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Claims for Patent: 8,101,161

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Claims for Patent: 8,101,161

Title:Method of enhancing hair growth
Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I ##STR00001## wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R.sub.1 and R.sub.2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal. Bimatoprost is preferred for this treatment.
Inventor(s): Woodward; David F. (Lake Forest, CA), VanDenburgh; Amanda M. (Huntington Beach, CA)
Assignee: Allergan, Inc. (Irvine, CA)
Application Number:11/805,122
Patent Claims: 1. A method for the conversion of vellus hair or intermediate hair to growth as terminal hair comprising the application to mammalian skin at the locale of vellus hair of a composition comprising a carrier and an effective amount of a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula; ##STR00010## wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to six carbon atoms, which radical may be interrupted by one or more oxa radicals and substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups wherein said alkyl radical comprises from one to six carbon atoms; B is a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals having from four to ten carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms; X is --N(R.sup.4).sub.2 wherein each R.sup.4 is independently selected from the group consisting of hydrogen, a lower alkyl radical having from one to six carbon atoms, ##STR00011## wherein R.sup.5 is a lower alkyl radical having from one to six carbon atoms; Z is .dbd.O, one of R.sub.1 and R.sub.2 is .dbd.O, --OH or a --O(CO)R.sub.6 group, and the other one is --OH or --O(CO)R.sub.6, or R.sub.1 is .dbd.O and R.sub.2 is H, wherein R.sub.6 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2)mR.sub.7 wherein m is 0 or an integer of from 1 to 10, and R.sub.7 is cycloalkyl radical, having from three to seven carbon atoms, or a hydrocarbyl aryl or heteroaryl radical, as defined above or a pharmacologically acceptable acid addition salt thereof.

2. The method of claim 1 wherein the concentration of the compound applied is from about 0.0000001% to about 50% by weight of the composition.

3. The method of claim 1 wherein the compound is represented by the formula: ##STR00012## wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, Y is a radical selected from the group consisting of alkyl, halo, nitro, amino, thiol, hydroxyl, alkyloxy, alkycarboxy, halo substituted alkyl wherein said alky radical comprises from one to six carbon atoms, n is 0 or an integer of from 1 to about 3 and R.sub.3 is .dbd.O, --OH or --O(CO)R.sub.6, hatched lines indicate .alpha. configuration and solid triangles are used to indicate .beta. configuration.

4. The method of claim 3 wherein the compound applied is bimatoprost.

5. The method of claim 1 wherein the concentration of the compound applied is from about 0.1% to about 30% by weight of the composition.

6. The method of claim 4 wherein the concentration of the compound applied is 0.03% by weight of the composition.

7. The method of claim 1 wherein the concentration of the compound applied is about 0.1% by weight of the composition.

8. The method of claim 4 wherein the concentration of the compound applied is 5% by weight of the composition.

9. A method for stimulating hair growth in a mammalian species comprising the application to mammalian skin of an effective amount of a composition comprising a carrier and cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I ##STR00013## wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to six carbon atoms, which radical may be interrupted by one or more oxa radicals and substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups wherein said alkyl radical comprises from one to six carbon atoms; B is a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals having from four to ten carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms; X is --N(R.sup.4).sub.2 wherein each R.sup.4 is independently selected from the group consisting of hydrogen, a lower alkyl radical having from one to six carbon atoms, ##STR00014## wherein R.sup.5 is a lower alkyl radical having from one to six carbon atoms; Z is .dbd.O; one of R.sub.1 and R.sub.2 is .dbd.O, --OH or a --O(CO)R.sub.6 group, and the other one is --OH or --O(CO)R.sub.6, or R.sub.1 is .dbd.O and R.sub.2 is H, wherein R.sub.6 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2)mR.sub.7 wherein m is 0 or an integer of from 1 to 10, and R.sub.7 is cycloalkyl radical, having from three to seven carbon atoms, or a hydrocarbyl aryl or heteroaryl radical, as defined above or a pharmacologically acceptable acid addition salt thereof, wherein the concentration of the compound applied is from about 0.1% to about 30% by weight of the composition.

10. The method of claim 9 wherein the compound is bimatoprost.

11. The method of claim 10 wherein the concentration of the compound applied is from 0.03% by weight of the composition.

12. The method of claim 10 wherein the concentration of the compound applied is 5% by weight of the composition.

13. A method for stimulating hair follicles to increase hair growth and one or more properties selected from the group consisting of luster, sheen, brilliance, gloss, glow, shine or patina of hair associated with the follicles, comprising the application to mammalian skin at the locale of the follicles of an effective amount of a composition comprising a carrier and cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I ##STR00015## wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to six carbon atoms, which radical may be interrupted by one or more oxide radicals and substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups wherein said alkyl radical comprises from one to six carbon atoms; B is a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals having from four to ten carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms; X is --N(R.sup.4).sub.2 wherein each R.sup.4 is independently selected from the group consisting of hydrogen, a lower alkyl radical having from one to six carbon atoms, ##STR00016## wherein R.sup.5 is a lower alkyl radical having from one to six carbon atoms; Z is .dbd.O; one of R.sub.1 and R.sub.2 is .dbd.O, --OH or a --O(CO)R.sub.6 group, and the other one is --OH or --O(CO)R.sub.6, or R.sub.1 is .dbd.O and R.sub.2 is H, wherein R.sub.6 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2)mR.sub.7 wherein m is 0 or an integer of from 1 to 10, and R.sub.7 is cycloalkyl radical, having from three to seven carbon atoms, or a hydrocarbyl aryl or heteroaryl radical, as defined above or a pharmacologically acceptable acid addition salt thereof wherein the concentration of the compound applied is from about 0.1% to about 30% by weight of the composition.

14. The method of claim 13 wherein the compound is bimatoprost.

15. The method of claim 14 wherein the concentration of the compound applied is from 0.03% by weight of the composition.

16. The method of claim 14 wherein the concentration of the compound applied is 5% by weight of the composition.

17. A method for increasing the number of hairs in a mammalian species comprising the topical application to mammalian skin of a composition comprising a carrier and an effective amount of a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I ##STR00017## wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to six carbon atoms, which radical may be interrupted by one or more oxa radicals and substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups wherein said alkyl radical comprises from one to six carbon atoms; B is a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals having from four to ten carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms; X is --N(R.sup.4).sub.2 wherein each R.sup.4 is independently selected from the group consisting of hydrogen, a lower alkyl radical having from one to six carbon atoms, ##STR00018## wherein R.sup.5 is a lower alkyl radical having from one to six carbon atoms; Z is .dbd.O; one of R.sub.1 and R.sub.2 is .dbd.O, --OH or a --O(CO)R.sub.6 group, and the other one is --OH or --O(CO)R.sub.6, or R.sub.1 is .dbd.O and R.sub.2 is H, wherein R.sub.6 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2)mR.sub.7 wherein m is 0 or an integer of from 1 to 10, and R.sub.7 is cycloalkyl radical, having from three to seven carbon atoms, or a hydrocarbyl aryl or heteroaryl radical, as defined above or a pharmacologically acceptable acid addition salt thereof, wherein the concentration of the compound applied is from about 0.1% to about 30% by weight of the composition, wherein said application provides an effective amount from 0.1 ng to 100 mg of compound per day.

18. The method of claim 17 wherein the compound is bimatoprost.

19. The method of claim 18 wherein said application provides an effective amount from 1 ng to 1 mg of the compound per day.

20. The method of claim 19 wherein said application provides an effective amount from 10 ng to 10 mg of the compound per day.

21. A method for stimulating hair follicles to increase hair growth and one or more properties selected from the group consisting of luster, sheen, brilliance, gloss, glow, shine or patina of hair associated with the follicles, comprising the application to mammalian skin of a composition comprising a carrier at the locale of the follicles of an effective amount of a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I ##STR00019## wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to six carbon atoms, which radical may be interrupted by one or more oxide radicals and substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups wherein said alkyl radical comprises from one to six carbon atoms; B is a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals having from four to ten carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms; X is --N(R.sup.4).sub.2 wherein each R.sup.4 is independently selected from the group consisting of hydrogen, a lower alkyl radical having from one to six carbon atoms, ##STR00020## wherein R.sup.5 is a lower alkyl radical having from one to six carbon atoms; Z is .dbd.O; one of R.sub.1 and R.sub.2 is .dbd.O, --OH or a --O(CO)R.sub.6 group, and the other one is --OH or --O(CO)R.sub.6, or R.sub.1 is .dbd.O and R.sub.2 is H, wherein R.sub.6 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or --(CH.sub.2)mR.sub.7 wherein m is 0 or an integer of from 1 to 10, and R.sub.7 is cycloalkyl radical, having from three to seven carbon atoms, or a hydrocarbyl aryl or heteroaryl radical, as defined above or a pharmacologically acceptable acid addition salt thereof, wherein the concentration of the compound applied is from about 0.1% to about 30% by weight of the composition, wherein said application provides an effective amount from 0.1 ng to 100 mg of compound per day.

22. The method of claim 21 wherein said compound is bimatoprost.

23. The method of claim 22 wherein said application provides an effective amount from 1 ng to 1 mg of the compound per day.

24. The method of claim 23 wherein said application provides an effective amount from 10 ng to 10 mg of the compound per day.
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