Potentiator for radiation therapy comprising pyridine derivative as active ingredient

Abstract

The present invention relates to a radiotherapy enhancer that can reduce the radiation dose and adverse drug reactions when used in combination with a cancer radiotherapy. There is provided a radiotherapy enhancer comprising, as an active ingredient, a pyridine derivative represented by general formula (1): wherein R 1 , R 2 , and R 4 may be the same or different from one another and represent a hydrogen atom, hydroxy group, or protected hydroxy group, excluding the case where R 1 , R 2 , and R 4 are all a hydrogen atom, and R 3 represents a halogen atom, amino group, carboxyl group, carbamoyl group, cyano group, nitro group, alkyl group having 1 to 6 carbon atoms, alkenyl group having 2 to 6 carbon atoms, or carbonyl group containing an alkoxy group having 1 to 6 carbon atoms).

1 . A radiotherapy enhancer comprising, as an active ingredient, a pyridine derivative represented by general formula (1): 
     
       
         
         
             
             
         
       
       wherein R 1 , R 2 , and R 4  may be the same or different from one another and represent a hydrogen atom, hydroxy group, or protected hydroxy group, excluding the case where R 1 , R 2 , and R 4  are all a hydrogen atom, and R 3  represents a halogen atom, amino group, carboxyl group, carbamoyl group, cyano group, nitro group, alkyl group having 1 to 6 carbon atoms, alkenyl group having 2 to 6 carbon atoms, or carbonyl group containing an alkoxy group having 1 to 6 carbon atoms. 
     
   
   
       2 . The radiotherapy enhancer according to  claim 1  comprising a pyridine derivative as an active ingredient, wherein, in the general formula (1), R 1  and R 2  may be the same or different from each other and represent hydroxy group or a protected hydroxy group, and R 4  represents a hydrogen atom. 
   
   
       3 . The radiotherapy enhancer according to  claim 1  comprising a pyridine derivative as an active ingredient, wherein, in the general formula (1), R 1  and R 4  may be the same or different from each other and represent hydroxy group or protected hydroxy group, and R 2  represents a hydrogen atom. 
   
   
       4 . The radiotherapy enhancer according to  claim 1  comprising a pyridine derivative as an active ingredient, wherein, in the general formula (1), any two of R 1 , R 2 , and R 4  represent hydroxy group, the remaining one represents a hydrogen atom, and R 3  represents a halogen atom or cyano group. 
   
   
       5 . The radiotherapy enhancer according to  claim 1  comprising a pyridine derivative as an active ingredient, wherein, in the general formula (1), R 1  and R 2  represent hydroxy group, R 3  represents a chlorine atom, and R 4  represents a hydrogen atom. 
   
   
       6 . The radiotherapy enhancer according to  claim 1  comprising a pyridine derivative as an active ingredient, wherein, in the general formula (1), R 1  and R 4  represent hydroxy group, R 3  represents cyano group, and R 2  represents a hydrogen atom. 
   
   
       7 . The radiotherapy enhancer according to any one of  claims 1  to  6 , which is for use in combination with a cancer radiotherapy. 
   
   
       8 . A cancer radiotherapy, characterized in that the radiotherapy enhancer according to any one of  claims 1  to  6  and radiation are used in combination. 
   
   
       9 . Use of a pyridine derivative represented by general formula (1): 
     
       
         
         
             
             
         
       
       wherein R 1 , R 2 , and R 4  may be the same or different from one another and represent a hydrogen atom, hydroxy group, or protected hydroxy group, excluding the case where R 1 , R 2 , and R 4  are all a hydrogen atom, and R 3  represents a halogen atom, amino group, carboxyl group, carbamoyl group, cyano group, nitro group, alkyl group having 1 to 6 carbon atoms, alkenyl group having 2 to 6 carbon atoms, or carbonyl group containing an alkoxy group having 1 to 6 carbon atoms), for the production of a radiotherapy enhancer. 
     
   
   
       10 . The use according to  claim 9 , wherein, in the general formula (1), R 1  and R 2  may be the same or different from each other and represent hydroxy group or protected hydroxy group, and R 4  represents a hydrogen atom. 
   
   
       11 . The use according to  claim 9 , wherein, in the general formula (1), R 1  and R 4  may be the same or different from each other and represent hydroxy group or a protected hydroxy group, and R 2  represents a hydrogen atom. 
   
   
       12 . The use according to  claim 9 , wherein, in the general formula (1), any two of R 1 , R 2 , and R 4  represent hydroxy group, the remaining one represents a hydrogen atom, and R 3  represents a halogen atom or cyano group. 
   
   
       13 . The use according to  claim 9 , wherein, in the general formula (1), R 1  and R 2  represent hydroxy group, R 3  represents a chlorine atom, and R 4  represents a hydrogen atom. 
   
   
       14 . The use according to  claim 9 , wherein, in the general formula (1), R 1  and R 4  represent hydroxy group, R 3  represents cyano group, and R 2  represents a hydrogen atom. 
   
   
       15 . The use according to any one of  claims 9  to  14 , which is for use in combination with a cancer radiotherapy.