301221-56-7Relevant 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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Page/Page column, (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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Page/Page column 64, (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
Asymmetric N-heterocyclic carbene catalyzed addition of enals to nitroalkenes: Controlling stereochemistry via the homoenolate reactivity pathway to access δ-lactams
White, Nicholas A.,Dirocco, Daniel A.,Rovis, Tomislav
supporting information, p. 8504 - 8507 (2013/07/19)
An asymmetric intermolecular reaction between enals and nitroalkenes to yield δ-nitroesters has been developed, catalyzed by a novel chiral N-heterocyclic carbene. Key to this work was the development of a catalyst that favors the δ-nitroester pathway over the established Stetter pathway. The reaction proceeds in high stereoselectivity and affords the previously unreported syn diastereomer. We also report an operationally facile two-step, one-pot procedure for the synthesis of δ-lactams.
INHIBITORS OF SPHINGOSINE KINASE
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Page/Page column 60, (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,
Catalytic asymmetric intermolecular stetter reaction of enals with nitroalkenes: Enhancement of catalytic efficiency through bifunctional additives
Dirocco, Daniel A.,Rovis, Tomislav
supporting information; experimental part, p. 10402 - 10405 (2011/08/22)
An asymmetric intermolecular Stetter reaction of enals with nitroalkenes catalyzed by chiral N-heterocyclic carbenes has been developed. The reaction rate and efficiency are profoundly impacted by the presence of catechol. The reaction proceeds with high selectivities and affords good yields of the Stetter product. Internal redox products were not observed despite of the protic conditions. The impact of catechol has been found to be general, facilitating far lower catalyst loadings than were previously achievable.
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.
