NOVEL ANTI-INFLAMMATORY ANDROSTANE DERIVATIVES

• US 20070297989A1
• Filed: 09/06/2007
• Published: 12/27/2007
• Est. Priority Date: 04/30/2001
• Status: Abandoned Application

• Current Assignee: Jeremy Payne, Keith Biggadike, Paul Jones
• Original Assignee: Jeremy Payne, Keith Biggadike, Paul Jones
• Inventors: Jones, Paul, BIGGADIKE, KEITH, Payne, Jeremy
• Application Number:
  US11/851,125
• Publication Number:
  US 20070297989A1
• Time in Patent Office: Days
• US Class Current: 424/43
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/04 Antipruritics
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 27/14 Decongestants or antiallergics
• CPC Class Codes: A61P 27/16 Otologicals
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 5/44 Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
• CPC Class Codes: C07J 31/006 not covered by C07J31/003

Abstract

Novel anti-inflammatory androstane derivatives
There are provided compound of formula (I) wherein

• R₁ represents C_1-6 alkyl or C_1-6 haloalkyl;
• R₂ represents C_3-8 cycloalkyl or C_3-8 cycloalkenyl either of which may optionally be substituted by one or more groups selected from oxo, methyl, methylene and halogen;
• R₃ represents hydrogen, methyl (which may be in either the α or β configuration) or methylene;
• R₄ and R₅ are the same or different and each represents hydrogen or halogen; and represents a single or a double bond; and solvates thereof, processes for preparing them and their use in therapy.

Claims

1. A method for the treatment of a human or animal subject having an inflammatory and/or allergic condition, which method comprises administering to the human or animal subject an effective amount of a pharmaceutical composition comprising a compound 6α

,9α

-Difluoro-11β

-hydroxy-16α

-methyl-17α

-(1-methycyclopropylcarbonyl)oxy-3-oxo-androsta-1,4-diene-17β

-carbothioic acid S-fluoromethyl ester, in admixture with one or more physiologically acceptable diluents or carriers, wherein said effective amount is from 20 to 2000 micrograms of said compound.

2. The method of claim 1, wherein said administration occurs from 1 to 8 times per day.

3. The method of claim 2, wherein said administration occurs once per day.

4. The method of claim 1, wherein the inflammatory and/or allergic condition is rhinitis.

5. The method of claim 1, wherein said effective amount is from 20-500 micrograms of said compound.

6. The method of claim 1, wherein said pharmaceutical composition is an aqueous formulation, and said administration is made via aerosolization and is topically delivered to the nasal cavity.

7. The method of claim 6, wherein said composition comprises a buffering agent and/or a tonicity modifying agent.

8. The method of claim 1, wherein said composition further comprises an antihistamine as a further pharmaceutically active compound for the treatment of said condition.

9. A method for the treatment of a human or animal subject having an inflammatory and/or allergic condition, which method comprises:

administering to the nasal cavity of the human or animal subject, an aqueous aerosol pharmaceutical composition comprising an effective amount of a compound 6α

,9α

-Difluoro-11β

-hydroxy-16α

-methyl-17α

-(1-methycyclopropylcarbonyl)oxy-3-oxo-androsta-1,4-diene-17β

-carbothioic acid S-fluoromethyl or a solvate thereof, wherein said effective amount is from 20-2000 micrograms of said compound.

10. The method of claim 9, wherein said effective amount of said aqueous aerosol pharmaceutical composition is delivered from one to four times per day.

11. The method of claim 10, wherein said aqueous aerosol pharmaceutical composition is delivered once per day.