Method of Treating Fibromyalgia or Associated Functional Symptoms of Fibromyalgia

Abstract

The invention relates to a method of treating fibromyalgia or associated functional symptoms of fibromyalgia using a 1-acylpiperidine substance P antagonist, the 1-acylpiperidine substance P antagonist comprising a compound of formula wherein X and Y are each independent of the other N and/or CH, and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl and for each compound, pharmaceutically-acceptable salts thereof.

1 . A method of treating fibromyalgia or associated functional symptoms of fibromyalgia comprising administering to a patient in need thereof, a 1-acylpiperidine substance P antagonist, the 1-acylpiperidine substance P antagonist comprising a compound of formula 
     
       
         
         
             
             
         
       
       wherein X and Y are each independent of the other N and/or CH, and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl and for each compound, pharmaceutically-acceptable salts thereof. 
     
   
   
       2 . The method of treatment according to  claim 1 , in which the compound is selected from the group consisting of
 (2R,4S)-N-[1-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-piperidin-4-yl]-quinoline-4-carboxamide; (2R,4S)-N-[1-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-piperidin-4-yl]-quinazoline-4-carboxamide; (2R,4S)-N-[1-(3,5-bis-trifluoromethyl-benzoyl)-2-(4-chloro-benzyl)-piperidin-4-yl]-quinoline-4-carboxamide; (2R,4S)-N-[1-(3,5-bis-trifluoromethyl-benzoyl)-2-(4-chloro-benzyl)-piperidinyl]-quinazoline-4-carboxamide; (2R,4S)-N-[1-(3,5-bis-trifluoromethyl-benzoyl)-2-(4-chloro-benzyl)-piperidinyl]-isoquinoline-1-carboxamide; and (2R,4S)-N-[1-(3,5-bis-trifluoromethyl-benzoyl)-2-(4-nitro-benzyl)-piperidinyl]-quinazoline-4-carboxamide and for each compound, salts thereof.   
   
   
       3 . The method of treatment according to  claim 2  in which such compound is (2R,4S)-N-[1-(3,5-bis-trifluoromethyl-benzoyl)-2-(4-chloro-benzyl)-piperidin-4-yl]-quinoline-4-carboxamide. 
   
   
       4 . The method of treatment according to  claim 1  comprising administering such compound to such patient at a dose of about 1 to about 40 mg/kg per day. 
   
   
       5 . The method of treatment according to  claim 4  comprising administering such compound to such patient at a dose of about 10 to about 20 mg/kg per day. 
   
   
       6 . The method of treatment according to  claim 1  comprising administering such compound to such patient orally. 
   
   
       7 . The method of treatment according to  claim 6  comprising administering such compound to such patient in the form of a tablet or a gelatin capsule. 
   
   
       8 . The method of treatment according to  claim 2  comprising administering such compound to such patient at a dose of about 1 to about 40 mg/kg per day. 
   
   
       9 . The method of treatment according to  claim 8  comprising administering such compound to such patient at a dose of about 10 to about 20 mg/kg per day. 
   
   
       10 . The method of treatment according to  claim 2  comprising administering such compound to such patient orally. 
   
   
       11 . The method of treatment according to  claim 10  comprising administering such compound to such patient in the form of a tablet or a gelatin capsule. 
   
   
       12 . The method of treatment according to  claim 3  comprising administering such compound to such patient at a dose of about 1 to about 40 mg/kg per day. 
   
   
       13 . The method of treatment according to  claim 12  comprising administering such compound to such patient at a dose of about 10 to about 20 mg/kg per day. 
   
   
       14 . The method of treatment according to  claim 3  comprising administering such compound to such patient orally. 
   
   
       15 . The method of treatment according to  claim 14  comprising administering such compound to such patient in the form of a tablet or a gelatin capsule. 
   
   
       16 . A method of treating fibromyalgia or associated functional symptoms of fibromyalgia comprising: administering to a patient in need thereof a compound selected from the group consisting of (2R,4S)-N-[1-(3,5-bisfluoromethyl-benzoyl)-2-(4-chlorobenzyl)-piperidin-4-yl]-4-oxo-4H-1-benzopyran-2-carboxamide; (2R,4S)-N-[1-(3,5-bisfluoromethyl-benzoyl)-2-benzyl-piperidin-4-yl]-4-oxo-4H-1-benzopyran-2-carboxamide; and (2R,4S)-N-[1-(3,5-bisfluoromethyl-benzoyl)-2-(4-chlorobenzyl)-piperidin-4-yl]-6-fluoro-4-oxo-4H-1-benzopyran-2-carboxamide, and pharmaceutically-acceptable salts thereof. 
   
   
       17 . The method of treatment according to  claim 16  comprising administering such compound to such patient at a dose of about 1 to about 40 mg/kg per day. 
   
   
       18 . The method of treatment according to  claim 17  comprising administering such compound to such patient at a dose of about 10 to about 20 mg/kg per day. 
   
   
       19 . The method of treatment according to  claim 16  comprising administering such compound to such patient orally. 
   
   
       20 . The method of treatment according to  claim 19  comprising administering such compound to such patient in the form of a tablet or a gelatin capsule.