Claims
- 1. A composition comprising a vitamin D analog and a retinoid, wherein:
(a) the vitamin D analog is capable of binding a vitamin D receptor or being converted in vivo into a compound capable of binding a vitamin D receptor; and (b) the retinoid is selected from the group consisting of 4-oxo-retinol, 4-oxo-retinal, and 4-oxo-retinyl ester.
- 2. A topical composition according to claim 1.
- 3. The composition of claim 1, wherein the vitamin D analog is selected from the group consisting of cholecalciferol, calcifediol, calcitriol, calcipotriol, ergocalciferol, dihydrotachysterol, 1, 25-dihydroxyergocalciferol, and 25-hydroxydihydrotachysterol.
- 4. The composition of claim 1, wherein the vitamin D analog is calcitriol.
- 5. The composition of claim 1, wherein the vitamin D analog is calcipotriol.
- 6. The composition of claim 1, wherein the retinoid is 4-oxo-retinol.
- 7. The composition of claim 1, wherein the vitamin D analog is calcitriol or calcipotriol at a concentration of about 0.005% and the retinoid is a 4-oxo-retinol.
- 8. The composition of claim 1, wherein the retinoid is 4-oxo-retinal.
- 9. A method of treating a subject suffering from a disorder characterized by abnormal cell-proliferation and/or cell-differentiation, comprising administering to the subject in need of such treatment a vitamin D analog and a retinoid either simultaneously or at different times, wherein:
(a) the vitamin D analog is capable of binding a vitamin D receptor or being converted in vivo into a compound capable of binding a vitamin D receptor; and (b) the retinoid is selected from the group consisting of 4-oxo-retinol, 4-oxo-retinoic acid, 4-oxo-retinal, and 4-oxo-retinyl ester.
- 10. The method of claim 9, wherein the retinoid is 4-oxo-retinol.
- 11. A method of treating a subject suffering from a disorder selected from the group consisting of psoriasis, acne, atopic dermatitis, eczema, rosacea, actinic keratosis, seborrheic dermatitis, and congenital keratinization disorders, comprising administering to the subject in need of such treatment a vitamin D analog and a retinoid either simultaneously or at different times, wherein:
(a) the vitamin D analog is capable of binding a vitamin D receptor or being converted in vivo into a compound capable of binding a vitamin D receptor; and (b) the retinoid is selected from the group consisting of 4-oxo-retinol, 4-oxo-retinoic acid, 4-oxo-retinal, and 4-oxo-retinyl ester.
- 12. The method of claim 11, wherein the disorder is psoriasis.
- 13. The method of claim 11, wherein the disorder is eczema.
- 14. The method of claim 11, wherein the disorder is acne.
- 15. The method of claim 11, wherein the disorder is atopic dermatitis.
- 16. The method of claim 11, wherein the retinoid is 4-oxo-retinol.
- 17. A method of treating one or more conditions of the skin selected from the group consisting of dry skin, photodamaged skin, age spots, aged skin, inflexibility of stratum corneum, wrinkles, fine lines, actinic blemishes, skin dyschromias, and ichthyosis, comprising applying to the skin having said one or more condition a vitamin D analog and a retinoid either simultaneously or at different times, wherein:
(a) the vitamin D analog is capable of binding a vitamin D receptor or being converted in vivo into a compound capable of binding a vitamin D receptor; and (b) the retinoid is selected from the group consisting of 4-oxo-retinol, 4-oxo-retinoic acid, 4-oxo-retinal, and 4-oxo-retinyl ester.
- 18. The method of claim 17, wherein the retinoid is 4-oxo-retinol.
- 19. A method of preventing or treating hair loss comprising applying to a scalp suffering from such condition either simultaneously or at different times:
(a) a vitamin D analog capable of binding a vitamin D receptor or being converted in vivo into a compound capable of binding a vitamin D receptor; and (b) a retinoid selected from the group consisting of retinoid D with an alcohol CH2OH terminal side chain, an ester of retinoid D having an ester bond, an ether of retinoid D having an ether bond, and retinoid D where the alcohol CH2OH terminal side chain is replaced with an aldehyde CHO terminal side chain, wherein each of the ester bond and the ether bond is formed with the oxygen at the terminal side chain of Retinoid D and wherein retinoid D with the alcohol CH2OH terminal side chain has the structure: 13wherein R1 is selected from the group consisting of 14wherein the keto group at the 4-position is free or protected, or is replaced by a thioketone group which is free or protected or is replaced by C1-6-alkylidene group; 15wherein X is selected from the group consisting of hydrogen and C1-6-alkyl and Y is selected from the group consisting of C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino and wherein the absolute configuration at the 4-position is independently R or S; 16wherein X1, Y1 are independently selected from the group consisting of hydrogen, C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6- alkyl substituted amino and Z1 is selected from the group consisting of C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino; 17wherein X2 is selected from the group consisting of hydrogen, C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino and Z2 is selected from the group consisting of C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino; and 18wherein X3 and Y3 are independently selected from the group consisting of hydrogens, C1-6-alkyl, hydroxyl, alkoxyl acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino so long as X3 and Y3 are not both hydrogens.
- 20. A method of restoring the natural color of gray hair comprising applying to a scalp with gray hair either simultaneously or at different times:
(a) a vitamin D analog capable of binding a vitamin D receptor or being converted in vivo into a compound capable of binding a vitamin D receptor; and (b) a retinoid selected from the group consisting of retinoid D with an alcohol CH2OH terminal side chain, an ester of retinoid D having an ester bond, an ether of retinoid D having an ether bond, and retinoid D where the alcohol CH2OH terminal side chain is replaced with an aldehyde CHO terminal side chain, wherein each of the ester bond and the ether bond is formed with the oxygen at the terminal side chain of Retinoid D and wherein retinoid D with the alcohol CH2OH terminal side chain has the structure: 19wherein R1 is selected from the group consisting of 20wherein the keto group at the 4-position is free or protected, or is replaced by a thioketone group which is free or protected or is replaced by C1-6-alkylidene group; 21wherein X is selected from the group consisting of hydrogen and C1-6-alkyl and Y is selected from the group consisting of C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino and wherein the absolute configuration at the 4-position is independently R or S; 22wherein X1, Y1 are independently selected from the group consisting of hydrogen, C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino and Z1 is selected from the group consisting of C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino; 23wherein X2 is selected from the group consisting of hydrogen, C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino and Z2 is selected from the group consisting of C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino; and 24wherein X3 and Y3 are independently selected from the group consisting of hydrogens, C1-6-alkyl, hydroxyl, alkoxyl, acyloxyl, halide, azide, sulfhydryl, amine and C1-6-alkyl substituted amino so long as X3 and Y3 are not both hydrogens.
RELATED APPLICATIONS
[0001] This application is a continuation-in-part of U.S. Ser. No. 09/351,020, now allowed, which is a continuation-in-part of U.S. Ser. No. 09/116,632, filed Jul. 16, 1998.
Continuation in Parts (2)
|
Number |
Date |
Country |
Parent |
09351020 |
Jul 1999 |
US |
Child |
09872662 |
Jun 2001 |
US |
Parent |
09116632 |
Jul 1998 |
US |
Child |
09351020 |
Jul 1999 |
US |