- First metal-free synthesis of tetracyclic pyrido and pyrazino thienopyrimidinone molecules
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We report herein a new metal free synthetic pathway to generate tetracyclic compounds from 3-aminothieno[3,2-b]pyridine-2-carboxylate. To enlarge the molecular diversity, we studied the Suzuki coupling of 9-chloro-6H-pyrido[1,2-a]pyrido[2,3:4,5]thieno[3,2-d]pyrimidin-6-one and several boronic acids were easily introduced.
- Aounzou, Mohammed,Campos, Joana F,Loubidi, Mohammed,Berteina-Raboin, Sabine
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- SULFONAMIDES AS TRPM8 MODULATORS
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Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
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- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
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Page/Page column 13
(2012/10/08)
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- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
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Page/Page column 25
(2011/07/30)
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- Synthesis of new thieno[3,2-b]pyridine derivatives by palladium-catalyzed couplings and intramolecular cyclizations
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Two methyl 3-aminothieno[3,2-b]pyridine-2-carboxylates were prepared from 3-fluoro or 3-nitropicolinonitriles and methyl thioglycolate in DMF/KOH(aq). From the unsubstituted precursor in the pyridine ring, di(hetero)arylamines were obtained by C-N Buchwald-Hartwig coupling with bromonitrobenzenes and with 2-bromopyridine. In the latter case a tetracyclic compound was formed by intramolecular cyclization. Using a brominated derivative in the pyridine ring as a coupling component, it was possible to synthesize C-C (Suzuki and Sonogashira) and C-N (Buchwald-Hartwig) coupling products and a tetracyclic compound obtained by bifunctionalization of the thienopyridine system.
- Calhelha, Ricardo C.,Queiroz, Maria-Jo?o R.P.
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experimental part
p. 281 - 283
(2010/03/26)
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- SULFONAMIDES AS TRPM8 MODULATORS
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ABSTRACT Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein A, B, G, Y, R1, R2, R3 and R4 are defined herein
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Page/Page column 215-216
(2009/03/07)
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- Azabicyclic-substituted fused-heteroaryl compounds for the treatment of disease
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The invention provides compounds of Formula I: wherein Azabicyclo is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which α7 is known to be involved.
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- Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
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The invention provides compounds of Formula I: 1where in W is 2These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful to treat diseases or conditions in which α7 is known to be involved.
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- Nucleophilic Displacements in Pyridine Rings
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The reactions of halopyridines containing an electron withdrawing group (-CN, -CO2R, -COMe, -NO2) with sulphur nucleophiles is reported.
- Dunn, A. D.,Norrie, R.
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