23-05-2013 дата публикации
Номер: US20130131044A1
Принадлежит:
The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. 2. The compound of wherein said non-interfering substituent is selected from one or more of the group consisting of alkyl claim 1 , cycloalkyl claim 1 , alkenyl claim 1 , cycloalkenyl claim 1 , alkynyl claim 1 , aryl claim 1 , heteroaryl claim 1 , arylalkyl claim 1 , heteroarylalkyl claim 1 , arylalkenyl claim 1 , heteroarylalkenyl claim 1 , arylalkynyl claim 1 , and heteroarylalkynyl claim 1 , each of which may be optionally substituted with one or more heteroatoms or additional non-interfering substituents.36-. (canceled)89-. (canceled)10. The compound of wherein the compound is selected from the following group:rac-(3aR,4R,5R,6R,7aS)-2-amino-6-(hydroxymethyl)-3a,4,5,6,7,7a-hexahydrobenzo[d]oxazole-4,5-diol;rac-(3aR,4R,5R,6R,7aS)-6-(hydroxymethyl)-2-(methylamino)-3a,4,5,6,7,7a-hexahydrobenzo[d]oxazole-4,5-diol;rac-(3aR,4R,5R,6R,7aS)-2-(ethylamino)-6-(hydroxymethyl)-3a,4,5,6,7,7a-hexahydrobenzo[d]oxazole-4,5-diol;rac-(3aR,4R,5R,6R,7aS)-6-(hydroxymethyl)-2-(propylamino)-3a,4,5,6,7,7a-hexahydrobenzo[d]oxazole-4,5-diol;rac-(3aR,4R,5R,6R,7aS)-2-(butylamino)-6-(hydroxymethyl)-3a,4,5,6,7,7a-hexahydrobenzo[d]oxazole-4,5-diol;rac-(3aR,4R,5R,6R,7aS)-2-(allylamino)-6-(hydroxymethyl)-3a,4,5,6,7,7a-hexahydrobenzo[d]oxazole-4,5-diol;rac-(3aR,4R,5R,6R,7aS)-6-(hydroxymethyl)-2-((4-methoxybenzyl)amino)-3a,4,5,6,7,7a-hexahydrobenzo[d]oxazole-4,5-diol;rac-(3aR,4R,5R,6R,7aS)-2-(dimethylamino)-6-(hydroxymethyl)-3a,4,5,6,7,7a-hexahydrobenzo[d]oxazole-4,5-diol;rac-(3aR,4R,5R,6R,7aS)-2-(ethyl(methyl)amino)-6-(hydroxymethyl)-3a,4,5,6,7,7a-hexahydrobenzo[d]oxazole-4,5-diol;(3aR,4R,5R,6R,7aS)-2-amino-6-(hydroxymethyl)-3a,4,5,6,7 ...
Подробнее