- PIPERIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The invention relates to new piperidine derivatives of the formula (I) to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 65
(2013/06/27)
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- New piperidine derivatives, pharmaceutical compositions and uses thereof
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The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Paragraph 0351; 0352
(2013/06/26)
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- ETHYNE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them
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Page/Page column 83
(2012/03/27)
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- New compounds, pharmaceutical compositions and uses thereof
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The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 35
(2012/09/05)
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- Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of β-amyloid1-42 secretion
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Flurbiprofen, a nonsteroidal antiinflammatory drug (NSAID), has been recently described to selectively inhibit β-amyloid1-42 (Aβ42) secretion, the most toxic component of the senile plaques present in the brain of Alzheimer patients. The use of this NSAID in Alzheimer's disease (AD) is hampered by a significant gastrointestinal toxicity associated with cyclooxygenase (COX) inhibition. New flurbiprofen analogues were synthesized, with the aim of increasing Aβ42 inhibitory potency while removing anti-COX activity. In vitro ADME developability parameters were taken into account in order to identify optimized compounds at an early stage of the project. Appropriate substitution patterns at the alpha position of flurbiprofen allowed for the complete removal of anti-COX activity, while modifications at the terminal phenyl ring resulted in increased inhibitory potency on Aβ42 secretion. In rats, some of the compounds appeared to be well absorbed after oral administration and to penetrate into the central nervous system. Studies in a transgenic mice model of AD showed that selected compounds significantly decreased plasma Aβ42 concentrations. These new flurbiprofen analogues represent potential drug candidates to be developed for the treatment of AD.
- Peretto, Ilaria,Radaelli, Stefano,Parini, Carlo,Zandi, Michele,Raveglia, Luca F.,Dondio, Giulio,Fontanella, Laura,Misiano, Paola,Bigogno, Chiara,Rizzi, Andrea,Riccardi, Benedetta,Biscaioli, Marcello,Marchetti, Silvia,Puccini, Paola,Catinella, Silvia,Rondelli, Ivano,Cenacchi, Valentina,Bolzoni, Pier Tonino,Caruso, Paola,Villetti, Gino,Facchinetti, Fabrizio,Del Giudice, Elda,Moretto, Nadia,Imbimbo, Bruno P.
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p. 5705 - 5720
(2007/10/03)
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- Enantioselective syntheses of 2-arylpropanoic acid non-steroidal antiinflammatory drugs and related compounds
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(S)-2-[4′-(2″-Methylpropyl)phenylpropanoic acid (ibuprofen) and (S)-2-(3′-benzoylphenyl)propanoic acid (ketoprofen) have been synthesised in high enantiomeric excess. Control of stereochemistry was achieved by a combination of Sharpless epoxidalion followed by catalytic hydrogenolysis of the introduced benzylic epoxide oxygen bond. Also, the coupling of organic compounds in the presence of palladium with enantiopure 2-(3-iodophenyl)propanoic and 2-(4-iodophenyl)propanoic acids, prepared by the methodology above, is a general method for the synthesis of optically active arylpropanoic acids.
- Hamon, David P.G.,Massy-Westropp, Ralph A.,Newton, Josephine L.
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p. 12645 - 12660
(2007/10/02)
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- Novel 2-[4-(3-methyl-2-thienyl)phenyl]propionic acid and pharmaceutically acceptable salt thereof and method for treating symptoms of inflammation and pain
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A novel 2-[4-(3-methyl-2-thienyl)phenyl]propionic acid and a pharmaceutically acceptable salt thereof. These compounds are useful for treating symptoms of inflammation and pain in mammals including man. This disclosure relates to such compounds, a process
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