- 3-SUBSTITUED IMIDAZO (4, 5-B) PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
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Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for e
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Page/Page column 70-71
(2011/10/10)
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- MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
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The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator ("CFTR"), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR (Formula I) or pharmaceutically acceptable salts thereof, wherein: ring A is selected from: (a), (b), (c), (d), wherein: R1 is -CH3 -CF3 or -CN; R2 is hydrogen, -CH3, -CF3, -OH, or -CH2OH; R3 is hydrogen, -CH3, -OCH3, or -CN; provided that both R2 and R3 are not simultaneously hydrogen; and one of X and Y is nitrogen and the other is carbon.
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Page/Page column 49-50
(2010/05/13)
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- Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs)
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A variety of basic, heterocyclic templates has been reported as potassium-competitive, acid pump antagonists. Herein, we report a comparison of potencies of these templates and others to establish which offers the best start point for further systematic o
- Panchal, Terry,Bailey, Nick,Bamford, Mark,Demont, Emmanuel,Elliott, Richard,Farre-Gutierrez, Irene,Garton, Neil,Hayhow, Thomas,Hutley, Gail,Naylor, Antoinette
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scheme or table
p. 6813 - 6817
(2010/06/16)
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- PYRROLOY2,3-c¨PYRIDINE COMPOUND, PROCESS FOR PRODUCING THE SAME, AND USE
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Provision of a compound having a superior proton pump action, which shows an antiulcer activity and the like after conversion to an in vivo proton pump inhibitor, a production method thereof and use thereof. A pyrrolo[2,3-c]pyridine compound represented by the formula: wherein each symbol is as defined in the specification.
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Page/Page column 36-37
(2010/11/27)
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- KINASE INHIBITORS
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The present invention provides kinase inhibitors of Formula I.
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Page/Page column 28
(2010/02/13)
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- Design, Synthesis, and Crystal Structure of Selective 2-Pyridone Tissue Factor VIIa Inhibitors
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Targeted 2-pyridones were selected as tissue Factor VIIa inhibitors and prepared from 2,6-dibromopyridine via a multistep synthesis. A variety of chemical transformations, including regioselective nucleophilic addition, selective nitrogen alkylation, and
- Parlow, John J.,Kurumbail, Ravi G.,Stegeman, Roderick A.,Stevens, Anna M.,Stallings, William C.,South, Michael S.
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p. 4696 - 4701
(2007/10/03)
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- Aprotic Nitration (NO2+BF4-) of 2-Halo- and 2,6-Dihalopyridines and Transfer-Nitration Chemistry of Their N-Nitropyridinium Cations
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NO2+BF4- nitration of 2,6-dibromo-1 and 2,6-dichloropyridine 2 in CH3CN results in predominant C-nitration, whereas in CH2Cl2, N-nitration is predominant.With 2,6-difluoropyridine 3 only C-nitration was observed.Dehalogenation of the C-nitrated 1 and 2 affords 3-nitropyridine (3-NP) in moderate but greatly improved yields over conventional protic nitration of pyridine.Despite favorable presence of steric inhibition to resonance and the I-effect of halogens, N-nitrated pyridinium salts 1b and 2b do not transfer-nitrate to aromatics even under forcing conditions.The lack of transfer-nitration reactivity is not due to in situ rearrangement of the nitro onium to nitrito oniums ions.A mechanism involving neighboring group participation by the 2,6-halogens is proposed.The monohalo-N-nitropyridinium cations transfer-nitrate toluene and benzene.Transfer nitration selectivity of the 2-bromo-N-nitro- and 2-chloro-N-nitropyridinium cations are comparable (KT/KB = 41-44), but the 2-fluoro-N-nitro cation is much less selective (more reactive) (KT/KB = 15.4), indicative of a stronger -I effect, weakening the N+-N+ bond.
- Duffy, Joseph L.,Laali, Kenneth Khosrow
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p. 3006 - 3009
(2007/10/02)
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- Continuous process for the production of polybromopyridine compounds
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A continuous process for producing a polybromopyridine compound comprises admixing a polychloropyridine compound with an anhydrous water soluble solvent in a first reaction zone to form a solution of the polychloropyridine compound. Hydrogen bromide gas is introduced into the solution while maintaining the temperature in the range of from about 70° to about 140° C. to produce a solution of the polybromopyridine compound. The solution is cooled to a temperature in the range of from about 5° to about 35° C. to precipitate the polybromopyridine compound from the anhydrous solvent. The polybromopyridine compound is separated from the anhydrous solvent and the anhydrous solvent is returned to the first reaction zone. Polybromopyridine compounds of increased purity are produced in a process having reduced material, energy and operating costs. The process does not require the use of water or other co-solvents nor the distillation of the reaction product mixture.
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