Tetrazole derivatives, anti-ulcer composition containing the same and method for treating ulcers

A tetrazole derivative of the formula:

• ##STR20## wherein R.sup.1 is hydrogen, an alkyl having 1 to 6 carbon atoms, a cycloalkyl having 3 to 12 carbon atoms or phenyl;
• l is 0;
• B is an alkylene having 1 to 6 carbon atoms;
• R.sup.2 is hydroxy, an alkoxy having 1 to 6 carbon atoms, or a group:
• ##STR21## wherein R.sup.3 and R.sup.4 are the same or different and are each hydrogen, an alkyl having 1 to 6 carbon atoms, a cycloalkyl having 3 to 12 carbon atoms, phenyl, a cycloalkyl-alkyl having 1 to 6 carbon atoms in the alkyl moiety and 3 to 8 carbon atoms in the cycloalkyl moiety, a phenylalkyl having 1 to 6 carbon atoms in the alkyl moiety, a hydroxyalkyl having 1 to 6 carbon atoms in the alkyl moiety;
• said cycloalkyl, phenyl and phenyl alkyl optionally have on the cycloalkyl or phenyl ring one or two substituents selected from the group consisting of an alkoxy having 1 to 6 carbon atoms, an alkyl having 1 to 6 carbon atoms, a halogen, an N,N-dialkylamino having 1 to 6 carbon atoms in each alkyl moiety, nitro, aminosulfonyl, hydroxy and an alkanoyloxy having 1 to 6 carbon atoms;
• provided that, (a) when l is 0, B is --CRR'-- (CH.sub.2).sub.p -- (wherein R and R' are each hydrogen, methyl or ethyl, and p is 0 or 1) and R.sup.1 is methyl, ethyl, n-butyl, cyclohexyl or an unsubstituted phenyl, R.sup.2 is other than hydroxy, or ethoxy, and (b) when l is 0, B is --CR"R'"--(CH.sub.2).sub.q -- (wherein R" and R'" are each hydrogen or methyl, and q is 0 or 1) and R.sup.1 is cyclohexyl, n-butyl or an unsubstituted phenyl, R.sup.2 is other than --NR.sup.3 'R.sup.4 ' (wherein one of R.sup.3 ' and R.sup.4 ' is hydrogen, methyl, ethyl or benzyl, and another one of them is hydrogen or ethyl);
• or a pharmaceutically-acceptable salt thereof.

An anti-ulcer composition which comprises, as an essential active ingredient, a therapeutically-effective amount of a tetrazole derivative of the formula:

• ##STR23## wherein R.sup.1 is hydrogen, an alkyl having 1 to 6 carbon atoms, a cycloalkyl having 3 to 12 carbon atoms or phenyl;
• l is 0;
• B is an alkylene having 1 to 6 carbon atoms;
• R.sup.2 is hydroxy, an alkoxy having 1 to 6 carbon atoms, or a group:
• ##STR24## wherein R.sup.3 and R.sup.4 are the same or different and are each hydrogen, an alkyl having 1 to 6 carbon atoms, a cycloalkyl having 3 to 12 carbon atoms, phenyl, a cycloalkyl-alkyl having 1 to 6 carbon atoms in the alkyl moiety and 3 to 8 carbon atoms in the cycloalkyl moiety, a phenylalkyl having 1 to 6 carbon atoms in the alkyl moiety or a hydroxyalkyl having 1 to 6 carbon atoms in the alkyl moiety;
• said cycloalkyl, phenyl and phenyl alkyl optionally have on the cycloalkyl or phenyl ring one or two substituents selected from the group consisting of an alkoxy having 1 to 6 carbon atoms, an alkyl having 1 to 6 carbon atoms, a halogen, an N,N-dialkylamino having 1 to 6 carbon atoms in each alkyl moiety, nitro, aminosulfonyl, hydroxy and an alkanoyloxy having 1 to 6 carbon atoms;
• provided that, (a) when l is 0, B is --CRR'--(CH.sub.2).sub.p -- (wherein R and R' are each hydrogen, methyl or ethyl, and p is 0 or 1) and R.sup.1 is methyl, ethyl, n-butyl, cyclohexyl or an unsubstituted phenyl, R.sup.2 is other than hydroxy or ethoxy and, (b) when l is 0, B is --CR"R'"--(CH.sub.2).sub.q -- (wherein R" and R'" are each hydrogen or methyl, and q is 0 or 1) and R.sup.1 is cyclohexyl, n-butyl or an unsubstituted phenyl, R.sup.2 is other than --NR.sup.3 'R.sup.4 ' (wherein one of R.sup.3' and R.sup.4' is hydrogen, methyl, ethyl or benzyl, and another of them is hydrogen or ethyl), or a pharmaceutically-acceptable salt thereof;
• in admixture with a pharmaceutically-acceptable diluent or carrier.