Marasmius androsaceus l.es fr extract, piperidone derivative, and their use for the preparation of antihypertensives

Abstract

The present invention relates to Marasmius androsaceus L.es Fr extract, a compound of formula I, or pharmaceutically acceptable salts thereof, and to methods for their preparation, pharmaceutical composition comprising the same as well as use of the extract or the compound in the preparation of a medicament for the prevention and/or treatment of hypertension and its related diseases.

1 . A compound of the following formula I or a pharmaceutically acceptable salt thereof: 
     
       
         
         
             
             
         
       
       wherein, 
       R 1  and each of R 2 , the same or different, independently represent hydrogen atom or C 1 -C 5  alkyl; 
          represents a single bond or a double bond, when   is a double bond, R 3  is oxygen atom; when  is a single bond, R 3  is hydroxyl group, wherein said compound is 1-ethyl-3,3,5,5-tetramethyl-4-piperidone or 3,3,5,5-tetramethyl-4-piperidanol. 
     
   
   
       2 . A compound of the following formula II or a pharmaceutically acceptable salt thereof: 
     
       
         
         
             
             
         
       
     
   
   
       3 .  Marasmius androsaceus  L.es Fr extract, characterized by comprising the compound of formula II as claimed in  claim 2 . 
   
   
       4 . A pharmaceutical composition, comprising the compound according to  claim 1  and one or more pharmaceutically acceptable carriers or excipients. 
   
   
       5 . A pharmaceutical composition, comprising the compound according to  claim 2  and one or more pharmaceutically acceptable carriers or excipients. 
   
   
       6 . A pharmaceutical composition, comprising the compound according to  claim 1 , wherein said compound is 1-ethyl-3,3,5,5-tetramethyl-4-piperidone. 
   
   
       7 . A pharmaceutical composition, comprising the compound according to  claim 1 , wherein said compound is 3,3,5,5-tetramethyl-4-piperidanol. 
   
   
       8 . The pharmaceutical composition of  claim 4 , in a dosage form suitable for oral, injection or topical administration. 
   
   
       9 . The pharmaceutical composition of  claim 5 , in a dosage form suitable for oral, injection or topical administration. 
   
   
       10 . A method for treating an individual with cardiovascular disease or cerebrovascular disease comprising administering the compound of  claim 1  to said individual. 
   
   
       11 . A method for treating an individual with cardiovascular disease or cerebrovascular disease comprising administering the compound of  claim 2  to said individual. 
   
   
       12 . The method of  claim 10 , wherein said compound is 1-ethyl-3,3,5,5-tetramethyl-4-piperidone. 
   
   
       13 . The method of  claim 10 , wherein said compound is 3,3,5,5-tetramethyl-4-piperidanol.