Heterocyclic derivatives as histamine h.sub.2- antagonists

Details Heterocyclic derivatives as histamine h.sub.2- antagonists Heterocyclic derivatives as histamine h.sub.2- antagonists

C - Chemistry, Metallurgy

07

D

260/271, 260/277

C07D 471/04 (2006.01) C07C 279/28 (2006.01) C07D 239/46 (2006.01) C07D 249/14 (2006.01) C07D 257/06 (2006.01) C07D 295/096 (2006.01)

Patent

CA 1189508

ABSTRACT OF THE DISCLOSURE The invention relates to compounds of the general formula (I) Image (I) and physiologically acceptable salts, hydrates and bioprecursors thereof, in which R1 represents hydrogens, C1-14 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, heteroaralkyl or alkyl substituted by cycloalkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino; and R2 represents hydrogen or C1-4 alkyl group; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom selected from oxygen or sulphur: Alk represents a straight or branched alkylene chain of l to 3 carbon atoms; Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3- or 1- and 4- positions: R5 represents hydrogen or acyl; n and m, which may be the same or different, are each 1 or 2; R3 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxy C2-6 alkyl, alkoxy C2-6 alkyl or C1-4 alkanoyloxy C2-6 alkyl; and R7 represents hydrogen, alkyl, alkenyl, aralkyl, acyloxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aralkyloxyalkyl, or the group (CH2)qR6 where q is zero, 1, 2, 3, 4, 5 or 6 and the alkylene chain (CH2)q may be straight or branched, and R6 is hydroxy, alkoxy, nitro, heteroaryl, tetra- hydropyranyloxy or CH2NHC(=X)NHR9 where X represents NCN, Abstract continued... NSO2 Methyl, NSO2 Phenyl or CHNO2 and R9 is alkyl; or R6 is the group NR10R11, where R10 is hydrogen or alkyl; and R11 is hydrogen, alkyl, alkenyl, aryl, aralkyl, or heteroaralkyl, or R11 is the group SO2R12 where R12 is alkyl or aryl; or R11 is the group COR13 where R13 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halo- methyl, heteroaryl, heteroaralkyl or the group NHR14 where R14 is hydrogen, alkyl, cycloalkylr aryl or aralkyl; or R10 and R11 together represent the group =CR15R16 where R15 represents aryl or heteroaryl and R16 represents hydrogen or alkyl; or R6 is the group SO2R17 in which R17 is hydroxy, alkyl, aryl or the group NR18R19 where R18 and R19, which may be the same or different, each represent hydrogen or alkyl; or R6 is the group COR20 where R20 is hydrogen, hydroxy, alkoxy, aryloxy, aralkyloxy, alkyl, aryl, aralkyl or the group NR21R22 where R21 is hydrogen or alkyl optionally substituted by a hydroxy or alkoxy group; and R22 is hydrogen, alkyl (optionally substituted by a hydroxy or alkoxy group), alkenyl, aryl, aralkyl or cycloalkyl, or NR21R22 forms a 5 to 8 membered ring which may contain another heteroatom, e.g. oxygen, or a double bond and/or may be substituted by hydroxy or one or two C1-3 alkyl groups or R6 is the group CR23=NR24 where R23 is hydrogen, alkyl, aryl or aralkyl and R24 is hydroxy, alkoxy, aralkyl- oxy or -NHC(=Y)NH2 where Y is oxygen or sulphur; or when A represents CR7 and B represents N, the groups R3 and R7 taken together represent Image or -(CH2)4-; with the proviso that when the group R6 contains a carbon atom through which it is linked to the alkylene group (CH2)q then the total number of carbon atoms in the resulting chain is not greater than 6 (i.e. q is not greater than 5). The compounds show pharmacological activity as selective histamine H2-antagonists.

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