- Design and synthesis of a hybrid series of potent and selective agonists of α7 nicotinic acetylcholine receptor
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α7 nicotinic acetylcholine receptor agonists are promising therapeutic candidates for the treatment of cognitive impairment. As a follow up of our internal medicinal chemistry program we investigated a novel series of α7 nAChR agonists. Starting from molecular docking studies on two series of molecules recently developed in our laboratories, an alternative scaffold was designed attempting to combine the optimal features of these previously identified urea and pyrazole compounds. Based on our previous SAR knowledge and on predicted drug-like properties, a small library was synthesized in parallel manner, affording compounds with excellent α7 nAChR activity, selectivity and preliminary ADME profile.
- Nencini, Arianna,Castaldo, Cristiana,Comery, Thomas A.,Dunlop, John,Genesio, Eva,Ghiron, Chiara,Haydar, Simon,Maccari, Laura,Micco, Iolanda,Turlizzi, Elisa,Zanaletti, Riccardo,Zhang, Jean
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p. 401 - 418
(2014/04/17)
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- MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF
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Compounds with α7 nicotinic acetylcholine receptor (α7 nAChR) agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric diseases.
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- SORDARIN DERIVATIVES FOR PREVENTING OR TREATING INFECTIOUS DISEASES CAUSED BY PATHOGENIC MICROORGANISMS
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This invention relates to a new sordarin derivative or a pharmaceutically acceptable salt thereof, which has antimicrobial activities (especially, antifungal activities), to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases in a human being or an animal.
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Page/Page column 99; 124
(2009/12/05)
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- MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF
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Compounds with α7 nicotinic acetylcholine receptor (α7 nAChR) agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric diseases.
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Page/Page column 23-24
(2008/06/13)
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- Benzenesulphonamide derivatives, method for production and use thereof for treatment of pain
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The present invention concerns novel benzenesulphonamide compounds, defined by formula I and the description, their method of preparation and their use in therapy.
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Page/Page column 19
(2008/06/13)
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- Therapeutic agents
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Compounds of formula I STR1 and pharmaceutically acceptable salts thereof in which R1, R2 and R3 independently represent hydrogen, hydroxy, halo, alkyl or alkoxy; ALK1 represents a C2-6 alkylene chain optionally substituted by one or more C1-2 alkyl groups; Y represents a piperidine ring which is attached through nitrogen to ALK1 ; R4 represents hydrogen or a C1-4 alkyl group; the broken line in --- represents a bond, or is absent and the free valency on Y is taken up by hydrogen and the free valency on CR4 is taken up by hydrogen or a C1-4 alkyl group; ALK2 is absent or represents a C1-4 alkylene chain optionally substituted by one or more C1-2 alkyl groups; and R5 and R6 independently represent hydrogen, alkyl, phenyl, alkyl (optionally substituted) or R5 and R6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring (with a proviso); are disclosed which are antiinflammatory, antiallergic and immunomodulatory agents. Compositions containing these compounds and processes to prepare these compounds are also disclosed.
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