Yoshitomi Pharmaceutical Industries, Ltd.

Masao Abe

Tetsuya Tahara

Minoru Moriwaki

Michio Terasawa

Jun Inui

Tomio Muro

Hiroshi Mikashima

Toshio Seki

Hiroyuki Sato

Shuji Yuasa

Ester-substituted thienotriazolodiazepine compounds and pharmaceutical

A trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different, and respectively represent hydrogen, C.sub.1-10 alkyl, C.sub.2-5 alkanoyl, formyl, C.sub.1-4 alkoxy-carbonyl, amidino, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylcarbonyl, phenyl, phenylalkyl, benzoyl, naphthoyl, phenylalkoxycarbonyl, benzylidene, pyridylcarbonyl, piperidyl, pyrrolidylidene or piperidylidene which may be optionally substituted on the ring or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom form 5 to 6-membered cycle which may have oxygen atom, sulfur atom or optionally substituted nitrogen atom in the cycle, or together with the adjacent nitrogen atom form phthalimido, R.sup.3 represents hydrogen or C.sub.1-4 alkyl, R.sup.4 represents hydrogen or C.sub.1-4 alkyl, R.sup.5 represents hydrogen, hydroxy, C.sub.1-4 alkyl or phenylalkoxy. R.sup.6 represents hydrogen or C.sub.1-4 alkyl, A represents single bond, C.sub.1-5 straight chain alkylene, or alkylene which is substituted by C.sub.1-4 alkyl, n represents 0 to 1, an optical isomer thereof and a pharmaceutically acceptable acid addition salt thereof. These compounds possess antihypertensive activity, and coronary, cerebral and kidney circulation-improving activities and are useful as antihypertensive agents and agents for prevention and treatment of circulatory diseases.

Trans-4-amino(alkyl)-1-pyridylcarbamoylcyclohexane compounds and

2-alkyl thieno(triazolo)diazepine compounds and pharmaceutical uses

A thienotriazolodiazepine compound of the formula: ##STR1## wherein A is alkylene or substituted alkylene and each other symbol is as defined in the specification and a pharmaceutically acceptable acid addition salt thereof, and pharmaceutical uses thereof. Said compounds exhibit PAF-antagonistic activity and are useful for the prevention or treatment of various PAF-induced diseases.

PAF-antagonistic thienotriazolodiazepine compounds and pharmaceutical

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Buzen, Japan

Masao Abe