Aminoalkylthiophene derivatives as histamine H.sub.2 -antagonist

Details Aminoalkylthiophene derivatives as histamine H.sub.2 -antagonist Aminoalkylthiophene derivatives as histamine H.sub.2 -antagonist

1980-06-06

1981-12-08

Schwartz, Richard A.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

26032625, 549 74, 549 75, 26032635, 549 76, 549 77, 2603265SM, 26032682, 26032683, 424251, 424267, 424273R, 424274, 424275, 544298, 544316, 544333, 546187, 546208, 546209, 546210, 546212, 546213, 546281, 546284, 548187, 548213, 548215, 548228, 548229, 548240, 548243, 548336, 549 59, 549 60, 549 65, A61K 31445, A61K 3144, C07D40912, C07D40914

Patent

active

043047807

ABSTRACT:
The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof,
in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl;
R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.4 represents hydrogen or lower alkyl; Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5-positions, or 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;
X represents --CH.sub.2 --, --O-- or --S--;
n represents zero, 1 or 2;
m represents 2, 3 or 4;
Alk represents a straight chain alkylene group of 1 to 3 carbon atoms;
(except that n is not zero when X is oxygen and Q is a furan or thiophen ring system)
q represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 --group;
p represents zero, 1 or 2;
E represents --CH.sub.2 --, --O-- or --S--; and
Z represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring which may be optionally substituted by one or more groups or Z represents ##STR3## where Q' represents any of the rings defined for Q; Alk' represents any of the groups defined for Alk; and R.sub.5 and R.sub.6, which may be the same or different, each represent any of the groups defined for R.sub.1 and R.sub.2 ;
(except that p is not zero when E is oxygen and Q' or Z is a furan or thiophen ring system)
The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

REFERENCES:
patent: 4128658 (1978-12-01), Price et al.
patent: 4203909 (1980-05-01), Algieri et al.
Chemical Abstracts, 90:87257u (1979), [Price, B. et al., German Ols 2,821,409, 11/30/78].

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