- β-GLUCOCEREBROSIDASE CHAPERONES
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The present application relates to compounds of the Formula (I): which are useful or the treatment of diseases in which the wild type or a mutant form of the enzyme β-glucocerebrosidase is implicated.
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- Rapid assembly of a library of lipophilic iminosugars via the thiol-ene reaction yields promising pharmacological chaperones for the treatment of Gaucher disease
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A highly divergent route to lipophilic iminosugars that utilizes the thiol-ene reaction was developed to enable the rapid synthesis of a collection of 16 dideoxyiminoxylitols bearing various different lipophilic substituents. Enzyme kinetic analyses revea
- Goddard-Borger, Ethan D.,Tropak, Michael B.,Yonekawa, Sayuri,Tysoe, Christina,Mahuran, Don J.,Withers, Stephen G.
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supporting information; experimental part
p. 2737 - 2745
(2012/06/01)
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- RECYCLIZATION REACTIONS. RECYCLIZATIONS OF 3-ACYLMETHYL-2,4-THIAZOLIDINEDIONES BY THE ACTION OF NUCLEOPHILES
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Four directions were established and investigated in the recyclization of 3-acylmethyl-2,4-thiazolidinediones with the participation of the side chain at the cyclic nitrogen atom and the formation of substituted 2-imidazolones or 2-oxazolones (under the influence of ammonia or hydroxides respectively), 2,5-diarylpyrazines (under the influence of methylamine), 6-monosubstituted or 2,6-disubstituted 4,5-dihydro-1,2,4-triazin-3-ones, and 5-substituted 1-amino-2-imidazolones (under the influence of hydrazine and phenylhydrazine).The directions of recyclization with hydrazines are determined by the stereochemical configuration of the intermediate hydrazones; the E-hydrazones of 3-acylmethyl-2,4-thiazolidenediones are converted into 4,5-dihydro-1,2,4-triazin-3-ones, while the Z izomers are converted into 1-amino-2-imidazolones.
- Shvaika, O. P.,Korotkikh, N. I.,Chervinskii, A. Yu.,Artemov, V. N.
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p. 1533 - 1543
(2007/10/02)
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