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Abstract

The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of formula (1.0) wherein R.sub.2 is a hydrogen or a methyl or ethyl group; R.sub.3 is a hydrogen or a methyl or ethyl group; n is 0, 1, 2, 3, 4, 5, or 6; and R.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) phenyl or substituted pneyly; (c) alkyl; (d) heterocyclic; (e) decahydronaphthalene; and (f) octahydroindene; with the proviso that when X is H, A can be --CH.sub.2 CH.sub.2, --COCH.sub.2 --CON(CH.sub.3)--, --CH.dbd.CH--, .alpha., --CH.sub.2 --NH--, --CH.sub.3 --N(CH.sub.3)--, --CH(OH)CH.sub.2 --, --NH--CH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.sub.2 O--, --CH.sub.2 S--, and --NHCOO--; when X is NH.sub.2, HN(CH.sub.3), N(CH.sub.3).sub.2, OH, OCH.sub.3, CH.sub.3, SH and SCH.sub.3 ; A can be --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.dbd.XH--, --COCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH( )H)CH.sub.2 --, or .beta.; and when R.sub.1 and X taken together denote a 5,6 or 6,6 saturated bicyclic ring structure, X can be NH, O, or S. The pharmaceutically acceptable salts, hydrates, and individual stereoisomers of compounds of structural formula (1.0), as well as mixtures thereof, are also contemplated as falling within the scope of the present invention. The invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of said formula and a method of treating conditions in which antagonism of histamine H.sub.3 receptors may be of therapeutic importance.

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First Claim