70151-22-3Relevant articles and documents
SGC STIMULATORS
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Paragraph 00263, (2018/05/27)
The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutical formulations comprising them and their uses thereof, alone or in combination with one or more additional agents, for treating various diseases, wherein an inc
BACE1 INHIBITORS
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Page/Page column 132, (2016/05/02)
The present invention provides a compound of formula I, having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
Structural Investigation of the Naphthyridone Scaffold: Identification of a 1,6-Naphthyridone Derivative with Potent and Selective Anti-HIV Activity
Tabarrini, Oriana,Massari, Serena,Sancineto, Luca,Daelemans, Dirk,Sabatini, Stefano,Manfroni, Giuseppe,Cecchetti, Violetta,Pannecouque, Christophe
experimental part, p. 1249 - 1257 (2012/05/04)
Building upon a large, previously reported series of anti-HIV 6-desfluoroquinolones endowed with a peculiar mechanism of action, the inhibition of Tat-mediated transcription, replacement of the quinolone nucleus with a naphthyridone core was shown to be very productive. In this work, the naphthyridone scaffold was investigated in depth by synthesizing various analogues. This led to the identification of NM13 as the most selective derivative obtained in MT-4 cells. It is the result of the successful combination of the 1,6-naphthyridone nucleus and the C7 benzothiazolpiperazine group, which, for the first time, not only grants potent anti-HIV activity but displays very high selectivity. Further studies aimed at a more thorough investigation of the anti-HIV profile of this new derivative are in progress. Best in class: The naphthyridone scaffold was investigated in depth by synthesizing various analogues that were tested for their anti-HIV activity. This led to the identification of a very potent and nontoxic compound, NM13, as the most selective anti-HIV derivative ever obtained in the quinolone class of transcription inhibitors. It is the result of a powerful combination of the 1,6-naphthyridone nucleus and the C7 benzothiazolpiperazine group.