- Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor
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Established therapy in Alzheimer's disease involves potentiation of the endogenous orthosteric ligand, acetylcholine, at the M1 muscarinic receptors found in higher concentrations in the cortex and hippocampus. Adverse effects, due to indiscrim
- Mistry, Shailesh N.,Valant, Celine,Sexton, Patrick M.,Capuano, Ben,Christopoulos, Arthur,Scammells, Peter J.
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p. 5151 - 5172
(2013/07/26)
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- BENZYL-SUBSTITUTED QUINOLONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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The present invention is directed to benzyl-substituted quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheime
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Page/Page column 23-24
(2008/06/13)
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- QUINOLONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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The present invention is directed to quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, pain or sleep disorders, and to novel M1 receptor positive allosteric modulator compounds of formulae (II) to (VIII). The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases in which the M1 receptor is involved.
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Page/Page column 33
(2008/06/13)
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- Synthesis of fluoro-4-hydroxyquinoline-3-carboxylic acids by the Gould-Jacobs reaction
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The synthesis of several fluoro-4-hydroxyquinoline-3-carboxylic acids by the Gould-Jacobs reaction is presented. These quinolines are important intermediates for the preparation of antibacterial fluoroquinolones.
- Leyva, Elisa,Monreal, Elena,Hernandez, Alma
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- An NMR study of halogenated 1,4-dihydro-1-ethyl-4-oxoquinoline-3-carboxylates
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Ethyl 1,4-dihydro-1-ethyl-4-oxoquinoline-3-carboxylate and 29 of its mono-, di-and tri-fluoro and/or -chloro derivatives were synthesized and their 1H, 13C and 19F NMR spectra were recorded. 1H, 13C and 19F chemical shifts, JHH, JFH, JCF and JFF coupling constants are reported. The 13C substituent chemical shift values of the chloro and fluoro substituents were calculated by linear multiple regression.
- Podanyi, Benjamin,Kereszturi, Geza,Vasvari-Debreczy, Lelle,Chinoin, Istvan Hermecz,Toth, Gabor
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p. 972 - 978
(2007/10/03)
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