55981-29-8Relevant articles and documents
ASPARAGINE ENDOPEPTIDASE (AEP) INHIBITORS, COMPOSITIONS, AND USES RELATED THERETO
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Page/Page column 4, (2020/12/11)
This disclosure relates to asparagine endopeptidase inhibitors and compositions and uses related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are useful for improving memory, treating or preventing cancer, neurodegenerative diseases, and cognitive disorders. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient.
Discovery of a series of potent arylthiadiazole H3 antagonists
Xiao, Dong,Palani, Anandan,Sofolarides, Michael,Huang, Ying,Aslanian, Robert,Vaccaro, Henry,Hong, Liwu,McKittrick, Brian,West Jr., Robert E.,Williams, Shirley M.,Wu, Ren-Long,Hwa, Joyce,Sondey, Christopher,Lachowicz, Jean
scheme or table, p. 861 - 864 (2011/03/18)
A series of 2-piperidinopiperidine-5-arylthiadiazoles was synthesized and subjected to a structure-activity relationship (SAR) investigation. The potency of this series was improved to the single digit nanomolar range. The key analogs were shown to be free of P450 issues, and they also maintained good ex vivo activity and brain penetration.
BIARYL SUBSTITUTED AZABICYCLIC ALKANE DERIVATIVES AS NICOTINIC ACETYLCHOLINE RECEPTOR ACTIVITY MODULATORS
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Page/Page column 41, (2009/06/27)
The invention relates to biaryl substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.