US4946787A
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N-(ω,(ω-1)-dialkyloxy)- and N-(ω,(ω-1)-dialkenyloxy)-alk-1-yl-N,N,N-tetrasubstituted ammonium lipids and uses therefor
Assignee: Syntex USA LLC
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Filing: 1989-10-27
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Granted: 1990-08-07
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Expires: 2009-10-27
Abstract
Abstract This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R 1 and R 2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R 3 , R 4 and R 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 3 , R 4 , and R 5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino; n is 1 to 8; and X is a pharmaceutically acceptable anion.
Inventors
- 👤 Deborah A. Eppstein
- 👤 Philip L. Felgner
- 👤 Thomas R. Gadek
- 👤 Gordon H. Jones
- 👤 Richard B. Roman
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 02:22
CPC Classifications
C; C12; C12N; C12N15/00; C12N15/09; C12N15/87; C12N15/88; A; A61; A61K; A61K47/00; A61K47/06; A61K47/16; A61K47/18; A61K47/186; A61K9/00; A61K9/0012; A61K9/0014; A61K9/0019; A61K9/10; A61K9/127; A61K9/1271; A61K9/1272; C07; C07D; C07D453/00; C07D453/02
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
115 words
A double coated liposome complex, comprising: a polyanion; a lipid of Formula I ##STR8## or an optical isomer thereof wherein R 1 and R 2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R 3 , R 4 and R 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 3 , R 4 , and R 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.
Claim 2
Dependent Claim
115 words
A double coated liposome complex, comprising: a polyanion; a lipid of Formula I ##STR8## or an optical isomer thereof wherein R 1 and R 2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R 3 , R 4 and R 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 3 , R 4 , and R 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.
Claim 3
Independent Claim
146 words
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 1 and R 2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R 3 , R 4 and R 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 3 , R 4 , and R 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.
Claim 4
Independent Claim
146 words
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 1 and R 2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R 3 , R 4 and R 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 3 , R 4 , and R 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.
Claim 5
Dependent Claim
50 words
The double coated liposome complex of claim 1 wherein R 1 and R 2 are the same and are alkyl of 10 to 20 carbon atoms, R 3 , R 4 , and R 5 are methyl or ethyl, n is 1 to 4, and X is a halide ion.
Claim 6
Dependent Claim
12 words
The double coated liposome complex of claim 2 wherein n is 1.
Claim 7
Dependent Claim
23 words
The double coated liposome complex of claim 4 wherein the lipid of Formula I is (±) N-(2,3-di-(9-(Z)-octadecenyloxy))-prop-1-yl-N,N,N-trimethylammonium chloride or an optical isomer thereof.
Claim 8
Dependent Claim
54 words
The method for making a double coated liposome complex of claim 2 wherein R 1 and R 2 are the same and are alkyl of 10 to 20 carbon atoms, R 3 , R 4 , and R 5 are methyl or ethyl, n is 1 to 4, and X is a halide ion.
Claim 9
Dependent Claim
16 words
The method for making a double coated liposome complex of claim 6 wherein n is 1.
Claim 10
Dependent Claim
27 words
The method for making a double coated liposome complex of claim 7 wherein the lipid of Formula I is (±) N-(2,3-di-(9-(Z)-octa-decenyloxy))-prop-1-yl-N,N,N-trimethylammonium chloride or an optical isomer thereof.
References Cited (Backward Citations)
No citation records indexed.
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