Sankyo Company, Limited

Ube Industries, Inc.

Keiichi Tabata

Yoshio Iizuka

Atsusuke Terada

Kazuo Hasegawa

Kazuyuki Wachi

Hachio Miyazawa

Koichi Kojima

Yasushi Takahashi

Tomio Kimura

Kazuo Koyama

Sadao Ishihara

Hiroshi Fujiwara

Nobuyoshi Iwata

Hiroshi Fukumi

Mitsuo Sugiyama

Shigeki Miyake

Nobuhiko Shibakawa

Shigeo Amemiya

Keiji Matsunobu

Etsuro Itoh

Hachio Miyazwa

Yoshimi Fujihara, Deceased

Mitsuko Makino

Pyrrolopyridazine derivatives having the general formula. ##STR1## In the above formula, R.sup.1 represents a C.sub.2 -C.sub.6 alkenyl-group, a halogeno-C.sub.2 -C.sub.6 -alkenyl group, a C.sub.6 -C.sub.10 aryl-C.sub.2 -C.sub.6 -alkenyl group, a C.sub.2 -C.sub.6 alkynyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.6 -alkyl group, a C.sub.5 -C.sub.7 cycloalkenyl-C.sub.1 -C.sub.6 -alkyl group or a halogeno-C.sub.1 -C.sub.6 -alkyl group; R.sup.2 and R.sup.3 are the same or different and each represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.6 -C.sub.10 aryl group; R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.5 represents a C.sub.6 -C.sub.10 aryl group or a 5-10 membered heteroaryl group comtaining heteroatom(s) selected from nitrogen, oxygen and sulfur;

Pyrrolopyridazine derivatives

A method for the treatment or prevention of an ulcerative disease comprising administering to a patient an effective amount of an active compound in admixture with a pharmacologically acceptable carrier or diluent, wherein said active compound is a thia-or oxazolidinone compound of the following formula or a pharmacologically acceptable salt thereof: ##STR1## wherein W is sulfur or oxygen and X is --N(R.sup.3)--, or X is sulfur or oxygen and W is --N(R.sup.3)--; R.sup.3 is hydrogen, C.sub.1 -C.sub.6 alkyl or aralkyl; R.sup.4 and R.sup.5 are the same or different and each is hydrogen, C.sub.1 -C.sub.6 alkyl,aralkyl, aryl, 5- or 6-membered aromatic heterocyclic; R.sup.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or aralkyl; and A is C.sub.2 -C.sub.6 alkylene.

Method for treating or preventing ulcerative diseases by administering

Described herein are of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Use of imidazopyrazole derivatives as analgesics and anti-inflammatory

Described herein are compounds of formula (I): ##STR1## �in which: R.sup.1 and R.sup.2 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl, aromatic heterocyclic, cyano or halogen; R.sup.3 is hydrogen, optionally substituted alkyl, aralkyl or acyl; R.sup.4 and R.sup.5 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl or aromatic heterocyclic!; and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Use of imidazopyrazole derivatives as analgesics anti-inflammatory agents

Described herein are compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Compounds of formula (I): ##STR1## [wherein: R.sup.1 is a cyclic amino group, or a dialkylamino group; R.sup.2 a group of formula --NHCHR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are each alkyl aryl or aralkyl, or together form a cycloalkyl group, or R.sup.2 is an aromatic heterocyclic group, or a group of formula --B--S(O).sub.m --R.sup.5 wherein R.sup.5 is a substituted alkyl group, or an aromatic heterocyclic group; B is an alkylene or alkylidene group; m is 0, 1 or 2; A is a group of formula --CH.dbd.CH-- or --(CH.sub.2).sub.n --, where n is 1, 2 or 3]; and salts thereof have valuable anti-ulcer activity.

Anti-ulcer pyridyloxy derivatives, their preparation and uses

Compounds of formula (I): ##STR1## [in which: R.sup.1 and R.sup.2 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl, aromatic heterocyclic, cyano or halogen; R.sup.3 is hydrogen, optionally substituted alkyl, aralkyl or acyl; R.sup.4 and R.sup.5 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl or aromatic heterocyclic]; and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.

Prostaglandin derivatives having an oxo group at specified positions in the .alpha. side chain have a variety of physiological effects, notably a strong anti-ulcer activity accompanied by a limited ability to inhibit blood platelet aggregation.

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Tokyo, Japan

Keiichi Tabata