- Amine, 1, 2-and 1, 3-diol, and its use for curing Alzheimer's disease
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Disclosed are compounds of formula: and pharmaceutically acceptable salts and esters thereof, useful in treating and/or preventing Alzheimer's disease and other similar diseases, wherein RN, RC, R1, n and R20 are defined herein. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
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Page/Page column 217
(2008/06/13)
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- Synthesis and characterization of nucleosides and oligonucleotides bearing adducts of butadiene epoxides on adenine N6 and guanine N2
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Butadiene is a major industrial chemical whose genotoxic effects are attributed to the reaction of its oxidized metabolites, butadiene monoepoxide (BDO) and butadiene diepoxide (BDO2), with DNA. Nucleosides and oligonucleotides containing regio- and stereochemically specific adducts of BDO and the BDO2-related compound, butene 3,4-diol 1,2-epoxide (BDE), on guanine [(2R)- and (2S)-N2-(1-hydroxy-3-buten-2-yl) and (2R,3R)- and (2S,3S)-N2-(2,3,4-trihydroxybut-1-yl), respectively] and on adenine [(2R)- and (2S)-N6-(1-hydroxy-3-buten-2-yl) and (2R,3R)- and (2S,3S)-N6-(2,3,4-trihydroxybut-1-yl), respectively] have been prepared by nonbiomimetic routes. For guanine adducts, 2-fluoro-O6-(trimethylsilylethyl)-2′-deoxyinosine was treated with (2R)- and (2S)-2-amino-3-buten-1-ol to give the BDO adducts and with (2R,3R)- and (2S,3S)-1-amino-2,3,4-butanetriol to produce the BDE adducts; the adducted oligonucleotides were prepared from 11-mer oligonucleotides containing the halopurine. Adenine adducts were prepared in a similar fashion using 6-chloropurine 2′-deoxyriboside as the reactive purine component.
- Nechev, Lubomir V.,Zhang, Mingzhu,Tsarouhtsis, Dimitrios,Tamura, Pamela J.,Wilkinson, Amanda S.,Harris, Constance M.,Harris, Thomas M.
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p. 379 - 388
(2007/10/03)
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- 2-Amino-1-(1,2-dioxolan-4-yl)ethanol compounds, their preparation and use
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2-Amino-1-(1,3-dioxolan-4-yl)ethanol compounds of formula (I) STR1 wherein R1 and R2 are identical or different and can be hydrogen or a lower alkyl group of 1-4 carbon atoms; or when R2 is an alkyl group of 1-4 carbon atoms, R1 can also be an alkoxy group of 1-4 carbon atoms; or R1 and R2 combined form an alkylene residue of 5 or 6 carbon atoms, are especially suited as intermediates in the production of opacifying compounds useful in X-ray contrast media.
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