USRE37078EExpiredUtility

Thiophene compounds

30
Assignee: ADIRPriority: Feb 23, 1995Filed: Aug 3, 1999Granted: Feb 27, 2001
Est. expiryFeb 23, 2015(expired)· nominal 20-yr term from priority
A61P 29/00C07D 333/24A61P 1/00A61P 17/00
30
PatentIndex Score
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Claims

Abstract

The invention relates to thiophene compounds of formula: wherein: X 1 , X 2 , Y 1 and Y 2 , which are identical or different, each represents hydrogen or halogen, (C 1 -C 5 )-alkyl or alkoxy, or trifluoromethyl, X 1 and Y 1 , which are identical or different, each represents C 1 -C 5 alkoxy, X 2 and Y 2 each represents hydrogen, R 1 represents hydrogen or (C 1 -C 5 )-alkyl, A represents a straight (C 1 -C 5 )-hydrocarbon chain of which each carbon atom is optionally mono- or di-substituted by a (C 1 -C 5 )-alkyl, and R 2 represents hydrogen, (C 1 -C 6 )-alkyl, cyclohexyl or benzyl; and their physiologically tolerable salts. The products of the invention may be used as anti-inflammatory agents.

Claims

exact text as granted — not AI-modified
We claim:  
     
       1. A thiophene compound selected from those of formula I:                    
       wherein: 
       X 1 , X 2 , Y 1  and Y 2   X   1    and Y   1 , which are identical or different, each represents (C 1 -C 5 ) alkoxy each in straight or branched chain,  
       X 2    and Y   2    each represents hydrogen,   
       R 1  represents hydrogen;  
       A represents a straight (C 1 -C 2 ) hydrocarbon chain, and  
       R 2  represents (C 1 -C 5 ) alkyl in straight or branched chain;  
       and physiologically tolerable addition salts thereof with appropriate bases. 
     
     
       2. A compound of claim  1  selected from the group consisting of 3-[4,5-bis(4-methoxyphenyl) thien-2-yl]-N-hydroxy-N-methylpropionamide and a calcium salt thereof. 
     
     
       3. A compound of claim  1  which is 4-[4,5-bis(4-methoxyphenyl) thien-2-yl]-N-hydroxy-N-methylbutanamide. 
     
     
       4. A compound of claim  1  which is 3-[4,5-bis(4-methoxyphenyl) thien-2-yl]-N-ethyl-N-hydroxypropionamide. 
     
     
       5. A method for treating a living animal body afflicted with a rheumatological inflammation or inflammation of the intestinal or cutaneous type in which leukotrienes are implicated, comprising the step of administering to the living animal body an amount of a compound of claim  1  which is effective for alleviation of said condition. 
     
     
       6. A pharmaceutical composition useful in the treatment of rheumatological inflammation comprising as active ingredient a compound according to claim  1 , in combination with one or more pharmaceutical excipients.

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