851233-58-4Relevant academic research and scientific papers
INHIBITING UBIQUITIN SPECIFIC PEPTIDASE 30
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, (2019/04/30)
The present disclosure relates to chemical entities useful as inhibitors of Ubiquitin Specific Peptidase 30 (USP30), pharmaceutical compositions comprising the chemical entities, and methods of using the chemical entities. The chemical entities as disclosed herein can be useful in the treatment of a disease, disorder, or condition involving mitochondrial dysfunction, including neurodegenerative diseases, motor neuron diseases, metabolic disorders, and cancers, among other ailments.
NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
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Page/Page column 67, (2008/12/07)
The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, R4, L2 and A are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS AND USES THEREOF
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Page/Page column 128, (2008/06/13)
The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in th
Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease
Helal, Christopher J.,Sanner, Mark A.,Cooper, Christopher B.,Gant, Thomas,Adam, Mavis,Lucas, John C.,Kang, Zhijun,Kupchinsky, Stanley,Ahlijanian, Michael K.,Tate, Bonnie,Menniti, Frank S.,Kelly, Kristin,Peterson, Marcia
, p. 5521 - 5525 (2007/10/03)
High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide (1). This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320 nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved.
