18-09-2014 дата публикации
Номер: US20140275022A1
Принадлежит:
The invention provides compounds 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:{'sup': 1', '3, 'Rand Rare H;'}{'sup': 2', '4, 'Rand Rare OH; and'}{'sup': 6', '6, 'sub': 3', '2', '3', '2', '2', '3', '2', '2', '2', '3', '2, 'each Ris independently selected from the group consisting of: H, CH, CHCH, (CH)CH, CHCH═CH, CHC≡CH, and OCH, or NRis azetidin-1-yl or pyrrolidin-1-yl;'}3. The compound of wherein:{'sup': 1', '3, 'Rand Rare OH;'}{'sup': 2', '4, 'Rand Rare H; and'}{'sup': 6', '6, 'sub': 3', '2', '3', '2', '2', '3', '2', '2', '2', '3', '2, 'each Ris independently selected from the group consisting of: H, CH, CHCH, (CH)CH, CHCH═CH, CHC≡CH, and OCH, or NRis azetidin-1-yl or pyrrolidin-1-yl;'}4. The compound of wherein:{'sup': 2', '3, 'Rand Rare OH;'}{'sup': 1', '4, 'Rand Rare H; and'}{'sup': 6', '6, 'sub': 3', '2', '3', '2', '2', '3', '2', '2', '2', '3', '2, 'each Ris independently selected from the group consisting of: H, CH, CHCH, (CH)CH, CHCH═CH, CHC≡CH, and OCH, or NRis azetidin-1-yl or pyrrolidin-1-yl;'}5. (canceled)6. The compound of wherein the compound is selected from the following group:(3aR,5R,6R,7R,7aR)-5-(hydroxymethyl)-2-(methylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol;(3aR,5R,6R,7R,7aR)-2-(dimethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol;(3aR,5R,6S,7S,7aR)-2-(ethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol;(3aR,5R,6R,7S,7aR)-5-(hydroxymethyl)-2-(methylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol;(3aR,5R,6R,7R,7aR)-2-(ethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol;(3aR,5R,6R,7R,7aR)-5-(hydroxymethyl)-2-( ...
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