Patent EP-0173516-A2 (EP)
Inventor: TODA MASAAKI
IPC: A61K31/165
Filed: 1985-08-15
Abstract: A novel (fused) benz(thio)amides of the general formula:
       
(wherein, symbol A represents a single bond or a group of methylene, ethylene, trimethylene, tetramethylene, vinylene, propenylene, butenylene, butadienylene or ethynylene group optionally being substituted by one, two or three of straight or branched alkyl group(s) of from 1 to 10 carbon atom(s) and/or phenyl group(s). 
     Symbol B represents
     (i) a carbocyclic ring of from 4to 8 members being unreplaced or replaced one, two or three of optional carbon atom(s) by oxygen, nitro and/or sulphur atom(s). (The ring may optionally be substituted by group(s) of oxo, thioxo and/or hydroxy group(s).) or   (ii) a dibalent group of formula:
       
Symbol T represents an oxygen atom or a sulphur atom. R 1  represents a group of general formula:
     
     
       (iv) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s).  
(wherein R 5  and R 6  independently represent a hydrogen atom or a halogen atom or a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s) being unreplaced or replaced one, two, three, four or five of optional carbon atom(s) by oxygen atom(s), sulphur atom(s), halogen atom(s), nitrogen atom(s), benzene ring(s), thiophene ring(s), naphthalene ring(s), carbocyclic ring(s) of from 4 to 7 carbon atom(s), carbonyl group(s), carbonyloxy group(s), hydroxy group(s), carboxy group(s), azido group(s) and/or nitro group(s)).
   R 2  represents a hydrogen atom or a straight or branched alkyl group of from 1 to 6 carbon atom(s).   R 3  represents a hydrogen atom, a halogen atom, a hydroxy group, a nitro group, a group of general formula: -COOR 7  [wherein R 7  represents a hydrogen atom or a straight or branched alkyl group of from 1 to 6 carbon atom(s).) or a straight or branched alkyl, alkoxy or alkylthio group of from 1 to 6 carbon atom(s).   R 4  represents       (i) when symbol B represents a closed ring, a group of general formula:
     
     
     or
       
(wherein symbol U represents an oxygen atom or a sulphur atom. R 8  represents a hydrogen atom or a straight or branched alkyl group of from 1 to 6 carbon atom(s). n and m represent an integer of from 1 to 10, respectively, p and q represent zero or an integer of from 1 to 10, respectively.) or   (ii) when symbol B do not represent a ring, a group of general formula:
     or
       
(wherein R 8 , p and q represent the same meaning as depicted hereinbefore. With the proviso that, when the symbol B represents a group of formula:
       
p does not represent zero).   With the proviso that, following compounds are excluded, i.e. compounds of general formula:
     (wherein the symbol A' is a vinylene or ethylene group optionally being substituted by straight or branched alkyl group(s) of from 1 to 4 carbon atom(s), R 4 ' is the general formula:
       
(wherein all the symbols are the same meaning as depicted hereinbefore.) and R 1'  is   (i) a group of the general formula:
       
(wherein R 5 ' and R 6'  are hydrogen atom(s), hydroxy group(s), halogen atom(s), straight or branched alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy or acyloxy group(s) of from 1 to 4 carbon atom(s) or cycloalkyl group(s) of from 3 to 6 carbon atom(s), independently.) or (ii) a group of the general formula:
       
(wherein R 5'  and R 6'  are the same meaning as depicted hereinbefore.)) or non-toxic salts thereof possess an antagonistic activity on leukotrienes (SRS), inhibitory activity on 5a-reductase, on phospholipase and on aldose reductase and are therefore useful for the prevention and/or treatment for diseases induced by leukotrienes, 5a-reductase, phospholipase and aldose reductase in mammals, especially human beings.