发明名称 9-CIS-RETINOIC ACID ESTERS AND AMIDES AND USES THEREOF
摘要 Esters and amides of 9-cis-retinoic acid are synthesized, formulated into pharmaceutically acceptable carriers and administered for the treatment of acne vulgaris, cystic acne, hyperpigmentation, hypopigmentation, psoriasis, dermal and epidermal hypoplasia and kerotoses, the reduction of wrinkling of the skin as an incident of aging and actinic damage, normalization of the production of sebum, the reduction of enlarged pores, promoting the rate of wound healing, limiting of scar tissue formation during healing and the like. They are additionally useful for treatment or amelioration of the same additional classes of skin disorders as is retinoic acid itself and other retinoids. These disorders include ichthyoses (e.g., ichthyosis hystrix, epidermolytic hyperkeratosis, and lamellar ichthyosis), follicular disorders (e.g., pseudofolliculites, senile comedones, nevus comidonicas, and trichostatis spinulosa), benign epithelial tumors (e.g., flat warts, trichoepithelioma, and molluscum contagiosum), perforated dematoses (e.g., elastosis perforans seripiginosa and Kyrles disease), and disorders of keratinization (e.g., Dariers disease, keratoderma, hyperkeratosis plantaris, pityriasis rubra pilaris, lichen planus acanthosis nigricans, and psoriasis). The esters and amides of 9-cis-retinoic acid are also effective for the non-irritating treatment of effects attributable to aging and particularly to photodamage and photoaging. The use of these compounds extends to non-irritating treatments involving the retardation and reversal of additional dermal and cosmetic conditions which are ameliorated by tretinoin such as the effacement of wrinkles, improvement in appearance, namely color and condition of the skin, spots caused from exposure to the sun as well as other skin disorders. The esters and amides of 9-cis-retinoic acid are exceptionally active when compared to other retinoids employed for such indications, and are also exceptionally safe in effective therapeutic doses in contrast to other retinoids.
申请公布号 WO9732839(A1) 申请公布日期 1997.09.12
申请号 WO1996US02979 申请日期 1996.03.04
申请人 MOLECULAR DESIGN INTERNATIONAL, INC. 发明人 PURCELL, WILLIAM, P.
分类号 A61K31/07;A61K31/165;A61K31/203;A61K31/232;C07C57/26;C07C403/16;C07D207/40;C07D207/404;(IPC1-7):C07C57/26 主分类号 A61K31/07
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