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EP0253393A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Methods for treatment of sundamaged human skin with retinoids

Assignee: Individual
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Filing: 1987-07-16
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Granted: —
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Expires: 2007-07-16
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Abstract

Abstract Various effects of photoaging or sundamage of skin including impairment of differentiation of epidermal epithelial cells and loss of collagen fibers, abnormal changes in elastic fibers and deterioration of small blood vessels in the dermis of the skin are retarded by applying topically to the epidermis in a maintenance therapy program effective amounts of retinoids including retinoid derivatives and stereoisomers thereof such that epithelial growths are substantially reduced and prevented and the skin substantially regains and maintains its firmness, turgor and elasticity. Moreover, with persistent treatment dermal blood cells and vessels increase and the epidermis and dermis thicken, resulting in improved ability of the skin to sense, resist and recover from irritation or injury. Further, hyperpigmentation, lines and wrinkles due to aging are reduced and prevented. The treatment is particularly useful for human facial skin and preferably applied in amounts insufficient to cause excessive irritation.

Inventors

  • 👤 Albert M. Kligman

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-28 10:43
CPC Classifications
C; C07; C07F; C07F7/00; C07F7/22; A; A61; A61Q; A61Q19/00; A61Q19/004; A61K; A61K8/00; A61K8/18; A61K8/30; A61K8/67; A61K8/671; A61P; A61P17/00; A61P3/00; A61P3/02; A61P43/00; A61Q19/08; C07F7/2224; C23; C23C; C23C16/00; C23C16/22; C23C16/30; C23C16/40; C23C16/407

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 91 words
A method for retarding and reversing the loss of collagen fibers, abnormal changes in elastic fibers, deterioration of small blood vessels, and formation of abnormal epithelial growths in sundamaged human skin, comprising applying topically to the surface of the skin a composition comprising effective amounts of a retinoid in an emollient vehicle in a program of maintenance therapy, whereby the skin substantially regains and maintains its firmness, turgor and elasticity during said therapy, said composition and amounts of retinoid therein being selected so as to provide a sub-irritating dose for application.
Claim 2
Independent Claim 91 words
A method for retarding and reversing the loss of collagen fibers, abnormal changes in elastic fibers, deterioration of small blood vessels, and formation of abnormal epithelial growths in sundamaged human skin, comprising applying topically to the surface of the skin a composition comprising effective amounts of a retinoid in an emollient vehicle in a program of maintenance therapy, whereby the skin substantially regains and maintains its firmness, turgor and elasticity during said therapy, said composition and amounts of retinoid therein being selected so as to provide a sub-irritating dose for application.
Claim 3
Dependent Claim 24 words
A method according to claim 1 wherein said retinoid is selected from the group consisting of retinoic acids, retinoic acid derivatives and stereoisomers thereof.
Claim 4
Dependent Claim 28 words
A method according to claim 2 wherein said retinoic acid, retinoic acid derivatives is selected from the group consisting of 13-cis-retinoic acid, 13-cis-retinoic acid derivatives and stereoisomers thereof.
Claim 5
Dependent Claim 26 words
A method according to claim 1 wherein said retinoid is selected from the group consisting of (E)-4-[4-methyl-6-(2,6,6-trimethyl-1-­ cyclohexen-1-yl)-1,3,5-hexatrienyl] benzoic acid; 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-­naphthalenyl)ethylnyl]-benzoic acid; and (E)-4-[2-­(5,6,7,8-tetrahydro-7-hydroxy-5,5,8,8-tetramethyl-­2-naphthalenyl-1-propenyl] benzyl alcohol.
Claim 6
Independent Claim 60 words
A method according to claiOm 1 wherein said retinoid is selected from the group consisting of 13-cis-retinoic acid; (all-E)-9-(4-­methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-­2,4,6,8-nonatetraenoic acid ethyl ester; (all-E)-9-­(4-methoxy-2,3,6,-trimethylphenyl)-3,7-dimethyl-­2,4,6,8,-nonatetraenoic acid; N-ethyl-9-(4-methoxy-­2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-­nonatetraenamide; (E,E)-9-(2,6-dichloro-4-methoxy-­3-methylphenyl)-3,7-dimethyl-2,4,6,8,-nonatetraenoic acid ethyl ester; 7,8-didehydroretinoic acid; (E,E)-4-[2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-­1-yl)-1,3-butadienyl] benzoic acid; (all-E)-3,7-­dimethyl-(3-thienyl)-2,4,6,8-nonatetraenoic acid; (E,E,E)-3-methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-­tetramethyl-2-naphthalenyl)-2,4,6-octatrienoic acid; (E)-6-[2-(2,6,6-trimethyl-1-cyclohexen-1-­yl)ethenyl]-2-naphthalenecarboxylic acid; (E,E,E)-­7-(2,3-dihydro-1,1,3,3-tetramethyl-1H-inden-5-yl)-­3-methyl-2,4,6-octatrienoic acid; (E)-4-[2-(2,3-­dihydro-1,1,3,3-tetra-methyl-1H-inden-5-yl)-1-­propenyl] benzoic acid; TTNPB (E)-4-[2-(5,6,7,8-­ tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl-1-­propenyl] benzoic acid; (E)-4-[2-(5,6,7,8-­tetrahydro-3-methyl-5,5,8,8-tetramethyl-2-­naphthalenyl)-1-propenyl] benzoic acid; (E)-­1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6-(1-methyl-­2-phenylethenyl) nathalene; 6-(1,2,3,4-­tetrahydro-1,1,4,4-tetra-methyl-6-naphthyl)-2-­naphthalene-carboxylic acid; (E)-6-[2-[4-­(ethylsulfonyl)phenyl]-1-methylethenyl]-1,2,3,4-­tetrahydro-1,1,4,4-tetramethylnaphthalene; and (E)-­2-(1,1,4,4-tetramethyl-1,2,3,4-tetrahydronaphth-7-­yl)-1-[4-tetrazol-5-yl)phenyl]-1-propene.
Claim 7
Independent Claim 60 words
A method according to claiOm 1 wherein said retinoid is selected from the group consisting of 13-cis-retinoic acid; (all-E)-9-(4-­methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-­2,4,6,8-nonatetraenoic acid ethyl ester; (all-E)-9-­(4-methoxy-2,3,6,-trimethylphenyl)-3,7-dimethyl-­2,4,6,8,-nonatetraenoic acid; N-ethyl-9-(4-methoxy-­2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-­nonatetraenamide; (E,E)-9-(2,6-dichloro-4-methoxy-­3-methylphenyl)-3,7-dimethyl-2,4,6,8,-nonatetraenoic acid ethyl ester; 7,8-didehydroretinoic acid; (E,E)-4-[2-methyl-4-(2,6,6-trimethyl-1-cyclohexen-­1-yl)-1,3-butadienyl] benzoic acid; (all-E)-3,7-­dimethyl-(3-thienyl)-2,4,6,8-nonatetraenoic acid; (E,E,E)-3-methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-­tetramethyl-2-naphthalenyl)-2,4,6-octatrienoic acid; (E)-6-[2-(2,6,6-trimethyl-1-cyclohexen-1-­yl)ethenyl]-2-naphthalenecarboxylic acid; (E,E,E)-­7-(2,3-dihydro-1,1,3,3-tetramethyl-1H-inden-5-yl)-­3-methyl-2,4,6-octatrienoic acid; (E)-4-[2-(2,3-­dihydro-1,1,3,3-tetra-methyl-1H-inden-5-yl)-1-­propenyl] benzoic acid; TTNPB (E)-4-[2-(5,6,7,8-­ tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl-1-­propenyl] benzoic acid; (E)-4-[2-(5,6,7,8-­tetrahydro-3-methyl-5,5,8,8-tetramethyl-2-­naphthalenyl)-1-propenyl] benzoic acid; (E)-­1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6-(1-methyl-­2-phenylethenyl) nathalene; 6-(1,2,3,4-­tetrahydro-1,1,4,4-tetra-methyl-6-naphthyl)-2-­naphthalene-carboxylic acid; (E)-6-[2-[4-­(ethylsulfonyl)phenyl]-1-methylethenyl]-1,2,3,4-­tetrahydro-1,1,4,4-tetramethylnaphthalene; and (E)-­2-(1,1,4,4-tetramethyl-1,2,3,4-tetrahydronaphth-7-­yl)-1-[4-tetrazol-5-yl)phenyl]-1-propene.
Claim 8
Dependent Claim 13 words
A method according to claim 1 wherein said skin is human facial skin.
Claim 9
Dependent Claim 13 words
A method according to claim 2 wherein said skin is human facial skin.
Claim 10
Dependent Claim 13 words
A method according to claim 3 wherein said skin is human facial skin.
Claim 11
Dependent Claim 14 words
A method according to claim 1 wherein said emollient vehicle is a cream ointment.

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