3,4-Disubstituted-1,2,5-oxadiazoles having histamine H2-receptor antagonist activity.

摘要

Histamine H<Sub>2</Sub>-antagonists of the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="22" wi="68" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein
<UnorderedLists id="ula01" listStyle="none"><ListItem>m is an integer of from 0 to 2 inciusive;</ListItem><ListItem>n is an integer of from 2 to 5 inclusive;</ListItem><ListItem>Z is oxvaen. sulfur or methviene: and</ListItem><ListItem>A is
<Chemistry id="chema02" num="0002"><Image id="ia02" he="23" wi="57" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry><Chemistry id="chema03" num="0003"><Image id="ia03" he="29" wi="58" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>in which R<Sup>1</Sup> is hydrogen, (lower)alkyl, or (lower) alkoxy, and R<Sup>2</Sup> is
<Chemistry id="chema04" num="0004"><Image id="ia04" he="13" wi="25" file="IMGA0004.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>in which q is an integer of from 1 to 4 inclusive, and R<Sup>3</Sup> and R<Sup>4</Sup> each are independently, (lower) alkyl, (lower)alkoxy (lower) alkyl in which the (lower) alkoxy moiety is at least two carbon atoms removed from the nitrogen atom, cyclo (lower) alkyl, or phenyl (lower) alkyl; provided that R<Sup>3</Sup> and R<Sup>4</Sup> may not both be cyclo (lower) alkyl; or R<Sup>3</Sup> and R<Sup>4</Sup>, taken together with the nitrogen atom to which they are attached, may be pyrrolidino, methylpyrrolidino, dimethylpyrrolidino, morpholino, thiomorpholino, piperidino, methylpiperidino, dimethylpiperidino, N-methylpiperazino, 1,2,3,6-tetrahydropyridyt, homopiperidino, heptamethyleneimino, octamethyleneimino, or 3-azabicyclo-[3.2.2]non-3-yl; and nontoxic, pharmaceutically acceptable salts, hydrates, solvates and N-oxides thereof.</ListItem></UnorderedLists>