US2017231966A1PendingUtilityA1

Inhibition of il-2 production

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Assignee: AYUMI PHARMACEUTICAL CORPPriority: Mar 22, 2013Filed: May 2, 2017Published: Aug 17, 2017
Est. expiryMar 22, 2033(~6.7 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 37/08A61P 37/00A61P 37/06A61P 29/00A61P 35/00A61P 27/02A61P 31/18A61P 17/04A61P 11/06A61P 19/02G01N 33/6869A61P 1/00A61K 31/428A61P 11/00A61P 17/00A61P 17/06C07D 277/66A61P 25/00A61P 21/04A61P 11/08C07K 16/246A61P 11/02A61P 13/12
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Claims

Abstract

An object is to find a substance which inhibits IL-2 production. IL-2 production can be inhibited by a compound represented by the following formula (I): wherein R 1 to R 4 and A are as defined in the present specification, or a pharmaceutically acceptable salt thereof.

Claims

exact text as granted — not AI-modified
1 .- 15 . (canceled) 
     
     
         16 . A method for treatment of a disease selected from the group consisting of rheumatoid arthritis, psoriasis, lupus nephritis, and psoriatic arthritis, the method comprising
 (i) administering to a subject in need thereof an effective amount of a compound represented by the formula (I):   
       
         
           
           
               
               
           
         
          wherein 
          A represents a lower alkylene group; 
          R 1  represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkyl group substituted by a halogen atom; 
          R 2  represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and 
          R 3  and R 4  each may be the same or different from each other and represent a hydrogen atom, a lower alkyl group, a lower alkyl group substituted by a hydroxyl group, a lower alkyl group substituted by a lower alkoxy group, a lower alkyl group substituted by a lower alkoxy group which is substituted by a lower alkoxy group or a lower alkyl group substituted by an acetoxy group, or a pharmaceutically acceptable salt thereof, and 
         (ii) inhibiting IL-2 production in the subject. 
       
     
     
         17 . The method according to  claim 16 , wherein the compound represented by the formula (I) is a compound wherein
 A represents a lower alkylene group;   R 1  represents a halogen atom;   R 2  represents a lower alkoxy group;   R 3  represents a lower alkyl group; and   R 4  represents a lower alkyl group substituted by a hydroxyl group, a lower alkyl group substituted by a lower alkoxy group, a lower alkyl group substituted by a lower alkoxy group which is substituted by a lower alkoxy group or a lower alkyl group substituted by an acetoxy group.   
     
     
         18 . The method according to  claim 16 , wherein the compound represented by the formula (I) is a compound where
 A represents trimethylene group or 1-methyltrimethylene group;   R 1  represents chlorine atom;   R 2  represents methoxy group;   R 3  represents isopropyl group; and   R 4  represents 2-hydroxyethyl group, 2-methoxyethyl group, 2-ethoxyethyl group, 2-(methoxymethoxy)ethyl group or 2-acetoxyethyl group.   
     
     
         19 . The method according to  claim 16 , wherein the compound represented by the formula (I) is (+)-3-acetyl-6-chloro-2-[2-(3-(N-(2-ethoxyethyl)-N-isopropylamino)propoxy)-5-methoxyphenyl]benzothiazoline, (±)-3-acetyl-6-chloro-2-[2-(3-(N-(2-ethoxyethyl)-N-isopropylamino)propoxy)-5-methoxyphenyl]benzothiazoline, (+)-3-acetyl-6-chloro-2-[2-(3-(N-(2-hydroxyethyl)-N-isopropylamino)propoxy)-5-methoxyphenyl]benzothiazoline or (+)-3-acetyl-6-chloro-2-[2-(3-(N-isopropyl-N-(2-methoxyethyl)amino)propoxy)-5-methoxyphenyl]benzothiazoline. 
     
     
         20 . The method of any one of  claims 16  to  19 , wherein the pharmaceutically acceptable salt of the compound represented by the formula (I) is a (−)-O,O′-diacetyl-L-tartaric acid salt or a hydrochloric acid salt.

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