US2003162757A1PendingUtilityA1

Method of treating alopecia

Priority: Feb 21, 1996Filed: Feb 28, 2003Published: Aug 28, 2003
Est. expiryFeb 21, 2016(expired)· nominal 20-yr term from priority
A61K 31/4025A61Q 7/00A61K 8/46A61K 8/63A61K 8/41A61K 31/00A61Q 7/02A61P 17/14A61K 31/138A61P 17/00A61K 31/4535A61K 31/565A61K 8/42A61K 31/192
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Claims

Abstract

A method of enhancing hair growth or treating alopecia in a subject uses topically administered estrogen receptor antagonists. Pharmaceutical formulations comprising estrogen receptor antagonists are described.

Claims

exact text as granted — not AI-modified
That which is claimed is:  
     
         1 . A method of treating alopecia in a subject in need thereof comprising topically applying to the skin of said subject an estrogen receptor antagonist or a pharmaceutically acceptable salt thereof in an amount sufficient to treat alopecia.  
     
     
         2 . A method according to  claim 1 , wherein said estrogen receptor antagonist is a steroid  
     
     
         3 . A method according to  claim 1 , wherein said subject is a female subject.  
     
     
         4 . A method according to  claim 1 , wherein said subject is a male subject.  
     
     
         5 . A method according to  claim 1 , wherein said estrogen receptor antagonist is applied to the scalp of a subject.  
     
     
         6 . A method according to  claim 1 , wherein said skin contains telogen-phase hair follicles.  
     
     
         7 . A method according to  claim 1 , wherein said estrogen receptor antagonist is selected from the group consisting of 7α-alkylamide analogs and 11β-alkylamide analogs of estradiol.  
     
     
         8 . A method according to  claim 1 , wherein said estrogen receptor antagonist is selected from the group consisting of 7α-[9-(4,4,5,5,5,-pentafluoropentylsulfinyl)nonyl]estra-1,3,5(10)-triene-3,17β-diol, N-n-butyl-N-methyl-11-(3,17β-dihydroxyestra-1,3,5(10)-triene-7α-yl)undecanamide, 11β-[4-[2-(dimethylaminoethoxy]phenyl]-estradiol, N-methyl-N-isopropyl-(3,17β-dihydroxy-estra-1,2,5(10)-trien-11-β-yl)-undecamide, [6-hydroxy-2(4-hydroxyphenyl)benzo[b]thien-3-yl] [4-[3-(1-pyrrolidin-yl)ethoxy]phenyl]methanone, 3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic acid, tamoxifen, clomiphene, and keoxifene.  
     
     
         9 . A method according to  claim 1 , wherein said estrogen receptor antagonist is a compound of Formula 1:  
       
         
           
           
               
               
           
         
       
       wherein m is from 1 to 15; 
 n is from 1 to 5;  
 R 1  is hydrogen, lower alkyl, or halogen;  
 R 2  is oxygen or hydroxyl;  
 R 3  is lower alkyl or haloalkyl; and  
 X is  
                     
 wherein R 4  is loweralkyl,  
 or a pharmaceutically acceptable salt thereof.  
 
     
     
         10 . A method according to  claim 9 , wherein 
 m is 9;    n is 3;    R 1  is hydrogen;    R 2  is hydroxyl;    R 3  is haloalkyl; and    X is —SO—.    
     
     
         11 . A method according to  claim 10 , wherein R 3  is —CF 2 CF 3 .  
     
     
         12 . A method according to  claim 9 , wherein 
 m is 10;    n is 3;    R 1  is hydrogen;    R 2  is hydroxyl;    R 3  is lower alkyl;    X is                          R 4  is methyl.    
     
     
         13 . A method of promoting hair growth in a subject in need thereof comprising topically applying to the skin of said subject a compound selected from the group consisting of estrogen receptor antagonists and pharmaceutically acceptable salts thereof in an amount sufficient to promote hair growth.  
     
     
         14 . A method according to  claim 13 , wherein said subject is afflicted with hair loss, and said compound is administered in an amount effective to treat hair loss.  
     
     
         15 . A topical pharmaceutical formulation comprising an estrogen receptor antagonist or a pharmaceutically acceptable salt thereof in an amount effective to treat alopecia in a pharmaceutically acceptable topical carrier.  
     
     
         16 . A topical pharmaceutical formulation of  claim 15 , wherein said estrogen receptor antagonist is a steroid.  
     
     
         17 . A topical pharmaceutical formulation of  claim 15 , wherein said estrogen receptor antagonist is 7α-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]estra- 1,3,5(10)-triene-3,17β-diol.  
     
     
         18 . A topical pharmaceutical formulation of  claim 15 , wherein said formulation is a gel.  
     
     
         19 . A topical pharmaceutical formulation of  claim 15 , wherein said formulation is a spray.

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