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LYSOSOMOTROPIC ACID CERAMIDASE INHIBITORS
专利权人:
Фонд Медицинского Университета Южной Каролины по развитию научных исследований (US)
发明人:
БЕЛЯВСКА Алисия (US),БЭЙ Эйпинг (US),СЗАЛК Зджислав М. (US),ХЭННАН Юзеф А. (US),НОРРИС Джеймс (US),ЗАЙЭНГ Лью (US)
申请号:
RU2011117722/13
公开号:
RU2011117722A
申请日:
2009.11.06
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. The compound for the inhibition of acid ceramidase, where 5 the inhibition is free of constant lysosomal destabilization and / or proteolytic degradation of acid ceramidase, and where the compound has the structure of Formula (Ia) where n is an integer from 0 to 13; R is selected from the group consisting of NH, NHR, NRR, and an N-heterocyclic compound; R is selected from the group consisting of H and alkyl; R is selected from the group consisting of H, OH, NO, NH, and NHR; R is selected from the group consisting of H, CH, CHOH, and CHO-C (= O) —CH (R) NRR; R is selected from the group consisting of H, OH, = O, and OC (= O) CH (R) NRR; each R, R and R are independently selected from the group including H, alkyl, aralkyl, and aryl; R is C (= O) - (CH) R, where m is an integer from 5 to 10; R is H, alkyl, cycloalkyl, or a heterocyclic compound; X is selected from the group consisting of O, NH, and S; and Y is CH2 or NH; or a pharmaceutically acceptable salt thereof. 2. The compound according to claim 1, where X is O.3. The compound according to claim 1, where Y is CH2.4. The compound according to claim 1, where R is H.5. The compound of claim 1, wherein R is NO2.6. The compound according to claim 1, where R is CH2 OH. The compound according to claim 1, where R is OH. The compound according to claim 1, where n is 7.9. The compound according to claim 1, where R is NHR6, where R is alkyl. The compound according to claim 1, where R is NR6R7, where R and R are each alkyl. The compound according to claim 1, where R is an N-heterocyclic compound selected from the group consisting of ui. The compound according to claim 1, where the compound is selected from the group consisting of: (1R, 2R) -2- [N- (12 '- {1 "-imidazole} -dedecanoyl) amino] -1- (4" -nitrophenyl) -1,3-propanediol (LCL433); (1R, 2R) -2- [N- (12 '- {1 "-morpholine} -dedecanoyl) amino] -1- (4" -nitrophenyl) -1,3 propanediol (LCL449); (1R, 2R) -2- [N- (12'-amino-dodecanoyl) amino] -1- (4 "nitrophenyl) -1,3-prop
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