid,Ndubaku, Chudi,Tsui, Vickie
, p. 10056 - 10070 (2018/01/10)
USP7 is a deubiquitinase implicated in destabilizing the tumor suppressor p53, and for this reason it has gained increasing attention as a potential oncology target for small molecule inhibitors. Herein we describe the biophysical, biochemical, and comput
4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
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, (2014/09/16)
The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
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, (2013/04/24)
The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them
INHIBITORS OF SPHINGOSINE KINASE
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, (2012/10/08)
The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12,
INHIBITORS OF AKT ACTIVITY
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Page/Page column 131, (2008/06/13)
Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
HYDANTOIN DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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Page/Page column 140, (2008/06/13)
This invention relates to compounds of Formula (1) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF- or combinations thereof.
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin- 1-yl-acetic acid antagonists of the human CCR5 chemokine receptor
Shankaran,Donnelly, Karla L.,Shah, Shrenik K.,Guthikonda, Ravindra N.,MacCoss, Malcolm,Mills, Sander G.,Gould, Sandra L.,Malkowitz, Lorraine,Siciliano, Salvatore J.,Springer, Martin S.,Carella, Anthony,Carver, Gwen,Hazuda, Daria,Holmes, Karen,Kessler, Joseph,Lineberger, Janet,Miller, Michael D.,Emini, Emilio A.,Schleif, William A.
, p. 3419 - 3424 (2007/10/03)
Efforts toward the exploration of the title compounds as CCR5 antagonists are disclosed. The basis for such work stems from the fact that cellular proliferation of HIV-1 requires the cooperative assistance of both CCR5 and CD4 receptors. The synthesis and SAR of pyrrolidineacetic acid derivatives as CCR5 antagonists displaying potent binding and antiviral properties in a HeLa cell-based HIV-1 infectivity assay are discussed.
