70151-22-3Relevant academic research and scientific papers
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 50, (2017/03/08)
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.
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.
FAAH INHIBITORS
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Page/Page column 153-154, (2012/07/13)
The present disclosure relates to compounds useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the com
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.
NOVEL COMPOSITIONS AND METHODS OF USE
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Page/Page column 117, (2009/09/04)
Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.
NEW COMPOUNDS 384
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Page/Page column 74-75, (2008/06/13)
The present invention relates to a compound of formula (I) as a free base or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical formulations containing said compound and to the use of said compound in therapy.
