N[.omega.,(.omega.-1)-dialkyloxy]- and N-[.omega.,(.omega.-1)-dialkenyloxy]-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor
AssigneeSyntex (U.S.A.) Inc.
InventorsDeborah A. Eppstein, Philip L. Felgner, Thomas R. Gadek, Gordon H. Jones, Richard B. Roman
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Abstract
This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
Claims13
A method for introducing a polyanion into a cell, said method comprising:
- forming a liposome from a positively charged lipid of Formula I ##STR8## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms;
- R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, pyrrolidino, piperidino, or morpholino;
- n is 1 to 8;
- and x is a pharmaceutically acceptable anion;
- contacting the liposome with a polyanion to form a positively-charged polyanion-liposome complex;
- and
- incubating the complex with a cell.
A method for introducing a biologically active substance into a cell, said method comprising:
- forming a liposome comprising:
- a compound of Formula I:
- ##STR9## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms;
- R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, pyrrolidino, piperidino, or morpholino;
- n is 1 to 8;
- and X is a pharmaceutically acceptable anion;
- and
- a biologically active substance;
- and incubating the liposome with a cell culture.
Dependencies are inferred from the claim text.