US 7,601,367 B2
Compositions and processes using siRNA, amphipathic compounds and polycations
Sean D. Monahan, Madison, Wis. (US); David L. Lewis, Madison, Wis. (US); Hans Herweijer, Madison, Wis. (US); Jon A. Wolff, Madison, Wis. (US); James E. Hagstrom, Middleton, Wis. (US); Aaron G. Loomis, Prairie du Sac, Wis. (US); Vladimir Trubetskoy, Middleton, Wis. (US); and Lori Higgs, Madison, Wis. (US)
Assigned to Mirus Bio LLC, Madison, Wis. (US)
Filed on May 14, 2004, as Appl. No. 10/845,968.
Application 10/845968 is a continuation in part of application No. 10/345021, filed on Jan. 15, 2003, abandoned.
Application 10/345021 is a continuation in part of application No. 10/186757, filed on Jul. 01, 2002, abandoned.
Application 10/186757 is a continuation in part of application No. 10/157674, filed on May 28, 2002, granted, now 7,101,995.
Prior Publication US 2005/0143332 A1, Jun. 30, 2005
Int. Cl. A61K 9/127 (2006.01); C07H 21/04 (2006.01); C12N 15/88 (2006.01)
U.S. Cl. 424—450  [536/24.5; 435/458] 6 Claims
 
1. A composition for delivery of siRNA to a mammalian cell comprising: said siRNA, a first amphipathic compound that is a cationic lipid, a second amphipathic compound that is a cationic lipid and a polycation, wherein the polycation is not a DNA-binding protein and is selected from the group consisting of: polyvinylamine, polyallylamine, polyethylenimine and ethoxylated polyethylenimine wherein said second amphipathic compound consists of an amphipathic compound having the structure:

OG Complex Work Unit Drawing
wherein R1 and R2 are selected from the group consisting of a C6 to C24 alkane, C6-C24 alkene, mono-substituted alkyl silane, di-substituted alkyl silane, tri-substituted alkyl silane, cycloalkyl, sterol, steroid, substituted lipid, acyl segment of a fatty acid, hydrophobic hormone, and hydrophobic hormone analog.