Cyclosporin derivatives for enhancing the growth of hair
AssigneeAllergan, Inc.
InventorsDavid F. Woodward, Michael E. Garst
Life of this patent
Estimating the term…
Abstract
The present invention provides a method for the treatment of alopecia and/or enhancing hair growth in a patient, wherein said method comprises administering, preferably topically, to the skin, e.g. the scalp or the eyelid, a therapeutically effective amount of a cyclosporin A derivative selected from the group consisting of compounds represented by the formula: wherein R1 is S-Alk-R wherein Alk is an alkylene or alkylenyl linkage, R is a hydrogen or a unsubstituted or substituted hydrocarbyl group and R2 is selected from the group consisting of hydroxyl, lower alkyl and hydroxyl substituted lower alkyl.
Claims22
A method for the treatment of alopecia in a patient, said method comprising administering, topically to the scalp of the patient, a therapeutically effective amount of a cyclosporine A derivative represented by the following formula:
- wherein R1 is S-Alk-R wherein Alk is an alkylene or alkylenyl linkage, R is a hydrogen or a unsubstituted or substituted hydrocarbyl group and R2 is selected from the group consisting of hydroxyl, lower alkyl and hydroxyl substituted lower alkyl.
A method for stimulating hair growth in a mammalian species comprising applying to mammalian skin an effective amount of a cyclosporine derivative represented by the following formula:
- wherein R1 is S-Alk-R wherein Alk is an alkylene or alkylenyl linkage, R is a hydrogen or a unsubstituted or substituted hydrocarbyl group and R2 is selected from the group consisting of hydroxy and lower alkyl.
A method for converting vellus hair or intermediate hair to terminal hair comprising applying to mammalian skin at the locale of vellus hair an effective amount of a cyclosporine compound represented by the following formula:
- wherein R1 is S-Alk-R wherein Alk is an alkylene or alkylenyl linkage, R is a hydrogen or a unsubstituted or substituted hydrocarbyl group and R2 is selected from the group consisting of hydroxy and lower alkyl.
A method of increasing one or more of length, thickness, number, and density, of eyelash hair or eyebrow hair, comprising administering an effective amount of a compound of the following formula:
- wherein R1 is S-Alk-R wherein Alk is an alkylene or alkylenyl linkage, R is a hydrogen or a unsubstituted or substituted hydrocarbyl group and R2 is selected from the group consisting of hydroxyl and lower alkyl to a person on the area where hair growth is desired.
A method for stimulating hair growth in a mammalian species comprising the application to mammalian skin of an effective amount of a cyclosporine derivative represented by the following formula:
- R1 is a hydrogen atom or a radical of formula (Ia):
- —S-Alk-R11 (Ia)
- in which
- Alk-R11 represents a methyl radical, or alternatively
- Alk represents a C2-C6 straight chain or branched alkylene radical or a C3-C6 cycloalkylene radical, and
- R11. represents
- a hydrogen atom or a hydroxyl, carboxyl or alkyloxycarbonyl radical, or
- an —NR12R13 radical in which R12 and R13, which are identical or different, represent a hydrogen atom or a phenyl, alkyl, C2-C4 alkenyl or C3-C6 cycloalkyl radical, said radical optionally substituted with selected from a halogen atom, an alkyloxy, alkyloxycarbonyl, amino, alkylamino and dialkylamino radical;
- or
- R12 and R13 represent a benzyl or saturated or unsaturated heterocycylic radical, said heterocycylic radical containing from 5 to 6 ring members and from 1 to 3 heteroatoms;
- or in which R12 and R13 form, together with the nitrogen atom to which they are attached, a saturated or unsaturated 4- to 6-membered heterocycle, which heterocycle having an additional heteroatom selected from nitrogen, oxygen and sulphur, and wherein said saturated or unsaturated heterocycle is optionally substituted by an alkyl, phenyl or benzyl radical, or R1 is a radical of the formula (Ib):
- —N(R14)—(CH2)n—NR12R13 in which R12 and R13 are as defined above, R14 represents a hydrogen atom or an alkyl radical and n is an integer ranging from 2 to 4,
- and R2 is selected from the group consisting of hydroxyl, lower alkyl and hydroxyl substituted lower alkyl,
- with the proviso that, when R1 is a hydrogen atom, then R2 is not an alkyl radical, and wherein the alkyl portions or radicals defined above are straight chain or branched and contain from 1 to 4 carbon atoms, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.