Title:
COMPOUNDS FOR TARGETING DRUG DELIVERY AND ENHANCING SIRNA ACTIVITY
Document Type and Number:
WIPO Patent Application WO/2012/170952
Kind Code:
A4
Abstract:
Here described are compounds of formula I: wherein R1 and R2 is independently selected from a group consisting of C10 to C18 alkyl, C12 to C18 alkenyl, and oleyl group; wherein R3 and R4 are independently selected from a group consisting of C1 to C6 alkyl, and C2 to C6 alkanol; wherein X is selected from a group consisting of -CH2-, -S-, and -O- or absent; wherein Y is selected from -(CH2)n, -S(CH2)n, -O(CH2)n-, thiophene, -SO2(CH2)n-, and ester, wherein n = 1 -4; wherein a = 1 -4; wherein b=l -4; wherein c=l-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.
Inventors:
NIITSU YOSHIRO (JP)
PAYNE JOSEPH E (US)
HOU ZHENG (US)
GAUDETTE JOHN A (US)
NAGARAJAN SRIDHAR C (US)
KNOPOV VICTOR (US)
WITTE RICHARD P (US)
AHMADIAN MOHAMMAD (US)
PERELMAN LOREN A (US)
TANAKA YASUNOBU (JP)
AKOPIAN VIOLETTA (US)
KARMALI PRIYA (US)
PAYNE JOSEPH E (US)
HOU ZHENG (US)
GAUDETTE JOHN A (US)
NAGARAJAN SRIDHAR C (US)
KNOPOV VICTOR (US)
WITTE RICHARD P (US)
AHMADIAN MOHAMMAD (US)
PERELMAN LOREN A (US)
TANAKA YASUNOBU (JP)
AKOPIAN VIOLETTA (US)
KARMALI PRIYA (US)
Application Number:
PCT/US2012/041753
Publication Date:
May 30, 2013
Filing Date:
June 08, 2012
Export Citation:
Assignee:
NITTO DENKO CORP (JP)
NIITSU YOSHIRO (JP)
PAYNE JOSEPH E (US)
HOU ZHENG (US)
GAUDETTE JOHN A (US)
NAGARAJAN SRIDHAR C (US)
KNOPOV VICTOR (US)
WITTE RICHARD P (US)
AHMADIAN MOHAMMAD (US)
PERELMAN LOREN A (US)
TANAKA YASUNOBU (JP)
AKOPIAN VIOLETTA (US)
KARMALI PRIYA (US)
NIITSU YOSHIRO (JP)
PAYNE JOSEPH E (US)
HOU ZHENG (US)
GAUDETTE JOHN A (US)
NAGARAJAN SRIDHAR C (US)
KNOPOV VICTOR (US)
WITTE RICHARD P (US)
AHMADIAN MOHAMMAD (US)
PERELMAN LOREN A (US)
TANAKA YASUNOBU (JP)
AKOPIAN VIOLETTA (US)
KARMALI PRIYA (US)
International Classes:
C07C237/08; A61K31/16; A61P1/16; C07C237/22; C07C323/60; C07C333/04
Attorney, Agent or Firm:
KNUDSEN, Peter, J. (2929 Arch StreetCira Centre, 12th Floo, Philadelphia PA, US)
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