发明名称 |
COMPOUNDS FOR TARGETING DRUG DELIVERY AND ENHANCING SIRNA ACTIVITY |
摘要 |
Here described are compounds of formula I:
wherein R 1 and R 2 is independently selected from a group consisting of C 10 to C 18 alkyl, C 12 to C 18 alkenyl, and oleyl group; wherein R 3 and R 4 are independently selected from a group consisting of C 1 to C 6 alkyl, and C 2 to C 6 alkanol; wherein X is selected from a group consisting of -CH 2 -, -S-, and -O- or absent; wherein Y is selected from -(CH 2 ) n , -S(CH 2 ) n , - O(CH 2 ) n -, thiophene, -SO 2 (CH 2 ) n -, and ester, wherein n = 1-4; wherein a = 1-4; wherein b=1-4; wherein c=1-4; and wherein Z is a counterion; and compounds consisting of the structure
(targeting molecule) m -linker-(targeting molecule) n ,
wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including one or both of these compounds which are useful for the delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations. |
申请公布号 |
EP2718261(B1) |
申请公布日期 |
2016.02.24 |
申请号 |
EP20120728010 |
申请日期 |
2012.06.08 |
申请人 |
NITTO DENKO CORPORATION |
发明人 |
SRIDHAR, C. NAGARAJAN;KARMALI, PRIYA;NIITSU, YOSHIRO;PAYNE, JOSEPH E.;HOU, ZHENG;GAUDETTE, JOHN A.;KNOPOV, VICTOR;WITTE, RICHARD P.;AHMADIAN, MOHAMMAD;PERELMAN, LOREN A.;TANAKA, YASUNOBU;AKOPIAN, VIOLETTA |
分类号 |
C07C237/08;A61K9/127;A61K31/16;A61P1/16;C07C237/22;C07C323/60;C07C333/04 |
主分类号 |
C07C237/08 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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