- TARGETED PEPTIDE CONJUGATES
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The present invention relates to the preparation and use of therapeutic compounds for the treatment of diseases at specific subcellular target areas such as specific cellular organelles. In particular, the therapeutic compounds of the invention are specific for modifying enzyme activity within targeted organelles or structures of cells and tissues. Subcellular organelles and structures that may be specifically targeted by compounds of the present invention include lysosomes, autophagasomes, the endoplasmic reticulum, the Golgi complex, peroxisomes, the nucleus, membranes and the mitochondria.
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Paragraph 0152; 0153
(2018/08/12)
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- An expeditious synthesis of iminosugars
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A short and expedient synthesis of the potent glycosidase inhibitors, 1-deoxynojirimycin, miglitol, miglustat, 1-deoxymannojirimycin, and 1-deoxygalactonojirimycin is presented.
- Gandy, Michael N.,Piggott, Matthew J.,Stubbs, Keith A.
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experimental part
p. 1409 - 1412
(2011/05/14)
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- The fluorination (at C5) of some derivatives of D-glucose
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The photobromination of various per-esters of β-D-glucopyranose and α- and β-D-glucopyranosyl fluoride has yielded 5-bromo derivatives capable of conversion into the corresponding 5-fluorides. The best reagent for this conversion was found to be silver te
- Skelton, Brian W.,Stick, Robert V.,Stubbs, Keith A.,Watts, Andrew G.,White, Allan H.
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p. 345 - 353
(2007/10/03)
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- FORMATION OF 6-DEOXY-6-IODOHEXOPYRANOSIDES AS SUBSTRATES FOR THE HEX-5-ENOSE DEGRADATION
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The synthesis of 6-deoxy-6-iodohexopyranosides as potential substrates for the hex-5-enose degradation has been examined for a range of mono-, di-, and poly-saccharide derivatives.It is shown that (1) unsubstituted D-glucopyranosides undergo selective, primary iodination without unwanted side-reactions; (2) primary iodination of D-galactopyranosides is accompanied by 3,6-anhydride formation, so that the desired reaction is only possible with protection of secondary hydroxyl groups; and (3) the extent of iodination in substrates of higher molecular weight is conveniently determined by reaction of acetylated (or methylated) derivatives with tributylstannane, followed by analysis of the resulting 6-deoxyhexopyranosides.The formation of 6-deoxy-6-iodohexopyranosyl residues in otherwise methylated plant galactomannans proceeds satisfactorily for (terminal) α-D-galactopyranosyl groups but incompletely for unbranched β-D-mannopyranosyl residues.
- Aspinall, Gerald O.,Carpenter, Roshan C.,Khondo, Lev
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p. 281 - 298
(2007/10/02)
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