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Pharmaceutical dopamine glycoconjugate compositions and methods of their preparation and use
专利权人:
Samuel T. Christian
发明人:
Samuel T. Christian
申请号:
US11965444
公开号:
US08252752B2
申请日:
2007.12.27
申请国别(地区):
US
年份:
2012
代理人:
摘要:
Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds according to FORMULA V and methods of their use,wherein, Ring 1 comprises an aryl or heteroaryl ring having 4 to 8 carbon atoms, among which atoms are counted “X” and “Y” each of X and Y is optional X, when present is either —C(R1)2— or —C(R)2— Y, when present, is either —CH2— or —CH2—CH2— z, R5 and R5′ are optional, and when present z, R5 and R5′ together form a lower alkyl or a substituted lower alkyl moiety N is part of either an amine or an amide linkage E is a saccharide which forms a linkage with N through a single bond from a carbon or oxygen atom thereof R1 and R4 are selected form the group consisting of hydrogen, hydroxyl, halogen, halo-lower alkyl, alkoxyl, alkoxyl-lower alkyl, halo-alkoxy, thioamido, amidosulfonyl, alkoxylcarbonyl, carboxamide, aminocarbonyl, and alkylamino-carbonyl R2 and R3 are hydroxyl R5 and R6, when present, are selected from the group consisting of hydrogen, hydroxyl, alkoxyl, carbonyl, alkoxylcarbonyl, aminocarbonyl, alkylamino-carbonyl and dialkylamino-carbonyl and, R6 and R6′ are selected from the group consisting of hydrogen, hydroxyl, alkoxyl, carboxyl, alkoxylcarbonyl, aminocarbonyl, alkylamino-carbonyl and dialylamino-carbonyl, with the proviso that Ring 1 is capable of binding to any of: a dopaminergic receptor selected from the group consisting of a D1 receptor and a D5 receptor a DAT transporter a VMAT transporter and, with the proviso that E is capable of binding to a GLUT transporter selected from the group consisting of a GLUT1 receptor and a GLUT3 receptor.
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