Thiophene derivatives and their pharmaceutical compositions and method of use
AssigneeGlaxo Group Limited
InventorsJohn Bradshaw, Duncan B. Judd, Barry J. Price, John W. Clitherow
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AssigneeGlaxo Group Limited
InventorsJohn Bradshaw, Duncan B. Judd, Barry J. Price, John W. Clitherow
Estimating the term…
The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which R.sub.4 represents hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, heteroaralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl, and R.sub.5 represents hydrogen or a C.sub.1-4 alkyl group or R.sub.4 and R.sub.5 may, 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 C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom selected from oxygen and sulphur; Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms; R.sub.3, which may be in either the 2 or 3-position, represents the group ##STR2## where X represents --CH.sub.2 --, --O-- or --S--; n represents zero, 1 or 2; m represents 2, 3 or 4; and where Y represents S, O, CHNO.sub.2 or NR.sub.7 where R.sub.7 is nitro, cyano, alkylsulphonyl or arylsulphonyl; R.sub.6 represents hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl or aralkyl; with the provisos that where R.sub.2 represents the group R.sub.4 R.sub.5 NAlk then R.sub.3 is in the 2-position; and where R.sub.2 represents hydrogen then R.sub.3 is in the 3-position. The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -- antagonists.
A compound of formula (I) ##STR24## and physiologically acceptable salts and hydrates thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 Nalk- in which R.sub.4 represents hydrogen, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, ar C.sub.1-6 alkyl wherein ar is phenyl or phenyl substituted with one or more C.sub.1-3 alkyl or C.sub.1-3 alkoxy groups or halogen atoms;
Dependencies are inferred from the claim text.