169544-41-6Relevant articles and documents
MMPL3 INHIBITORS, COMPOSITIONS AND USES THEREOF
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Paragraph 0176, (2020/06/10)
Disclosed are inhibitors of mycobacterial membrane protein MmpL3, compositions comprising the inhibitors, and methods of preparation and use thereof.
FUSED PYRAZOLE COMPOUNDS AS CB1R ANTAGONISTS AND USES THEREOF
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Page/Page column 75, (2015/11/03)
The present invention relates to compounds of formula I, or isotopic forms, stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, S-oxides or N- oxides thereof, and processes for their preparation. The invention furt
Novel pyrazole derivatives as neutral CB1 antagonists with significant activity towards food intake
Manca, Ilaria,Mastinu, Andrea,Olimpieri, Francesca,Falzoi, Matteo,Sani, Monica,Ruiu, Stefania,Loriga, Giovanni,Volonterio, Alessandro,Tambaro, Simone,Bottazzi, Mirko Emilio Heiner,Zanda, Matteo,Pinna, Gerard Aime,Lazzari, Paolo
, p. 256 - 269 (2013/06/26)
In spite of rimonabant's withdrawal from the European market due to its adverse effects, interest in the development of drugs based on CB1 antagonists is revamping on the basis of the peculiar properties of this class of compounds. In particular, new strategies have been proposed for the treatment of obesity and/or related risk factors through CB1 antagonists, i.e. by the development of selectively peripherally acting agents or by the identification of neutral CB1 antagonists. New compounds based on the lead CB1 antagonist/inverse agonist rimonabant have been synthesized with focus on obtaining neutral CB1 antagonists. Amongst the new derivatives described in this paper, the mixture of the two enantiomers (±)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-(2-cyclohexyl-1- hydroxyethyl)-4-methyl-1H-pyrazole ((±)-5), and compound 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-[(Z)-2-cyclohexyl-1-fluorovinyl] -4-methyl-1H-pyrazole ((Z)-6), showed interesting pharmacological profiles. According to the preliminary pharmacological evaluation, these novel pyrazole derivatives showed in fact both neutral CB1 antagonism behaviour and significant in vivo activity towards food intake.