Cosmetic use of N-heteroarylbisamide analogs and related compounds
View Patent ↗Cosmetic and dermatological compositions comprising N-heteroarylbisamide analogs and methods of using such compositions to impart anti-aging benefits to the skin and/or improve skin conditions resulting from reduced collagen and hyaluronic acid production are disclosed. The N-heteroarylbisamides are believed to stimulate collagen and hyaluronic acid production and restore or maintain homeostasis for these compounds.
1. A method for improving the aesthetic appearance of human skin comprising topically applying to an area of the skin in need thereof an amount of a cosmetic composition comprising a cosmetically acceptable vehicle and a dermatologically effective amount of a N-heteroarylbisamide of formula I:
where:
Q is N or C;
R, R 2 , R 2 , R 3 , R 4 and R 6 are independently H, C 1 -C 8 alkyl, heteroalkyl, alkoxyalkyl, heteroalkoxyalkyl, C 3 -C 8 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkyl-aryl, heteroalkyl-aryl, aryl-alkyl, and/or heteroaryl-alkyl; and
R 1 and R 5 are independently H, C 1 -C 8 alkyl, heteroalkyl, alkoxyalkyl, heteroalkoxyalkyl, C 3 -C 8 cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkyl-aryl, heteroalkyl-aryl, aryl-alkyl, and/or heteroaryl-alkyl or WR wherein W is CO, CO 2 , CONH, SO 2 , PO 3 , or CH(Oalkyl) 2 ;
and n is 3.
2. The method according to claim 1 , wherein the skin enhancement is an increase in the production of procollagen or collagen, and the aesthetic improvement is selected from the group consisting of:
(a) treatment, reduction, and/or prevention of the appearance of fine lines or wrinkles,
(b) improvement of the skin's thickness, plumpness, and/or tautness;
(c) improvement in skin barrier repair and/or function;
(d) improvement in appearance of skin contours;
(e) increase in skin elasticity and/or resiliency;
(f) treatment, reduction, and/or prevention of skin sagging;
(g) smooth scars and stretch marks; and/or
(h) reduction in pore size.
3. The method according to claim 1 , wherein the skin enhancement is an increase in the production of hyaluronic acid and the aesthetic improvement is selected from the group consisting of:
(a) improvement in the skin's suppleness, softness, tone, radiance, and/or clarity;
(b) improvement in skin texture and/or promotion of retexturization;
(c) restoration of skin luster and/or brightness;
(d) replenishment of essential nutrients and/or constituents in the skin; and/or
(e) improvement of skin moisturization and/or complexion.
4. The method according to claim 1 , wherein the skin enhancement is the modulation of fibroblasts and the aesthetic improvement is selected from the group consisting of:
(a) increase in the production of structural proteins and glucosaminoglycans;
(b) improvement in the structure of collagen;
(c) homoeostasis of structural protein and glucosaminoglycans;
(d) down-regulation of cytokine production;
(e) increased activation of fibroblasts to fibrocytes;
(f) increase in the viability and/or function of fibroblasts;
(g) improvement in maintenance and remodeling of elastin; and/or
(h) improvement in skin barrier repair and/or function.
5. The method according to claim 1 , wherein the skin enhancement is the modulation of kertinocytes and the aesthetic improvement is selected from the group consisting of:
(a) improve the viability and/or function of the keratinocytes
(b) down-regulate the production of inflammatory factors and/or cytokines;
(c) improve skin barrier repair and/or function;
(d) improve thickness of the epidermis;
(e) improve uniformity of epidermal cells;
(f) improvement in pigmentation; and/or
(g) smooth scars and stretch marks.
6. The method of claim 1 , wherein the skin enhancement is improving and maintaining the quality and viability of the extracellular matrix and the aesthetic improvements is selected from the group consisting of:
(a) treatment, reduction, and/or prevention of the appearance of fine lines or wrinkles;
(b) improvement in the skin's thickness, plumpness, and/or tautness;
(c) improvement in skin barrier repair and/or function;
(d) improvement in appearance of skin contours;
(e) increased skin elasticity and/or resiliency;
(f) treatment, reduction, and/or prevention of skin sagging;
(g) smoothing scars and stretch marks;
(h) reduction of pore size;
(i) improvement in the skin's suppleness, softness, tone, radiance, and/or clarity;
(j) improvement in the skin texture and/or promotion of its retexturization;
(k) restoration of skin luster and/or brightness;
(k) replenishment of essential nutrients and/or constituents in the skin; and/or
(l) improvement in skin moisturization and/or type.
7. The method according to claim 1 , wherein the skin enhancement is improving and maintaining the quality and viability of the epidermis and the aesthetic improvement is selected from the group consisting of:
(a) improvement in skin barrier repair and/or function;
(b) improvement of thickness of the epidermis;
(c) improvement in uniformity of epidermal cells;
(d) improvement in pigmentation; and/or
(e) smoothing scars and stretch marks.
8. The method of claim 1 wherein the dermatologically effective amount of the cosmetic composition is applied to the area of skin in need thereof for a time sufficient to improve the area of skin's aesthetic appearance.
9. The method according to claim 8 , wherein the composition is applied to said skin at least once daily for a period of at least four weeks.