Patch for anti-dermatophytosis

Abstract

A patch for nails or skin for prevention or treatment of dermatophytosis, containing a layer including a pressure sensitive adhesive layer and a compound represented by the formula: wherein R 1 represents hydrogen, C 1-16 alkyl, or trifluoromethyl; R 2 represents hydrogen, C 1-6 alkyl, halogen, —COO(C 1-6 alkyl), or (CH 2 ) 1-3 COOR; R 3 represents hydrogen, C 1-6 alkyl, amino, trifluoromethyl, or OR; R 4 represents hydroxyl; R 5 represents hydrogen, C 1-6 alkyl, hydroxyl, or halogen; R 6 represents hydrogen, C 1-6 alkyl, trifluoromethyl, halogen, amino, —NR a R b , nitro, hydroxy-C 1-6 alkyl, —CONR a R b , —COO(C 1-6 alkyl), —COOH, —(CH 2 ) 1-3 COOR, or OR a (R a and R b each represents hydrogen, C 1-6 alkyl, or C 1-6 acyl); R 7 represents hydrogen, C 1-6 alkyl, —OR, or halogen; R 8 represents hydrogen, C 1-6 alkyl, hydroxyl, amino, or nitro; and R represents hydrogen or C 1-6 alkyl; or a salt thereof.

1 . A patch for a nail and/or skin for the prevention or treatment of dermatophytosis which comprises a layer comprising a pressure sensitive adhesive layer and a compound represented by the following formula (I): 
       
         
           
           
               
               
           
         
         wherein 
         R 1  represents a hydrogen atom, C 1-6  alkyl, or trifluoromethyl, 
         R 2  represents a hydrogen atom, C 1-6  alkyl, halogen, —COO(C 1-6  alkyl), or (CH 2 ) 1-3 COOR, wherein R represents a hydrogen atom or C 1-6  alkyl, 
         R 3  represents a hydrogen atom, C 1-6  alkyl, amino, trifluoromethyl, or OR, wherein R represents a hydrogen atom or C 1-6  alkyl, 
         R 4  represents a hydroxyl group, 
         R 5  represents a hydrogen atom, C 1-6  alkyl, a hydroxyl group, or halogen, 
         R 6  represents a hydrogen atom, C 1-6  alkyl, trifluoromethyl, halogen, amino, —NR a R b , nitro, hydroxy-C 1-6  alkyl, —CONR a R b , —COO(C 1-6  alkyl); —COOH, —(CH 2 ) 1-3 COOR, or OR a , wherein R represents a hydrogen atom or C 1-6  alkyl, and R a  and R b  are the same or different from each other, and each represents a hydrogen atom, C 1-6  alkyl, or C 1-6  acyl, 
         R 7  represents a hydrogen atom, C 1-6  alkyl, —OR, wherein R represents a hydrogen atom or C 1-6  alkyl, or halogen, and 
         R 8  represents a hydrogen atom, C 1-6  alkyl, a hydroxyl group, amino, or nitro or a salt thereof. 
       
     
     
         2 . The patch for a nail and/or skin according to  claim 1 , wherein in the compound represented by the formula (I),
 R 1  is a hydrogen atom or C 1-6  alkyl,   R 2  is a hydrogen atom, C 1-6  alkyl, halogen, or —(CH 2 ) 1-3 COOR, wherein R represents a hydrogen atom or C 1-6  alkyl,   R 3  is a hydrogen atom, or C 1-6  alkyl,   R 4  is a hydroxyl group,   R 5  is a hydrogen atom,   R 6  is a hydrogen atom, C 1-6  alkyl, trifluoromethyl, halogen, amino, —NR a R b , nitro, hydroxy-C 1-6  alkyl, —CONR a R b , —COOH, or OR a , wherein R a  and R b  are the same or different from each other, and each represent a hydrogen atom, C 1-6  alkyl, or C 1-6  acyl,   R 7  is a hydrogen atom, and   R 8  is a hydrogen atom, C 1-6  alkyl, amino, or nitro;   or a salt thereof.   
     
     
         3 . The patch for a nail and/or skin according to  claim 1 , wherein in the compound represented by the formula (I),
 R 1  is C 1-6  alkyl,   R 2  is a hydrogen atom, C 1-6  alkyl, or halogen,   R 3  is C 1-6  alkyl,   R 4  is a hydroxyl group,   R 5  is a hydrogen atom,   R 6  is a hydrogen atom, C 1-6  alkyl, halogen, or OR a , wherein R a  represents a hydrogen atom, C 1-6  alkyl, or C 1-6  acyl,   R 7  is a hydrogen atom, and   R 8  is a hydrogen atom;   or a salt thereof.   
     
     
         4 . The patch for a nail and/or skin according to  claim 1 , wherein in the compound represented by the formula (I), R 1  is C 1-6  alkyl, R 2  is a hydrogen atom, R 3  is C 1-6  alkyl, R 4  is a hydroxyl group, R 5  is a hydrogen atom, R 6  is C 1-6  alkyl, R 7  is a hydrogen atom, and R 8  is a hydrogen atom; or a salt thereof. 
     
     
         5 . The patch for a nail and/or skin according to  claim 1 , wherein the compound represented by formula (I) is 2-(3,5-dimethyl-1H-pyrazol-1-yl)-5-methylphenol or a salt thereof. 
     
     
         6 . The patch for a nail and/or skin according to  claim 1 , wherein the pressure sensitive adhesive layer comprises an acrylic-based pressure sensitive adhesive. 
     
     
         7 . The patch for a nail and/or skin according to  claim 6 , wherein the acrylic-based pressure sensitive adhesive comprises a copolymer of 2-ethylhexyl acrylate and N-vinylpyrrolidone. 
     
     
         8 . The patch for a nail and/or skin according to  claim 1 , wherein the compound represented by the formula (I) or a salt thereof is contained in an amount of 5 to 30% by mass based on the total amount of the pressure sensitive adhesive. 
     
     
         9 . The patch for a nail and/or skin according  claim 1 , wherein the compound represented by the formula (I) or a salt thereof is contained in an amount of 5 to 20% by mass based on the total amount of the pressure sensitive adhesive. 
     
     
         10 . The patch for a nail and/or skin according to  claim 1 , wherein the compound represented by the formula (I) or a salt thereof is combined in an amount of 5 to 15% by mass based on the total amount of the pressure sensitive adhesive. 
     
     
         11 . The patch for a nail and/or skin according to  claim 1 , wherein the dermatophytosis is caused by tinea unguium. 
     
     
         12 . The patch for a nail and/or skin according to  claim 8 , wherein the pressure sensitive adhesive is an acrylic-based pressure sensitive adhesive. 
     
     
         13 . The patch for a nail and/or skin according to  claim 9 , wherein the pressure sensitive adhesive is an acrylic-based pressure sensitive adhesive. 
     
     
         14 . The patch for a nail and/or skin according to  claim 10 , wherein the pressure sensitive adhesive is an acrylic-based pressure sensitive adhesive.