The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Dec. 08, 1981

Filed:

Jun. 06, 1980
Applicant:
Inventors:

Michael Martin-Smith, Hertford, GB;

Barry Price, Hertford, GB;

John Bradshaw, Ware, GB;

John W Clitherow, Sawbridgeworth, GB;

Assignee:

Glaxo Group Limited, London, GB;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K / ; A61K / ; C07D / ; C07D / ;
U.S. Cl.
CPC ...
424263 ; 26032625 ; 549 74 ; 549 75 ; 26032635 ; 549 76 ; 549 77 ; 2603 / ; 26032682 ; 26032683 ; 424251 ; 424267 ; 4242 / ; 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 ;
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.


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