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US4003990A Expired / Lapsed US ⏱️ 0.0 years remaining

Anti-inflammatory polymers, pharmaceutical compositions containing the same and process for producing said polymers

Assignee: L'Oréal SA
•
Filing: 1975-11-07
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Granted: 1977-01-18
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Expires: 1995-11-07
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Abstract

Abstract A polymer has on its macromolecular chains in the form of a lateral branching an anti-inflammator residue having a carboxylic acid function chemically linked to the macromolecular chains by an intermediate covalent function.

Inventors

  • 👤 Bernard Jacquet
  • 👤 Christos Papantoniou
  • 👤 Pierre Dufaure
  • 👤 Claude Mahieux

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-06 03:56
CPC Classifications
A; A61; A61K; A61K8/00; A61K8/18; A61K8/72; A61K8/81; A61K8/8141; A61K8/8147; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61Q; A61Q19/00; C; C07; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/26; C07D209/28; C07D277/00; C07D277/02; C07D277/20; C07D277/22; C07D277/30; C08; C08F; C08F8/00; A61K2800/00; A61K2800/40; A61K2800/57

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 207 words
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and at least one anti-inflammatory polymer containing repeating units of the formula ##STR37##wherein R 1 and R 2 are selected from the group of values consisting of a. R 2 is --O--CO--CH-- 2 -- n O--Z, R 1 is hydrogen and n is 1-10, b. R 2 is --CH 2 --O--CO--CH 2 --o--Z and R 1 is hydrogen or methyl, c. R 2 is --CH 2 --NH--CO--CH 2 O--Z and R 1 is hydrogen, d. R 2 is --CO--NH--CH 2 --NH--CO--CH 2 --O--Z and R 1 is hydrogen, and ##STR38##wherein r and r' represent alkyl having 1-3 carbon atoms, Y represents chlorine or bromine, and R 1 is hydrogen or methyl, and Z is the acyl residue of an anti-inflammatory carboxylic pharmaceutical agent selected from the group consisting of ##STR39## wherein X 1 represents Cl, Br, F or I and said alkyl has 1-3 carbon atoms, ##STR40## wherein Z 1 is selected from the group consisting of hydrogen and methyl, and X 2 is selected from the group consisting of hydrogen and methoxy, ##STR41##said anti-inflammatory polymer being present in a sufficient amount effective to produce a delayed and prolonged action of the residue of said anti-inflammatory carboxylic pharmaceutical agent.
Claim 2
Dependent Claim 207 words
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and at least one anti-inflammatory polymer containing repeating units of the formula ##STR37##wherein R 1 and R 2 are selected from the group of values consisting of a. R 2 is --O--CO--CH-- 2 -- n O--Z, R 1 is hydrogen and n is 1-10, b. R 2 is --CH 2 --O--CO--CH 2 --o--Z and R 1 is hydrogen or methyl, c. R 2 is --CH 2 --NH--CO--CH 2 O--Z and R 1 is hydrogen, d. R 2 is --CO--NH--CH 2 --NH--CO--CH 2 --O--Z and R 1 is hydrogen, and ##STR38##wherein r and r' represent alkyl having 1-3 carbon atoms, Y represents chlorine or bromine, and R 1 is hydrogen or methyl, and Z is the acyl residue of an anti-inflammatory carboxylic pharmaceutical agent selected from the group consisting of ##STR39## wherein X 1 represents Cl, Br, F or I and said alkyl has 1-3 carbon atoms, ##STR40## wherein Z 1 is selected from the group consisting of hydrogen and methyl, and X 2 is selected from the group consisting of hydrogen and methoxy, ##STR41##said anti-inflammatory polymer being present in a sufficient amount effective to produce a delayed and prolonged action of the residue of said anti-inflammatory carboxylic pharmaceutical agent.
Claim 3
Dependent Claim 19 words
The pharmaceutical composition of claim 1 wherein said polymer has an average molecular weight between about 2,000 and 1,000,000.
Claim 4
Dependent Claim 94 words
The pharmaceutical composition of claim 1 which is a copolymer further containing repeating units of the formula ##STR42##wherein R' 7 represents hydrogen or methyl and R 1 represents a member selected from the group consisting of (a) --O--CO--R 3 wherein R 3 represents a saturated hydrocarbon chain having 8-18 carbon atoms, (b) --CO--O--R 4 wherein R 4 represents a saturated hydrocarbon chain having 8-18 carbon atoms or n,n'-dialkylaminoethyl wherein said alkyl moieties have 1-3 carbon atoms, (c) --CH 2 --O--CO--R 5 wherein R 5 is a saturated hydrocarbon having 2-18 carbon atoms and ##STR43##
Claim 5
Dependent Claim 28 words
The pharmaceutical composition of claim 1 wherein said anti-inflammatory polymer is present in an amount between 0.1-10 percent by weight based on the total weight of said composition.
Claim 6
Dependent Claim 25 words
A dosage unit of the pharmaceutical composition of claim 1 in an amount sufficient to provide 100 mg to 5 g of said anti-inflammatory polymer.
Claim 7
Dependent Claim 164 words
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and at least one anti-inflammatory polymer containing repeating units of the formula ##STR44##wherein R 1 and R 2 are selected from the group of values consisting of a. R 2 is --O--CO--CH 2 -- n O--Z, R 1 is hydrogen and n is 1-10, b. R 2 is --CH 2 --O--CO--CH 2 --O--Z and R 1 is hydrogen or methyl, c. R 2 is --CH 2 --NH--CO--CH 2 --0--Z and R 1 is hydrogen, d. R 2 is --CO--NH--CH 2 --NH--CO--CH 2 --0--Z and R 1 is hydrogen, and ##STR45## wherein r and r' represent alkyl having 1-3 carbon atoms, Y represents chlorine or bromine, and R 1 is hydrogen or methyl, and Z is the acyl residue of an anti-inflammatory pharmaceutical agent whose molecule comprises a carboxylic acid function, said anti-inflammatory polymer being present in a sufficient amount effective to produce a delayed and prolonged action of the residue of said anti-inflammatory carboxylic pharmaceutical agent.
Claim 8
Dependent Claim 164 words
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and at least one anti-inflammatory polymer containing repeating units of the formula ##STR44##wherein R 1 and R 2 are selected from the group of values consisting of a. R 2 is --O--CO--CH 2 -- n O--Z, R 1 is hydrogen and n is 1-10, b. R 2 is --CH 2 --O--CO--CH 2 --O--Z and R 1 is hydrogen or methyl, c. R 2 is --CH 2 --NH--CO--CH 2 --0--Z and R 1 is hydrogen, d. R 2 is --CO--NH--CH 2 --NH--CO--CH 2 --0--Z and R 1 is hydrogen, and ##STR45## wherein r and r' represent alkyl having 1-3 carbon atoms, Y represents chlorine or bromine, and R 1 is hydrogen or methyl, and Z is the acyl residue of an anti-inflammatory pharmaceutical agent whose molecule comprises a carboxylic acid function, said anti-inflammatory polymer being present in a sufficient amount effective to produce a delayed and prolonged action of the residue of said anti-inflammatory carboxylic pharmaceutical agent.
Claim 9
Dependent Claim 19 words
The pharmaceutical composition of claim 6 wherein said polymer has an average molecular weight between about 2,000 and 1,000,000.
Claim 10
Dependent Claim 28 words
The pharmaceutical composition of claim 6 wherein said anti-inflammatory polymer is present in an amount between 0.1-10 percent by weight based on the total weight of said composition.
Claim 11
Dependent Claim 25 words
A dosage unit of the pharmaceutical composition of claim 6 in an amount sufficient to provide 100 mg to 5 g of said anti-inflammatory polymer.

References Cited (Backward Citations)

No citation records indexed.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-01-18 1980-07-19 1981-01-18 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-01-18 1984-07-19 1985-01-18 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-01-18 1988-07-19 1989-01-18 $7700.00 Window Closed / Lapsed

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