Mitsubishi Chemical Industries Limited

Mitsubishi Kasei Corporation

Mitsubishi Chemical Corporation

Mamoru Sugano

Akihiro Tobe

Ryoji Kikumoto

Issei Nitta

Kunihiro Ninomiya

Harukazu Fukami

Shinichiro Fujimori

Yasuhiro Morinaka

Tomoko Bessho

Kunihiro Ninomiya, Deceased

Haruko Harada

Satoshi Yamazaki

Ken-ichi Saito

Hiroto Hara

Kenichiro Nakao

Tomoshi Yamazaki

Makoto Kawamura

Shuji Morita

Ken-Ichi Saito

Ryozo Yamaguchi

Tadashi Oohama

Ken-ichi Sato

A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

4-Acylaminopyridine derivative

4-acylaminopyridine derivative

There are disclosed a 9-acylamino-tetrahydroacridine derivative represented by the following formula (I): ##STR1## wherein R ##STR2## are as defined in the specification, its optical antipode or pharmaceutically acceptable acid addition salt thereof and a memory enhancing agent containing the same as an active ingredient.

9-acylamino-tetrahydroacridine derivatives and memory enhancing agent

Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piperazino group, imidazolyl group 4-alkyl substituted imidazolyl group or substituted amino group,

Ethanone oximes and pharmaceutical compositions thereof

Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piparazino group, imidazolyl group, 4-alkyl substituted imidazolyl group or substituted amino group,

A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylkene; Y is -(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.3 hydroxyalkyl or phenyl; or a pharmaceutically acceptable salt thereof is disclosed. The compound has anti-ulcer effect.

Arylsulfone compounds as anti-ulcer agents

A novel sulfone compound represented by the general formula (I) ##STR1## wherein R.sup.1 is cyclohexyl, phenyl; or a phenyl substituted with a group selected from nitro, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are respectively hydrogen, halogen, cyano or carbonyl, wherein R.sup.1 and R.sup.2 may form an o-phenylene or an o-phenylene substituted with at least one group selected from nitro C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and halogen; X is oxygen or methylene; Y is --(CH.sub.2).sub.n --, wherein n is an integer of 0, 5 or 6, or ##STR2## wherein m is an integer 1-3; R.sup.6 is hydrogen, C.sub.1 -C.sub.3 alkyl, .omega.-alkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms, or .omega.-dialkylaminoalkyl, wherein each alkyl has 1-3 carbon atoms; R.sup.7 is hydrogen or C.sub.1 -C.sub.3 alkyl; and R.sup.6 and R.sup.7 may form a ring together with N, or ##STR3## wherein R.sup.8 is hydrogen, C.sub.1 -C.sub.3 hydroxyalkyl or phenyl; or a pharmaceutically acceptable salt thereof is disclosed. The compound has anti-ulcer effect.

O-aminoalkylene (or aminoalkyleneoxy) phenylsulfone compounds having

Alkylenedioxybenzene derivatives are prepared and found to be useful as pharmaceutical agents, particularly as hypotensives.

Alkylenedioxybenzene and acid addition salts thereof useful as

Alkylenedioxybenzene derivatives and acid addition salts thereof

(3-Aminopropoxy)bibenzyl derivatives are prepared and found useful as pharmaceutical agents, particularly as inhibitors of platelet aggregation.

Pharmaceutically active (3-cyclic aminopropoxy)bibenzyls as inhibitors

Pharmaceutically active (3-aminopropoxy)bibenzyl derivatives

17-Ketals of 3-alkoxyestra-2,5(10)-dien-17-ones are prepared by reacting 17-ketals of 3-alkoxyestra-1,3,5(10)-trien-17-ones with sodium or potassium, liquid ammonia and a tertiary alcohol in the presence of an alicyclic hydrocarbon and/or an aliphatic hydrocarbon, and a solvent selected from the group consisting of tetrahydrofuran, dioxane and tetrahydropyran. Yield and selectivity of this reaction are improved by using the 17-ketal of the 3-alkoxyestra-1,3,5(10)-trien-17-one, sodium or potassium, liquid ammonia and the solvent in such proportions that the 17-ketal of the 3-alkoxyestra-1,3,5(10)-trien-17-one is substantially dissolved in the reaction system and that two liquid phases are formed, the lower phase being colored.

Process for producing 17-acetals of 3-alkoxyestra-2,5 (10)-dien-17-ones

Growing community of inventors

Kawasaki, Japan

Mamoru Sugano