WO2003009820B1

WO2003009820B1 - Methods for promotion of hair growth comprising topical application of prostaglandin analogues

Info

Publication number: WO2003009820B1
Application number: PCT/US2002/023584
Authority: WO
Inventors: Gerald D Cagle; Michael V W Bergamini
Original assignee: Alcon Inc; Gerald D Cagle; Michael V W Bergamini
Priority date: 2001-07-25
Filing date: 2002-07-25
Publication date: 2003-11-13
Also published as: WO2003009820A2; WO2003009820A3; CA2449462A1; MXPA04000712A; JP2004538288A; EP1408913A2

Abstract

Methods for the promotion of hair growth in mammals, comprising the topical application of PGF2a or tetrahydro-furanyl prostaglandin analogues in specific concentrations are disclosed.

Claims

34AMENDED CLAIMS[received by the Internationa Bureau on 07 April 2003 (07.04.03); claim 1 replaced by new claim 1; original claims 3 and 8 cancelled; remaining claims unchanged (3 pages)]

1. A method far promoting hair growth in a mammal, comprising the topical application to mammalian skin of an effective amount of a PGF_2α analogue selected from the group consisting of:

acid forms of the foregoing, together with their pharmaceutically acceptable salts, esters and amides; and

compounds of formula IV:

wherein:

Ri = OR, where R = H; C Cι₂ straight-chain or branched alkyl; C₁-C₁₂ straight-chain or branched acyl; C₃-Cs cycloalkyl; or a cationic salt moiety; or R = NR R^δ, where R⁴ and R⁵ are the same or different and are H; C1-C12 straight-chain or branched alkyl; C C₁₂ straight- chain or branched acyl; or C₃-Cs cycloalkyl;

R2, 3 = H, or C1-C5 straight-chain or branched alkyl; or R₂ and R₃ taken together may represent O; 35

X = O, S, or CH₂;

-_— represents any combination of a single bond, or a cis or trans double bond for the alpha (upper) chain; and a single bond or trans double bond for the omega (lower) chain; 9 = H, C1-C-10 straight-chain or branched alkyl, or C1-C10 straight-chain or branched acyl; R-n = H, C₁-C₁₀ straight-chain or branched alkyl, or C₁-C₁₀ straight-chain or branched acyl; Y = O; or H and OR₁₅ in either configuration wherein R15 = H, Cι-C₁₀ straight-chain or branched alkyl, or C1-C₁0 straight-chain or branched acyl; and Z = Cl or CF₃;

with the proviso that the following compounds are excluded: cioprostenol, fluprostenol, travoprost, and 13,14-dihydro-16-((3- trifluoromethyl)ρheπoxy)-16-tetranor prostaglandin Fι_α; and salts, esters, and amides thereof.

2. The method of claim 1 , wherein the PGF_2α analogue is a compound of formula IV having the structure of formula V:

wherein:

R¹ = OR or NR³R⁴,where

R = H, a cationic salt moiety, a pharmaceutically acceptable amine moiety, or CrCi2 alkyl, cycloalkyl, or aryl;

R³ and R⁴ = same or different - H, alkyl, cycloalkyl, aryl, or OR⁵, with the proviso that R³ and R⁴ cannot both = OR⁵, where

R⁶ - H, alkyl, acyl, cycloalkyl, or aryl; and

R² = Cl or CF₃.

3. [cancelled]

4. The method of claim 1 , wherein the PGF_aα analogue is applied in a composition comprising from about 0.0000001% to about 50% by weight of said PGF_aoι analogue.

5. The method of claim 4, wherein the composition comprises from about 0.0001 % to about 5% by weight ofthe PGF_2ft analogue.

6. The method of claim 5, wherein the composition comprises from about 0.0001% to about 0,1% by weight ofthe PGF_2α analogue.

7. The method of claim 2, wherein the PGF_2α analogue is applied in a composition having a concentration from about 0.0001% to about 0,1% by weight of the PGp2_α analogue.

8. [cancelled]