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EP0273202B1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Use of hydroxycarboxylic acids to enhance therapeutic effects of topical compositions for fungal infections and pigmented spots.

Assignee: Individual
•
Filing: 1987-11-25
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Granted: 1995-06-21
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Expires: 2007-11-25
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Abstract

No abstract record available.

Inventors

  • 👤 Eugene J. Dr. Van Scott
  • 👤 Ruey J. Dr. Yu

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-07 19:12
CPC Classifications
A; A61; A61Q; A61Q17/00; A61Q17/005; A61K; A61K31/00; A61K31/185; A61K31/19; A61K31/191; A61K31/194; A61K31/195; A61K31/20; A61K31/202; A61K31/33; A61K31/335; A61K31/365; A61K31/366; A61K31/395; A61K31/40; A61K31/403; A61K31/404; A61K31/405; A61K31/41; A61K31/415; A61K31/435; A61K31/44; A61K31/445; A61K31/66; A61K31/70; A61K31/7042; A61K31/7048; A61K31/715; A61K45/00; A61K45/06; A61K47/00; A61K47/06; A61K47/08; A61K47/12; A61K47/16; A61K47/18; A61K47/183; A61K47/24; A61K47/26; A61K8/00; A61K8/18; A61K8/30; A61K8/33; A61K8/34; A61K8/347; A61K8/36; A61K8/362; A61K8/365; A61K8/37; A61K8/375; A61K8/38; A61K8/40; A61K8/42; A61K8/43; A61K8/49; A61K8/494; A61K8/4953; A61K8/4973; A61K8/60; A61K8/63; A61K8/67; A61K8/671; A61K8/673; A61K8/675; A61K8/676; A61K9/00; A61K9/0012; A61K9/0014; A61Q17/04; A61Q19/00; A61Q19/007; A61Q19/008; A61Q19/02; A61Q19/08; A61Q19/10; A61Q5/00; A61Q5/006; A61Q5/02; A61Q7/00

Claims Analysis

Total Claims: 21
Claim 1
Independent Claim 81 words
Use of - a topical dermatologic agent together with - an enhancing effective amount of at least one compound selected from the group consisting of hydroxycarboxylic acids and ketocarboxylic acids and esters, lactones, or salt forms thereof, wherein the composition must not contain reductive diphenols together with a plant extract, for the preparation of a topical dermatologic therapeutic composition with enhanced therapeutic effect for use in the treatment of fungal infections, and pigmented spots including pigmented age spots, melasma, and lentigines.
Claim 2
Dependent Claim 36 words
Use of the composition of claim 1, wherein said agent is a member selected from the group consisted of: clotrimazole, candicidin; griseofulvin, hydroquinone and its monomethyl and benzyl ethers; ketoconazole, miconazole, nystatin, flucytosine, amphotericins and tolnaftate.
Claim 3
Dependent Claim 122 words
Use of the composition of claim 1 or 2 wherein said hydroxycarboxylic acid is hydroxymonocarboxylic acid having the following chemical structural formula: R₁(CR₂OH) m (CH₂) n COOH wherein R₁, R₂=H, alkyl, aralkyl or aryl group of saturated or unsaturated, straight or branched chain or cyclic form, having 1 to 25 carbon atoms. m=1,2,3,4,5,6,7,8 or 9 n=0 or a numerical number up to 23 present as free acid, lactone or salt form, and as optically active or inactive isomer such as D, L, and DL forms; the hydrogen atom attached to the carbon atom may be substituted by a nonfunctional F, Cl, Br, I, or S atom or a lower alkyl or alkoxy saturated or unsaturated radical, having 1 to 9 carbon atoms.
Claim 4
Dependent Claim 98 words
Use of the composition of claim 3 wherein said hydroxymonocarboxylic acid is a member selected from the group consisted of 2-hydroxyacetic acid; 2-hydroxypropanoic acid; 2-methyl 2-hydroxypropanoic acid; 2-hydroxybutanoic acid; phenyl 2-hydroxyacetic acid; phenyl 2-methyl 2-hydroxyacetic acid; 3-phenyl 2-hydroxypropanoic acid; 2,3-dihydroxypropanoic acid; 2,3,4-trihydroxybutanoic acid; 2,3,4,5-tetrahydroxypentanoic acid; 2,3,4,5,6-pentahydroxyhexanoic acid; 2-hydroxydodecanoic acid; 2,3,4,5,6,7-hexahydroxyheptanoic acid; diphenyl 2-hydroxyacetic acid; 4-hydroxymandelic acid; 4-chloromandelic acid; 3-hydroxybutanoic acid; 4-hydroxybutanoic acid; 2-hydroxyhexanoic acid; 5-hydroxydodecanoic acid; 12-hydroxydodecanoic acid; 10-hydroxydecanoic acid; 16-hydroxyhexadecanoic acid; 2-hydroxy-3-methylbutanoic acid; 2-hydroxy-4-methylpentanoic acid; 3-hydroxy-4-methoxymandelic acid; 4-hydroxy-3-methoxymandelic acid; 2-hydroxy-2-methylbutanoic acid; 3-(2-hydroxyphenyl) lactic acid; 3-(4-hydroxyphenyl) lactic acid; hexahydromandelic acid; 3-hydroxy-3-methylpentanoic acid; 4-hydroxydecanoic acid; 5-hydroxydecanoic acid; aleuritic acid.
Claim 5
Dependent Claim 26 words
Use of the composition of claim 3 wherein said lactone is an intermolecular or intramolecular lactone including linear acid polymer, ribonolactone, gluconolactone, galactonolactone, gulonolactone and mannonolactone.
Claim 6
Dependent Claim 85 words
Use of the composition of claim 1 or 2 wherein said compound is a keto or hydroxyketomonocarboxylic acid selected from the group consisting of pyruvic acid, hydroxypyruvic acid, hydroxypyruvic acid phosphate, methyl pyruvate, ethyl pyruvate, propyl pyruvate, isopropyl pyruvate, phenyl pyruvic acid, methyl phenyl pyruvate, ethyl phenyl pyruvate, propyl phenyl pyruvate; formyl formic acid, methyl formyl formate, ethyl formyl formate, propyl formyl formate, benzoyl formic acid, methyl benzoyl formate, ethyl benzoyl formate, propyl benzoyl formate, 4-hydroxybenzoyl formic acid, 4-hydroxyphenyl pyruvic acid, and 2-hydroxyphenyl pyruvic acid.
Claim 7
Dependent Claim 89 words
Use of the composition of claim 1 or 2 wherein said compound is a hydroxydicarboxylic acid having the following chemical structural formula: wherein m=1,2,3,4,5,6,7,8, or 9 n=0 or a numerical number up to 23 present as free acid, lactone or salt form, and as optically active or inactive D, L, and meso isomer; hydrogen atom attached to the carbon atom may be substituted by a nonfunctional F, Cl, Br, I, or S atom or a lower alkyl or alkoxy saturated or unsaturated radical, having 1 to 9 carbon atoms.
Claim 8
Dependent Claim 54 words
Use of the composition of claim 7 wherein said hydroxydicarboxylic acid is a member selected from the group consisted of 2-hydroxypropanedioic acid; 2-hydroxybutanedioic acid; erythraric acid; threaric acid; arabiraric acid; ribaric acid; xylaric acid; lyxaric acid; glucaric acid; galactaric acid; mannaric acid; gularic acid; allaric acid; altraric acid; idaric acid; talaric acid; 2-hydroxy-2-methylbutanedioic acid.
Claim 9
Dependent Claim 20 words
Use of the composition of claim 7 wherein said lactone is an intermolecular or intramolecular lactone including saccharic acid, 1,4-lactone.
Claim 10
Dependent Claim 62 words
Use of the composition of claim 1 or 2 wherein said compound is a hydroxycarboxylic acid having the following formula: R (OH) m (COOH) n Wherein m,n = 1,2,3,4,5,6,7,8 or 9 R= alkyl, aralkyl or aryl group of saturated or unsaturated, straight or branched chain or cyclic form, having 1 to 25 carbon atoms, present as free acid, lactone or salt form.
Claim 11
Dependent Claim 114 words
Use of the composition of claim 10 wherein said acid is a member selected from the group consisting of citric acid, isocitric acid, agaricic acid, quinic acid, citramalic acid, glucuronic acid, glucuronolactone, galacturonic acid, galacturonolactone, uronic acids, uronolactones, asorbic acid, dihydroascorbic acid, dihydroxytartaric acid, 1-hydroxy-1-cyclopropanecarboxylic acid, 5-hydroxylysine, 3-hydroxy-2-aminopentanoic acid; 4-hydroxy-3-pentenoic acid, 4-hydroxy-2, 2-diphenylbutanoic acid, and 3-hydroxy-3-methylglutaric acid and ester, lactone or salt forms thereof, and as an optically active or inactive D, L, DL or meso isomer; the hydrogen atom attached to the carbon atom may be substituted by a nonfunctional F, Cl, Br, I or S atom or a lower alkyl or alkoxy saturated or unsaturated radical having 1 to 9 carbon atoms.
Claim 12
Dependent Claim 16 words
Use of the composition of claim 10 wherein the lactone is an inter or intramolecular lactone.
Claim 13
Dependent Claim 98 words
Use of the composition of claim 1 or 2 wherein said compound is selected from the group consisting of: Citramalic acid, Diphenyl 2-hydroxyacetic acid (benzilic acid), 2-phenyl 3-hydroxypropanoic acid (tropic acid), aleuritic acid, ribonic acid, ribonoloactone, 2,3,4-trihydroxybutanoic acid, 2,3,4,5-tetrahydroxypentanoic acid, 2,3,4,5,6-pentahydroxyhexanoic acid, 2-hydroxylauric acid, 2,3,4,5,6,7-hexahydroxyheptanoic acid, 4-hydroxymandelic acid, 4-chloromandelic acid, 2-hydroxy-3-methylbutanoic acid, 2-hydroxy-4-methylpentanoic acid, 3-hydroxy-4-methoxymandelic acid, 4-hydroxy-3-methoxymandelic acid, 3-(3-hyroxphenyl) lactic acid, 3-(4-hydroxyphenyl) lactic acid, hexahydromandelic acid, 3-hydroxy-3-methylpentanoic acid, 1-hydroxy-1-cyclopropane carboxylic acid, 4-hydroxybutanoic acid, 2-hydroxyhexanoic acid, 5-hydroxylauric acid, 12-hydroxylauric acid, 10-hydroxydecanoic acid, 16-hydroxyhexadecanoic acid, 4-hydroxydecanoic acid, 5-hydroxydecanoic acid, and 4-hydroxy-2, 2-diphenylbutanoic acid as a free acid or salt form.
Claim 14
Dependent Claim 32 words
Use of the composition of any of claims 1 to 13 wherein the topical dermatologic agent is selected from the group consisting of hydroquinone and hydroquinone monoether including menomethyl and monobenzyl ether.
Claim 15
Dependent Claim 95 words
Use of the composition of claim 14 wherein said hydroxycarboxylic acids and related ketocarboxylic acid and ester, lactone or salt forms thereof include glycolic acid, benzilic acid, tropic acid, lactic acid, malic acid, citric acid, isocitric acid, citramalic acid, tartronic acid, tartaric acid, gluconic acid, galactonic acid, alpha hydroxyisobutyric acid, phenyllactic acid, mandelic acid, atrolactic acid, gluconolactone, galactonolactone, ribonic acid, ribonolactone, pantoic acid, pantolactone, pantothenic acid, alpha hydroxybutyric acid, Beta hydroxybutyric acid, quinic acid, pyruvic acid, phenyl pyruvic acid, methyl pyruvate, ethyl pyruvate, ascorbic acid, benzoyl formic acid, methyl benzoyl formate, and ethyl benzoyl formate.
Claim 16
Dependent Claim 20 words
Use of the composition of any of claims 1 to 13 wherein the topical dermatologic agent is an antifungal agent.
Claim 17
Dependent Claim 18 words
Use of the composition of any of claims 1 to 4 wherein said hydroxycarboxylic acid is glycolic acid.
Claim 18
Dependent Claim 18 words
Use of the composition of any of claims 1 to 4 wherein said hydroxycarboxylic acid is lactic acid.
Claim 19
Dependent Claim 14 words
Use of the composition of claim 10 wherein said hydroxycarboxylic acid is citric acid.
Claim 20
Dependent Claim 13 words
Use of the composition of claim 13 wherein said hydroxycarboxylic acid is gluconolactone.
Claim 21
Dependent Claim 14 words
Use of the composition of claim 7 wherein said hydroxycarboxylic acid is tartaric acid.

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