EP0118316A2
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Synthetic phospholipid compounds, their preparation and use
Assignee: Lipid Specialties Inc
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Filing: 1984-03-07
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Granted: —
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Expires: 2004-03-07
Abstract
Abstract Synthetic phospholipid compounds which are phosphatidylethanolamine polycarboxyl polyalkylene glycols are prepared by the reaction of a phosphatidylethanolamine, a polycarboxylic acid compound, such as succinic or glutaryl anhydride, and a polyalkylene glycol, such as polyethylene glycol.
Inventors
- 👤 Barry D. Sears
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 20:07
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127; A61K47/00; A61K47/06; A61K47/24; A61K9/0012; A61K9/0019; A61K9/1271; C; C07; C07F; C07F9/00; C07F9/02; C07F9/06; C07F9/08; C07F9/09; C07F9/10; C08; C08G; C08G65/00; C08G65/02; C08G65/32; C08G65/329; C08G65/335; C08G65/3356
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
79 words
A synthetic phospholipid compound having the structural formula: wherein R l and R 2 each represent hydrogen or an organic acyl radical; R 3 represents a C2 or C 3 alkylene radical; X represents hydrogen or an alkyl radical; R 4 represents a C2 to C 10 alkylene radical; R 5 represents an organic linking radical; R 6 represents hydrogen or a C 1 to C 4 alkyl radical; and n represents a number of from 0 to 200.
Claim 2
Dependent Claim
79 words
A synthetic phospholipid compound having the structural formula: wherein R l and R 2 each represent hydrogen or an organic acyl radical; R 3 represents a C2 or C 3 alkylene radical; X represents hydrogen or an alkyl radical; R 4 represents a C2 to C 10 alkylene radical; R 5 represents an organic linking radical; R 6 represents hydrogen or a C 1 to C 4 alkyl radical; and n represents a number of from 0 to 200.
Claim 3
Dependent Claim
23 words
A phospholipid compound according to claim 1 wherein R 1 and R 2 each represent a C 2 to C 20 fatty-acid radical.
Claim 4
Dependent Claim
19 words
A phospholipid compound according to claim 1 wherein R 1 and R 2 are organic radicals derived from soybeans.
Claim 5
Dependent Claim
17 words
A phospholipid compound according to claim 1, 2 or 3 wherein R 5 represents a polymethylene radical.
Claim 6
Dependent Claim
19 words
A phospholipid compound according to claim 4 wherein R 5 represents a C 1 to C 4 methylene radical.
Claim 7
Dependent Claim
20 words
A phospholipid compound according to any one of the preceding claims wherein n represents a number from 2 to 20.
Claim 8
Dependent Claim
19 words
A synthetic phospholipid compound according to claim 1 which is a soy phosphatidylethanolamine succinyl or glutaryl polyethylene glycol compound.
Claim 9
Dependent Claim
52 words
A synthetic phospholipid compound having the structural formula: wherein R 1 and R 2 each represent a C 2 to C 20 hydrocarbon organic acyl radical; X represents hydrogen or a methyl radical; m represents a number of from 1 to 4; and n represents a number of from 0 to 200.
Claim 10
Dependent Claim
52 words
A synthetic phospholipid compound having the structural formula: wherein R 1 and R 2 each represent a C 2 to C 20 hydrocarbon organic acyl radical; X represents hydrogen or a methyl radical; m represents a number of from 1 to 4; and n represents a number of from 0 to 200.
Claim 11
Independent Claim
26 words
A method of preparing a phosphatidylalkanolamine polycarboxyl polyalkylene glycol compound, which method comprises reacting a phosphatidylalkanolamine, a polycarboxylic acid or derivative thereof and a polyalkylene glycol.
Claim 12
Independent Claim
26 words
A method of preparing a phosphatidylalkanolamine polycarboxyl polyalkylene glycol compound, which method comprises reacting a phosphatidylalkanolamine, a polycarboxylic acid or derivative thereof and a polyalkylene glycol.
Claim 13
Dependent Claim
53 words
A method according to claim 9 which comprises reacting a dicarboxylic acid anhydride with a poly C 2 or C 3 alkylene glycol, to form the carboxyl poly C 2 or C 3 alkylene glycol compound and thereafter reacting the carboxyl poly C 2 or C 3 alkylene glycol compound with a phosphatidylethanolamine.
Claim 14
Dependent Claim
24 words
A method according to claim 9 or 10 wherein the polyalkylene glycol is polyethylene glycol having a molecular weight of from 150 to 3000.
Claim 15
Dependent Claim
24 words
A method according to claim 9, 10 or 11 wherein the polycarboxylic acid derivative is a C 2 to C 7 dicarboxylic acid anhydride.
Claim 16
Independent Claim
17 words
A method according to any one of claims 9 to 12 wherein the phosphatidylalkanolamine is phosphatidylethanolamine. .
Claim 17
Dependent Claim
15 words
A method according to claim 13 wherein the phosphatidylethanolamine is derived from crude soy lecithin.
Claim 18
Independent Claim
23 words
A method according to any one of claims 9 to 14 which includes recovering the phosphatidylalkanolamine polycarboxyl polyalkylene glycol by extracting with acetone.
Claim 19
Dependent Claim
41 words
A method according to claim 9 which comprises reacting a dicarboxylic acid anhydride with a phosphatidylethanolamine, to form the phosphatidylethanolamine carboxylic acid compound and thereafter reacting the phosphatidylethanolamine carboxylic acid compound with a poly C 2 or C 3 alkylene glycol.
Claim 20
Independent Claim
24 words
A method according to any one of claims 9 to 16 wherein the dicarboxylic acid derivative is succinyl acid anhydride or glutaric acid anhydride.
Claim 21
Independent Claim
39 words
A method of solubilizing, in an aqueous environment, a water-insoluble compound, which method comprises mixing a solubilizing amount of a hydrated phospholipid compound as claimed in any one of claims 1 to 8 with water and a water-insoluble compound.
Claim 22
Dependent Claim
27 words
An aqueous composition which comprises water, a micelle-forming amount of a synthetic phospholipid as claimed in any one of claims 1 to 8 and a water-insoluble compound.
Claim 23
Dependent Claim
21 words
An aqueous composition according to claim 19, which solution has micelles therein of less than 20 nm (200 Angstroms) in size.
Claim 24
Dependent Claim
24 words
An aqueous composition according to claim 19 or 20 which comprises a therapeutic drug, petroleum jelly or a fragrance oil as the water-insoluble compound.
References Cited (Backward Citations)
No citation records indexed.
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