US2010152148A1PendingUtilityA1

Novel compounds

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Assignee: BIGGADIKE KEITHPriority: Jul 11, 2003Filed: Mar 1, 2010Published: Jun 17, 2010
Est. expiryJul 11, 2023(expired)· nominal 20-yr term from priority
A61P 5/44A61P 37/08A61P 3/04A61P 43/00A61P 37/00A61P 5/00A61P 27/16A61P 27/02A61P 29/00A61P 17/06A61P 11/00A61P 19/00A61P 11/04A61P 17/00A61P 11/02A61P 17/04A61P 11/06A61P 1/00C07J 1/0011C07D 233/54C07D 451/02C07J 3/00C07D 215/26A61K 31/56
52
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Claims

Abstract

A compound of formula (I): wherein X represents O or S; R 1 represents C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylmethyl or C 3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl groups or halogen atoms or R 1 represents aryl, substituted aryl, heteroaryl or substituted heteroaryl; R 2 represents hydrogen, methyl, which may be in either the α or β configuration, or methylene; R 3 and R 4 are the same or different and each independently represents hydrogen, halogen or a methyl group; and represents a single or a double bond; or a physiologically acceptable salt or solvate thereof, and pharmaceutical formulations and methods of use thereof.

Claims

exact text as granted — not AI-modified
1 . A method of treatment of a human subject with skin disease, an inflammatory bowel condition, an auto-immune disease, conjunctivitis, nasal polyps, chronic obstructive pulmonary disease, interstitial lung disease or fibrosis, which method comprises administering to said human an effective amount of 6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-(2,2,3,3-tetramethylcyclopropylcarbonyl)oxy-androsta-1,4-diene-17β-carboxylic acid cyanomethyl ester or a physiologically acceptable solvate thereof. 
   
   
       2 . The method of  claim 1 , wherein the skin disease is selected from the group consisting of eczema, psoriasis, allergic dermatitis, neurodermatitis, pruritis and hypersensitivity reactions. 
   
   
       3 . The method of  claim 2 , wherein the skin disease is allergic dermatitis. 
   
   
       4 . The method of  claim 1 , wherein the inflammatory bowel condition is ulcerative colitis or Crohn's disease. 
   
   
       5 . The method of  claim 1 , wherein the auto-immune disease is rheumatoid arthritis. 
   
   
       6 . The method of  claim 1 , wherein the step administering to said human an effective amount of 6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-(2,2,3,3-tetramethylcyclopropylcarbonyl)oxy-androsta-1,4-diene-17β-carboxylic acid cyanomethyl ester or a physiologically acceptable solvate thereof, is via oral, buccal, sublingual, parenteral, local or rectal administration. 
   
   
       7 . The method of any one of  claim 2 , wherein the step administering to said human an effective amount of 6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-(2,2,3,3-tetramethylcyclopropylcarbonyl)oxy-androsta-1,4-diene-17β-carboxylic acid cyanomethyl ester or a physiologically acceptable solvate thereof, is via oral, buccal, sublingual, parenteral, local or rectal administration. 
   
   
       8 . The method of  claim 3 , wherein the step administering to said human an effective amount of 6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-(2,2,3,3-tetramethylcyclopropylcarbonyl)oxy-androsta-1,4-diene-17β-carboxylic acid cyanomethyl ester or a physiologically acceptable solvate thereof, is via oral, buccal, sublingual, parenteral, local or rectal administration. 
   
   
       9 . The method of  claim 4 , wherein the step administering to said human an effective amount of 6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-(2,2,3,3-tetramethylcyclopropylcarbonyl)oxy-androsta-1,4-diene-17β-carboxylic acid cyanomethyl ester or a physiologically acceptable solvate thereof, is via oral, buccal, sublingual, parenteral, local or rectal administration. 
   
   
       10 . The method of  claim 5 , wherein the step administering to said human an effective amount of 6α,9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-(2,2,3,3-tetramethylcyclopropylcarbonyl)oxy-androsta-1,4-diene-17β-carboxylic acid cyanomethyl ester or a physiologically acceptable solvate thereof, is via oral, buccal, sublingual, parenteral, local or rectal administration.

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