US2021340114A1PendingUtilityA1

Heterocyclic compound

Assignee: TAKEDA PHARMACEUTICALS COPriority: Oct 24, 2014Filed: Apr 9, 2021Published: Nov 4, 2021
Est. expiryOct 24, 2034(~8.2 yrs left)· nominal 20-yr term from priority
A61K 31/421C07D 239/34A61P 43/00C07D 231/12C07D 213/65C12N 15/09A61K 31/505C07D 231/22C07D 263/38A61K 31/4418A61P 27/02C07K 14/47A61K 31/415C07D 213/70C07D 263/46
70
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Claims

Abstract

Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4. A compound represented by the formula (I): wherein each symbol is as defined in the Description, or a salt thereof has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.

Claims

exact text as granted — not AI-modified
1 . A compound represented by the formula (I): 
       
         
           
           
               
               
           
         
       
       wherein
 ring A is an optionally further substituted monocyclic nitrogen-containing aromatic heterocycle; 
 X is CH 2  or O; and 
 R is a C 1-6  alkyl group, 
 or a salt thereof. 
 
     
     
         2 . The compound according to  claim 1 , wherein R is a methyl or ethyl group, or a salt thereof. 
     
     
         3 . Methyl 2-((1-(3,5-bis(trifluoromethyl)phenyl)-1H-pyrazol-3-yl)oxy)acetate or a salt thereof 
     
     
         4 . Ethyl 3-(3-(3,5-bis(Trifluoromethyl)phenyl)-1H-pyrazol-1-yl) propanoate or a salt thereof. 
     
     
         5 . A medicament comprising the compound according to  claim 1  or a salt thereof. 
     
     
         6 . A medicament comprising the compound according to  claim 2  or a salt thereof. 
     
     
         7 . A method of lowering retinol binding protein 4 in a mammal, comprising administering an effective amount of the compound according to  claim 1 , or a salt thereof to the mammal. 
     
     
         8 . A method for the prophylaxis or treatment of macular degeneration and/or Stargardt's disease in a mammal, comprising administering an effective amount of the compound according to  claim 1 , or a salt thereof to the mammal. 
     
     
         9 . A method of lowering retinol binding protein 4 in a mammal, comprising administering an effective amount of the compound according to  claim 2 , or a salt thereof to the mammal. 
     
     
         10 . A method for the prophylaxis or treatment of macular degeneration and/or Stargardt's disease in a mammal, comprising administering an effective amount of the compound according to  claim 2 , or a salt thereof to the mammal.

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