US5264216A
Expired / Lapsed
US
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Pharmaceutical uses of bilobalide and derivatives thereof and pharmaceutical compositions adapted for such use
Assignee: Indena SpA
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Filing: 1992-03-25
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Granted: 1993-11-23
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Expires: 2012-03-25
Abstract
Abstract A method of treating an infection in an individual, by administering an effective dose of bilobalide or of a pharmacologically acceptable derivative thereof. Activity against infection with Pneumocystis carinii has major utility in treating AIDS-associated infections. Bilobalide may be administered systemically or topically in accordance with the invention. For systemic use, oral and parenteral routes of administration may be used.
Inventors
- 👤 Ezio Bombardelli
- 👤 Mario Ghione
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 01:32
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/34; A61K31/365; A61P; A61P1/00; A61P1/02; A61P13/00; A61P13/02; A61P15/00; A61P31/00; A61P31/04; A61P31/10; A61P33/00; A61P33/02; Y; Y02; Y02A; Y02A50/00; Y02A50/30
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
76 words
A method of combatting an infection in an individual having an infection with a pathological strain selected from the group consisting of Trichomonas vaginalis, Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Lactobacillus sp. and Pneumocystis carinii, which comprises administering to the individual via a route of administration which delivers it to the site of infection, an effective dose of bilobalide or of a pharmacologically acceptable derivative thereof, whereby an antibiotic effect against said pathological strain is obtained.
Claim 2
Independent Claim
76 words
A method of combatting an infection in an individual having an infection with a pathological strain selected from the group consisting of Trichomonas vaginalis, Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Lactobacillus sp. and Pneumocystis carinii, which comprises administering to the individual via a route of administration which delivers it to the site of infection, an effective dose of bilobalide or of a pharmacologically acceptable derivative thereof, whereby an antibiotic effect against said pathological strain is obtained.
Claim 3
Dependent Claim
32 words
A method according to claim 1 wherein said pharmacologically acceptable derivatives are esters in which one or both of the hydroxy groups of bilobalide are esterified with a C 2-22 carboxylic acid.
Claim 4
Dependent Claim
49 words
A method according to claim 2 wherein the C 2-22 carboxylic acids are selected from C 2-22 alkanoic acids, C 2-22 alkenoic acids and C 2-22 alkadienoic acids having the formulae C n H 2n+1 COOH, C n H 2n-1 COOH and C n H 2n-3 COOH (n=1-21), respectively.
Claim 5
Dependent Claim
13 words
A method according to claim 13 wherein n is from 17 to 21.
Claim 6
Dependent Claim
17 words
A method according to claim 1 wherein said pharmacologically acceptable derivatives are complexes of bilobalide with phospholipids.
Claim 7
Dependent Claim
67 words
A method according to claim 5 wherein said complexes have the formula ##STR3## wherein R and R 1 , which can be the same or different are each an acyl residue of a C 16-22 saturated or unsaturated fatty acid, and R 2 is --CH 2 CH 2 N(CH 3 ) 3 , --CH 2 CH 2 NH 3 or --CH 2 CH 2 (COOH)NH 3 .
Claim 8
Independent Claim
28 words
A method of treating a vaginal infection in an individual, which comprises administering an effective dose of bilobalide or of a pharmacologically acceptable derivative thereof to the vagina.
Claim 9
Independent Claim
28 words
A method of treating a vaginal infection in an individual, which comprises administering an effective dose of bilobalide or of a pharmacologically acceptable derivative thereof to the vagina.
Claim 10
Dependent Claim
32 words
A method according to claim 7 wherein said pharmacologically acceptable derivatives are esters in which one or both of the hydroxy groups of bilobalide are esterified with a C 2-22 carboxylic acid.
Claim 11
Dependent Claim
49 words
A method according to claim 8 wherein the C 2-22 carboxylic acids are selected from C 2-22 alkanoic acids, C 2-22 alkenoic acids and C 2-22 alkadienoic acids having the formulae C n H 2n+1 COOH, C n H 2n-1 COOH and C n H 2n-3 COOH (n=1-21), respectively.
Claim 12
Dependent Claim
13 words
A method according to claim 9 wherein n is from 17 to 21.
Claim 13
Dependent Claim
17 words
A method according to claim 10 wherein said pharmacologically acceptable derivatives are complexes of bilobalide with phospholipids.
Claim 14
Dependent Claim
67 words
A method according to claim 11 wherein said complexes have the formula ##STR4## wherein R and R 1 , which can be the same or different are each an acyl residue of a C 16-22 saturated or unsaturated fatty acid, and R 2 is --CH 2 CH 2 N(CH 3 ) 3 , --CH 2 CH 2 NH 2 or --CH 2 CH 2 (COOH)NH 2 .
Claim 15
Dependent Claim
31 words
A method according to claim 1 wherein said infection is with an individual with Pneumocystis carinii, which comprises administering an effective dose of bilobalide or of a pharmacologically acceptable derivative thereof.
Claim 16
Dependent Claim
62 words
A pharmaceutical composition for combatting a vaginal infection in an individual having a vaginal infection with a pathological strain selected from the group consisting of Trichomonas vaginalis, Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Lactobacillus sp. and Pneumocystis carinii which comprises bilobalide or a pharmacologically acceptable derivative thereof and a pharmceutically acceptable excipient, said composition being in a form adapted for vaginal administration.
Claim 17
Dependent Claim
62 words
A pharmaceutical composition for combatting a vaginal infection in an individual having a vaginal infection with a pathological strain selected from the group consisting of Trichomonas vaginalis, Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Lactobacillus sp. and Pneumocystis carinii which comprises bilobalide or a pharmacologically acceptable derivative thereof and a pharmceutically acceptable excipient, said composition being in a form adapted for vaginal administration.
Claim 18
Dependent Claim
15 words
A pharmaceutical composition according to claim 14 being in the form of a vaginal suppository.
References Cited (Backward Citations)
US4892883A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1996-11-22 | 1997-05-24 | 1997-11-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-11-22 | 2001-05-24 | 2001-11-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-11-22 | 2005-05-24 | 2005-11-23 | $7700.00 | Window Closed / Lapsed |