- PYRAZOLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS
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The present disclosure provides compounds of Formula (LA) and/ or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of ty r-osine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and p h ar-maceutically acceptable salts thereof
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Page/Page column 89
(2014/03/26)
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- Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers
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A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity.
- Martini, Elisabetta,Ghelardini, Carla,Dei, Silvia,Guandalini, Luca,Manetti, Dina,Melchiorre, Michele,Norcini, Monica,Scapecchi, Serena,Teodori, Elisabetta,Romanelli, Maria Novella
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p. 1431 - 1443
(2008/09/18)
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