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
Life of this patent
Estimating the term…
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.
Claims8
A double coated liposome complex, comprising:
- a polyanion;
- a 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;
- and
- a negatively charged co-lipid.
A method for making a double coated liposome complex, comprising the steps of:
- forming a liposome from a positively charged lipid 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
- contacting the liposome with a polyanion to obtain a polyanion-lipid complex;
- and
- contacting the polyanion-lipid complex with an excess of a negatively charged lipid.
Dependencies are inferred from the claim text.