US2017327474A1PendingUtilityA1

Therapeutic agent for pain

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Assignee: ASTELLAS PHARMA INCPriority: Sep 7, 2010Filed: Jul 31, 2017Published: Nov 16, 2017
Est. expirySep 7, 2030(~4.2 yrs left)· nominal 20-yr term from priority
A61P 25/04A61P 29/00A61P 21/00A61P 25/00C07D 249/08A61K 31/4196C07D 403/04A61K 31/4245C07D 413/12
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Claims

Abstract

[Problem] Provided is a pharmaceutical, in particular, a pharmaceutical composition which is useful for the treatment of pain. [Means for Solution] The present inventors have made extensive studies using model animals with pain for the purpose of providing a therapeutic agent for pain. As a result, they have found that 11β-hydroxydehydrogenase type 1 (11β-HSD1) inhibitor, in particular, a triazole compound having a cyclic group at the 3-position (or 5-position) of a triazole ring has a good effect of ameliorating chronic pain. That is, according to the present invention, a pharmaceutical composition comprising an 11β-HSD1 inhibitor, in particular, the triazole compound of the present invention, as an active ingredient, is useful for the treatment of pain (particularly, neuropathic pain or fibromyalgia).

Claims

exact text as granted — not AI-modified
1 . (canceled) 
     
     
         2 . A method for treating fibromyalgia, comprising administering, to a subject in need thereof, an effective amount of a compound selected from the group consisting of:
 3-(2-chloro-4-fluorophenyl)-4-methyl-5-[1-methyl-1-(2,4,6-trifluorophenoxy)ethyl]-4H-1,2,4-triazole,   3-[1-(4-chloro-2,6-difluorophenoxy)-1-methylethyl]-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole,   4-{5-[1-(4-chloro-2,6-difluorophenoxy)-1-methylethyl]-4-ethyl-4H-1,2,4-triazol-3-yl}benzamide,   4-{5-[1-(4-chloro-2,6-difluorophenoxy)-1-methylethyl]-4-methyl-4H-1,2,4-triazol-3-yl}-3-fluorobenzamide,   4-{4-cyclopropyl-5-[1-(2,4-difluorophenoxy)-1-methylethyl]-4H-1,2,4-triazol-3-yl}-3-fluorobenzamide, and   3-fluoro-4-{4-isopropyl-5-[1-methyl-1-(2,4,6-trifluorophenoxy)ethyl]-4H-1,2,4-triazol-3-yl}benzamide, or   a pharmaceutically acceptable salt thereof.   
     
     
         3 . The method according to  claim 2 , wherein said compound is 3-(2-chloro-4-fluorophenyl)-4-methyl-5-[1-methyl-1-(2,4,6-trifluorophenoxy)ethyl]-4H-1,2,4-triazole or a pharmaceutically acceptable salt thereof. 
     
     
         4 . The method according to  claim 2 , wherein said compound is 3-[1-(4-chloro-2,6-difluorophenoxy)-1-methylethyl]-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole or a pharmaceutically acceptable salt thereof. 
     
     
         5 . The method according to  claim 2 , wherein said compound is 4-{5-[1-(4-chloro-2,6-difluorophenoxy)-1-methylethyl]-4-ethyl-4H-1,2,4-triazol-3-yl}benzamide or a pharmaceutically acceptable salt thereof. 
     
     
         6 . The method according to  claim 2 , wherein said compound is 4-{5-[1-(4-chloro-2,6-difluorophenoxy)-1-methylethyl]-4-methyl-4H-1,2,4-triazol-3-yl-3-fluorobenzamide or a pharmaceutically acceptable salt thereof. 
     
     
         7 . The method according to  claim 2 , wherein said compound is 4-4-cyclopropyl-5-[1-(2,4-difluorophenoxy)-1-methylethyl]-4H-1,2,4-triazol-3-yl}-3-fluorobenzamide or a pharmaceutically acceptable salt thereof. 
     
     
         8 . The method according to  claim 2 , wherein said compound is 3-fluoro-4-{4-isopropyl-5-[1-methyl-1-(2,4,6-trifluorophenoxy)ethyl]-4H-1,2,4-triazol-3-yl}benzamide or a pharmaceutically acceptable salt thereof.

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