US2008306123A1PendingUtilityA1

Novel compounds

56
Assignee: PFIZERPriority: Jun 17, 2003Filed: May 21, 2008Published: Dec 11, 2008
Est. expiryJun 17, 2023(expired)· nominal 20-yr term from priority
A61P 3/04A61P 43/00A61P 25/18A61P 25/22A61P 25/14A61P 25/20A61P 25/24A61P 25/36A61P 25/04A61P 29/00A61P 25/00A61P 25/06A61P 25/16A61P 25/28A61P 13/00A61P 15/00A61P 15/10C07D 207/14A61K 31/40
56
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Claims

Abstract

A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R 1 is H, C 1-6 alkyl, —C(X)Y, C 3-8 cycloalkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C 1-8 alkyl, C 1-8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S—C 1-4 alkyl; R 2 is aryl or heteroaryl, each optionally substituted by at least one substituent independently selected from C 1-8 alkyl, C 1-8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S—C 1-4 alkyl; R 3 is C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-6 alkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C 1-6 alkyl, C 1-6 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S—C 1-4 alkyl; X is S or O; Y is H, C 1-6 alkyl, aryl, het, aryl-C 1-4 alkyl or het-C 1-4 alkyl; and n is 1 or 2, provided that when n is 1, m is 0 or 1 and when n is 2, m is 0, wherein if m is 0, then * represents a chiral center. The compounds of the invention exhibit activity as both serotonin and noradrenaline re-uptake inhibitors and therefore have utility in a variety of therapeutic areas, for example urinary incontinence.

Claims

exact text as granted — not AI-modified
1 .- 15 . (canceled) 
   
   
       16 . A method of treating urinary disorders, depression, pain, premature ejaculation, ADHD or fibromyalgia, which comprises administering a therapeutically effective amount of a compound of Formula (I) 
     
       
         
         
             
             
         
       
     
     and the pharmaceutically and/or veterinarily acceptable salts thereof, wherein R 1  is H;
 R 2  is phenyl, naphthyl or quinolinyl, each optionally substituted by at least one substituent independently selected from C 1-8 alkyl, C 1-8 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S—C 1-4 alkyl; 
 R 3  is C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl-C 1-6 alkyl, aryl, het aryl-C 1-4 alkyl or het-C 1-4 alkyl, wherein the cycloalkyl, aryl or het groups are optionally substituted by at least one substituent independently selected from C 1-6 alkyl, C 1-6 alkoxy, OH, halo, CF 3 , OCF 3 , SCF 3 , hydroxy-C 1-6 alkyl, C 1-4 alkoxy-C 1-6 alkyl and C 1-4 alkyl-S—C 1-4 alkyl; 
 n is 1, and m is 0, wherein * represents a chiral centre; 
 aryl is phenyl, naphthyl, anthracyl or phenanthryl; and 
 het is an aromatic or non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom, optionally fused to a 5- or 6-membered carbocyclic group or a second 4-, 5- or 6-membered heterocycle which contains at least one N, O or S heteroatom to a patient in need of such treatment. 
 
   
   
       17 . A method of  claim 16 , wherein the urinary disorder is urinary incontinence. 
   
   
       18 . (canceled)

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