Method and composition for the treatment of diarrhea and gastrointestinal spasms

Abstract

Anti-diarrheal and/or gastrointestinal anti-spasmodic pharmaceutical compositions containing [A] a polyamine of the formula: R 1 —N 1 (R 2 )—(CH 2 )x-N 2 H—Q—N 3 H—(CH 2 )y-N 4 (R 3 )—R 4   (I) wherein: R 1 , R 2 , R 3 and R 4 may be the same or different and are H, alkyl, cycloalkyl or aralkyl having from 1 to 12 carbon atoms, or a heterocyclic group having from 3 to 10 atoms wherein the hetero atom is said N 1 or N 4 ; Q is a cycloalkyl group having from 3 to 10 carbon atoms; x is an integer from 3 to 6, inclusive; and y is an integer from 3 to 6, inclusive; or (II) a salt thereof with a pharmaceutically acceptable acid; and [B] a pharmaceutically acceptable carrier therefor as well as methods of treatment utilizing the polyamines are disclosed.

What is claimed is:  
     
         1 . An anti-diarrheal or gastrointestinal anti-spasmodic pharmaceutical composition comprising [A] an effective amount of a compound having the formula: 
       R 1 —N 1 (R 2 )—(CH 2 )x-N 2 H—Q—N 3 H—(CH 2 )y-N 4 (R 3 )—R 4   (I) 
       wherein: R 1 , R 2 , R 3  and R 4  may be the same or different and are H, alkyl, cycloalkyl or aralkyl having from 1 to 12 carbon atoms, or a heterocyclic group having from 3 to 10 atoms wherein the hetero atom is said N 1  or N 4 ; 
 Q is a cycloalkyl group having from 3 to 10 carbon atoms;  
 x is an integer from 3 to 6, inclusive;  
 and y is an integer from 3 to 6, inclusive;  
 or (II) a salt thereof with a pharmaceutically acceptable acid; and [B] a pharmaceutically acceptable carrier therefor.  
 
     
     
         2 . A composition according to  claim 1  wherein Q is connected either cis or trans as the (1,2), (1,3), (1,4), (1,5) or (1,6) isomer.  
     
     
         3 . A composition according to  claim 1  wherein Q is cyclohexyl.  
     
     
         4 . A composition according to  claim 1  wherein x is 3 and y is 3.  
     
     
         5 . A composition according to  claim 1  wherein x is 3, y is 3, R 1  and R 3  are both H and R 2  and R 4  are both ethyl.  
     
     
         6 . A composition according to  claim 1  wherein Q is cyclohexyl; x and y are 3; R 1  and R 3  are both H, and R 2  and R 4  are both ethyl.  
     
     
         7 . A composition according to  claim 6  wherein said polyamine is the trans (1,4) isomer.  
     
     
         8 . A method of treating diarrhea or gastrointestinal spasm in a human or non-human animal in need thereof comprising administering to said animal an effective amount of a compound having the formula: 
       R 1 —N 1 (R 2 )—(CH 2 )x-N 2 H—Q—N 3 H—(CH 2 )y-N 4 (R 3 )—R 4   (I) 
       wherein: R 1 , R 2 , R 3  and R 4  may be the same or different and are H, alkyl, cycloalkyl or aralkyl having from 1 to 12 carbon atoms, or a heterocyclic group having from 3 to 10 atoms wherein the hetero atom is said N 1  or N 4 ; 
 Q is a cycloalkyl group having from 3 to 10 carbon atoms;  
 x is an integer from 3 to 6, inclusive;  
 and y is an integer from 3 to 6, inclusive;  
 or (II) a salt thereof with a pharmaceutically acceptable acid.  
 
     
     
         9 . A method according to  claim 8  wherein Q is connected either cis or trans as the (1,2), (1,3), (1,4), (1,5) or (1,6) isomer.  
     
     
         10 . A method according to  claim 8  wherein Q is cyclohexyl.  
     
     
         11 . A method according to  claim 8  wherein x is 3 and y is 3.  
     
     
         12 . A method according to  claim 8  wherein x is 3, y is 3, R 1  and R 3  are both H and R 2  and R 4  are both ethyl.  
     
     
         13 . A method according to  claim 8  wherein Q is cyclohexyl; x and y are 3; R 1  and R 3  are both H, and R 2  and R 4  are both ethyl.  
     
     
         14 . A method according to  claim 13  wherein said polyamine is the trans (1,4) isomer.