US4234599A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Treatment of skin keratoses with α-hydroxy acids and related compounds
Assignee: Individual
•
Filing: 1978-10-04
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Granted: 1980-11-18
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Expires: 1998-10-04
Abstract
Abstract Preventive as well as therapeutic treatment to alleviate the symptoms of skin keratoses consisting of topical application of a solution, gel, lotion, cream or ointment containing one or more of the α- or β-hydroxy acids or α-keto acids, esters thereof, and their amine salts is disclosed. The compounds include free acid or amine salt forms of α-hydroxy-butyric acid, α-hydroxyisobutyric acid, α-hydroxyisocaproic acid, α-hydroxyisovaleric, atrolactic acid, β-hydroxybutyric acid, β-phenyl lactic acid, β-phenylpyruvic acid, citric acid, ethyl pyruvate, galacturonic acid, glucoheptonic acid, glucoheptono 1,4-lactone, gluconic acid, gluconolactone, glucuronic acid, glucuronolactone, glycolic acid, isopropyl pyruvate, lactic acid, malic acid, mandelic acid, methyl pyruvate, mucic acid, pyruvic acid, saccharic acid, saccharic acid 1,4-lactone, tartaric acid, and tartronic acid. The therapeutic composition may include one or more of the compounds present in the total amount of from three to thirty percent. Topical application to affected areas has been found to achieve from substantial to complete remissions of the keratoses in humans.
Inventors
- 👤 Eugene J. Van Scott
- 👤 Ruey J. Yu
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 23:06
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/7004; A61K31/185; A61K31/19; A61K31/33; A61K31/335; A61K31/365; A61K8/00; A61K8/18; A61K8/30; A61K8/33; A61K8/36; A61K8/365; A61Q; A61Q19/00; A61K2800/00; A61K2800/74; A61K2800/75
Claims Analysis
Total Claims: 28
Claim 1
Independent Claim
101 words
A method for alleviating the symptoms of actinic or nonactinic skin keratoses comprising topically applying to involved areas of the body an effective amount of a composition comprising: a therapeutically effective amount of a member selected from the group consisting of α-hydroxybutyric acid, α-hydroxyisobutyric acid, α-hydroxyisocaproic acid, α-hydroxyisovaleric acid, atrolactic acid, β-hydroxybutyric acid, β-phenyl lactic acid, β-phenylpyruvic acid, citric acid, ethyl pyruvate, galacturonic acid, glucoheptonic acid, glucoheptono 1,4-lactone, gluconic acid, gluconolactone, glucuronic acid, glucuronolactone, glycolic acid, isopropyl pyruvate, mandelic acid, methyl pyruvate, mucic acid, pyruvic acid, saccharic acid, saccharic acid 1,4-lactone, tartaric acid and tartronic acid in a pharmaceutically acceptable vehicle.
Claim 2
Independent Claim
101 words
A method for alleviating the symptoms of actinic or nonactinic skin keratoses comprising topically applying to involved areas of the body an effective amount of a composition comprising: a therapeutically effective amount of a member selected from the group consisting of α-hydroxybutyric acid, α-hydroxyisobutyric acid, α-hydroxyisocaproic acid, α-hydroxyisovaleric acid, atrolactic acid, β-hydroxybutyric acid, β-phenyl lactic acid, β-phenylpyruvic acid, citric acid, ethyl pyruvate, galacturonic acid, glucoheptonic acid, glucoheptono 1,4-lactone, gluconic acid, gluconolactone, glucuronic acid, glucuronolactone, glycolic acid, isopropyl pyruvate, mandelic acid, methyl pyruvate, mucic acid, pyruvic acid, saccharic acid, saccharic acid 1,4-lactone, tartaric acid and tartronic acid in a pharmaceutically acceptable vehicle.
Claim 3
Dependent Claim
71 words
The method of claim 1 wherein said composition further comprises a base selected from the group consisting of ammonium hydroxide, an organic primary, secondary, tertiary or quaternary alkylamine, alkanolamine, diamine, dialkylamine, dialkanolamine, alkylalkanolamine, trialkylamine, trialkanol amine, dialkyl alkanolamine, or alkyl dialkanolamine wherein the alkyl or alkanol substituent has from 1 to 8 carbon atoms present in an amount effective to establish a pH of said composition of between 3.0 and 7.5.
Claim 4
Dependent Claim
23 words
The method of claim 1 wherein said member is present in a concentration of from 3-to-30 percent by weight of the total composition.
Claim 5
Dependent Claim
23 words
The method of claim 3 wherein said member is present in a concentration of from 5-to-20 percent by weight of the total composition.
Claim 6
Dependent Claim
35 words
The method of claim 2 wherein said base comprises a member selected from the group consisting of methylamine, ethylamine, monoethanolamine, monoisopropanolamine, ethylenediamine, 1,2-diaminopropane, dimethylamine, diethylamine, diethanolamine, diisopropanolamine, N-methylethanolamine, N-ethylethanolamine, triethylamine, triethanolamine, N-methyldiethanolamine, tri-isopropylamine and choline.
Claim 7
Dependent Claim
37 words
The method of claim 1 wherein the vehicle comprises a mixture of water, ethanol and propylene glycol wherein the concentration of ethanol and propylene glycol does not exceed 70 to 30 percent, respectively, of the total composition.
Claim 8
Dependent Claim
25 words
The method of claim 6 wherein the vehicle comprises a mixture of water, ethanol, and propylene glycol present in a volume ratio of 40:40:20, respectively.
Claim 9
Dependent Claim
27 words
The method of claim 6 wherein the vehicle further comprises a gelling agent present in a concentration of from 0.1 to 5 percent of the total concentration.
Claim 10
Dependent Claim
22 words
The method of claim 8 wherein said gelling agent is a member selected from the group consisting of hydroxyethylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose.
Claim 11
Dependent Claim
23 words
The method of claim 8 wherein said member is present in a concentration of from 1 to 3 percent of the total composition.
Claim 12
Dependent Claim
21 words
The method of claim 1 wherein said vehicle is a member selected from the group consisting of hydrophilic ointment and petrolatum.
Claim 13
Dependent Claim
22 words
The method of claim 6 wherein said vehicle comprises water, ethanol, and propylene glycol present in a volume ratio of 30:60:10, respectively.
Claim 14
Independent Claim
163 words
A method for alleviating the symptoms of actinic or nonactinic skin keratoses comprising topically applying to involved areas of the body an effective amount of a composition comprising: a therapeutically effective amount of a product prepared by reacting, in aqueous or alcoholic aqueous solution, an acid selected from the group consisting of α-hydroxybutyric acid, α-hydroxyisobutyric acid, α-hydroxyisocaproic acid, α-hydroxyisovaleric acid, atrolactic acid, β-hydroxybutyric acid, β-phenyl lactic acid, β-phenylpyruvic acid, citric acid, ethyl pyruvate, galacturonic acid, glucoheptonic acid, glucoheptono 1,4-lactone, gluconic acid, gluconolactone, glucuronic acid, glucuronolactone, glycolic acid, isopropyl pyruvate, lactic acid, mandelic acid, methyl pyruvate, mucic acid, pyruvic acid, saccharic acid, saccharic acid 1,4-lactone, tartaric acid and tartronic acid, or the anhydride thereof, and a base selected from the group consisting of ammonium hydroxide, an organic primary, secondary, tertiary or quaternary alkylamine, alkanolamine, diamine, dialkylamine, dialkanolamine, alkylalkanolamine, trialkylamine, trialkanol amine, Dialkyl alkanol amine, or alkyldialkanolamine wherein the alkyl or alkanol substituent has from 1 to 8 carbon atoms in a pharmaceutically acceptable vehicle.
Claim 15
Independent Claim
163 words
A method for alleviating the symptoms of actinic or nonactinic skin keratoses comprising topically applying to involved areas of the body an effective amount of a composition comprising: a therapeutically effective amount of a product prepared by reacting, in aqueous or alcoholic aqueous solution, an acid selected from the group consisting of α-hydroxybutyric acid, α-hydroxyisobutyric acid, α-hydroxyisocaproic acid, α-hydroxyisovaleric acid, atrolactic acid, β-hydroxybutyric acid, β-phenyl lactic acid, β-phenylpyruvic acid, citric acid, ethyl pyruvate, galacturonic acid, glucoheptonic acid, glucoheptono 1,4-lactone, gluconic acid, gluconolactone, glucuronic acid, glucuronolactone, glycolic acid, isopropyl pyruvate, lactic acid, mandelic acid, methyl pyruvate, mucic acid, pyruvic acid, saccharic acid, saccharic acid 1,4-lactone, tartaric acid and tartronic acid, or the anhydride thereof, and a base selected from the group consisting of ammonium hydroxide, an organic primary, secondary, tertiary or quaternary alkylamine, alkanolamine, diamine, dialkylamine, dialkanolamine, alkylalkanolamine, trialkylamine, trialkanol amine, Dialkyl alkanol amine, or alkyldialkanolamine wherein the alkyl or alkanol substituent has from 1 to 8 carbon atoms in a pharmaceutically acceptable vehicle.
Claim 16
Dependent Claim
16 words
The method of claim 13 wherein said composition has a pH of from 3.0 to 7.5.
Claim 17
Dependent Claim
23 words
The method of claim 13 wherein said product is present in a concentration of from 3-to-30 percent by weight of the total composition.
Claim 18
Dependent Claim
23 words
The method of claim 13 wherein said product is present in a concentration of from 5-to-20 percent by weight of the total composition.
Claim 19
Dependent Claim
37 words
The method of claim 13 wherein the vehicle comprises a mixture of water, ethanol and propylene glycol wherein the concentration of ethanol and propylene glycol does not exceed 70 and 30 percent, respectively, of the total composition.
Claim 20
Dependent Claim
25 words
The method of claim 17 wherein the vehicle comprises a mixture of water, ethanol, and propylene glycol present in a volume ratio of 40:40:20, respectively.
Claim 21
Dependent Claim
27 words
The method of claim 17 wherein the vehicle further comprises a gelling agent present in a concentration of from 0.1 to 5 percent of the total concentration.
Claim 22
Dependent Claim
22 words
The method of claim 19 wherein said gelling agent is a member selected from the group consisting of hydroxyethylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose.
Claim 23
Dependent Claim
23 words
The method of claim 19 wherein said member is present in a concentration of from 1 to 3 percent of the total composition.
Claim 24
Dependent Claim
21 words
The method of claim 13 wherein said vehicle is a member selected from the group consisting of hydrophilic ointment and petrolatum.
Claim 25
Dependent Claim
22 words
The method of claim 17 wherein said vehicle comprises water, ethanol, and propylene glycol present in a volume ratio of 30:60:10, respectively.
Claim 26
Independent Claim
40 words
A method for alleviating the symptoms of actinic or non-actinic skin keratoses comprising topically applying to involved areas of the body an effective amount of a composition comprising: a therapeutically effective amount of malic acid in a pharmaceutically acceptable vehicle.
Claim 27
Independent Claim
40 words
A method for alleviating the symptoms of actinic or non-actinic skin keratoses comprising topically applying to involved areas of the body an effective amount of a composition comprising: a therapeutically effective amount of malic acid in a pharmaceutically acceptable vehicle.
Claim 28
Dependent Claim
58 words
The method of claim 24 wherein composition further comprises a base selected from the group consisting of ammonium hydroxide, an organic primary, secondary, tertiary or quaternary alkylamine, alkanolamine, diamine, dialkylamine, dialkanolamine, alkylalkanolamine, trialkylamine, trialkanol amine, dialkyl alkanol amine, or alkyldialkanolamine wherein the alkyl or alkanol substituent has from 1 to 8 carbon atoms in a pharmaceutically acceptable vehicle.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-11-18 | 1984-05-19 | 1984-11-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-11-18 | 1988-05-19 | 1988-11-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-11-18 | 1992-05-19 | 1992-11-18 | $7700.00 | Window Closed / Lapsed |