29-05-2014 дата публикации
Номер: US20140148600A1
Принадлежит:
The present invention relates to thiazole compounds of formula I, the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses for treatments against tumor and multiple sclerosis as inhibitors of histone deacetylase. 2. The compound according to claim 1 , wherein claim 1 ,In the general formula I:{'sub': 2', '1', '6', '3', '6', '1', '6', '6', '10', '2', '8', '6', '10', '6', '10, 'Ris hydrogen, C-Calkyl, C-Ccycloalkyl, C-Calkyl optionally substituted by hydroxyl, benzyloxyl or C-Caryl, C-Calkenyl, C-Caryl, or C-Caryl optionally substituted by halogen or nitro;'}n is 0;X is —NH—;{'sub': 1', '10', '6', '10', '1', '6', '6', '10', '6', '10', '2', '6, 'Y is —(C-Calkyl)-, —(C-Caryl)-, —(C-Calkyl)-(C-Caryl)- or —(C-Caryl)-(C-Calkenyl)-;'}{'sub': '8', 'Ris hydrogen.'}5. The compound according to claim 4 , wherein in general formula IV:{'sub': 2', '1', '6', '3', '6', '1', '6', '3', '6', '1', '6', '2', '8', '2', '8', '6', '10', '1', '6', '6', '10', '2', '8', '6', '10', '2', '8', '6', '10', '6', '10', '6', '10, 'Ris hydrogen, C-Calkyl, C-Ccycloalkyl, C-Calkyl optionally substituted by hydroxyl, C-Ccycloalkyl optionally substituted by C-Calkyl, C-Calkenyl, C-Calkenyl optionally substituted by hydroxyl, C-Caryl, C-Calkyl optionally substituted by C-Caryl or benzyloxyl, C-Calkenyl optionally substituted by C-Caryl, C-Calkoxyl optional substituted by C-Caryl, C-Caryl optionally substituted by halogen, or C-Caryl optionally substituted by nitro;'}{'sub': 4b', '5b', '1', '6', '1', '6', '1', '6', '3', '6', '2', '6', '2', '6', '2', '6', '6', '10, 'Rand Reach independently are hydrogen, fluoro, C-Calkyl, C-Calkyl optionally substituted by hydroxyl, C-Calkyl optionally substituted by fluoro, C-Ccycloalkyl, C-Calkenyl, C-Calkenyl optionally substituted by hydroxyl, C-Calkenyl optionally substituted by fluoro, or C-Caryl; or,'}{'sub': 4b', '5b, 'Rand Rtogether ...
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