Mitsubishi Chemical Industries Limited

Mitsubishi Kasei Corporation

Issei Nitta

Akihiro Tobe

Shinichiro Fujimori

Kunihiro Ninomiya

Ryoji Kikumoto

Mamoru Sugano

Shinya Inoue

Kenichiro Nakao

Shuji Morita

Ken-Ichi Saito

Toshio Haruyama

Harukazu Fukami

Satoshi Yamazaki

Akira Maruyama

Motoyoshi Miyake

Tomoshi Yamazaki

Makoto Kawamura

Hiromi Okushima

Mitsuo Egawa

Rikizo Furuya

Hiroaki Ueno

Junko Takashima

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 4-piperidinecarboxamide derivatives represented by the general formula (I): ##STR1## wherein each R.sup.1 and R.sup.2 represents a hydrogen atom, or R.sup.1 together with R.sup.2 represents a cyclopentanespiro or cyclohexanespiro group; R.sup.3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an aralkyl group or an indolylalkyl group; and n is an integer of 1 or 2; is disclosed herein. The novel compound is useful as the agent for improving the impaired brain fuction.

4-piperidinecarboxamide derivatives

Novel 4-aminopyridine derivatives represented by the general formula (I): ##STR1## wherein A and B independently represent ##STR2## and n is an integer of 1 or 2; as well as their pharmaceutically acceptable acid addition salts are disclosed herein. The novel compounds are useful as the agent for improving impaired brain function.

4-aminopyridine derivatives for improving impaired brain function

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

A phenylpiperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or alkoxy group having 1 to 3 carbon atoms, or

Phenylpiperazine derivatives and their acid addition salts

This invention relates novel thieno[2,3-d]pyrimidine derivatives represented by the following general formula (I): ##STR1## or salts thereof; wherein R.sup.1 and R.sup.2 independently represent hydrogen, halogen or alkyl group having 1 to 6 carbon atoms; or R.sup.1 and R.sup.2 may concatenate to form a cycloalkylene group having 5 or 6 ring carbon atoms; R.sup.3 and R.sup.4 independently represent hydrogen or alkyl group having 1 to 6 carbon atoms; R.sup.5 represents a member selected from

Thieno[2,3-d]pyrimidine derivatives and salts thereof

A piperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1 is --OH, --OR.sup.3, --SR.sup.3, --SOR.sup.3 or --SO.sub.2 R.sup.3 wherein R.sup.3 is alkyl group having 1 to 3 carbon atoms;

Piperazine derivatives and their acid addition salts

Novel corticoid 17.alpha.-alkoxycarbonyl carboxylate derivatives are disclosed. These derivatives have strong topical anti-inflammatory activity and extremely weak systemic adverse reactions and are useful for the treatment of acute and chronic eczema, eczema seborrhoicorum, contact dermatitis, atopic dermatitis, asthma, etc.

Corticoid derivatives and process for production thereof

This is disclosed novel intermediates, i.e. 17.beta.-ethynylsteroids, which are useful for the preparation of corticoids such as hydrocortisone and prednisolone, and a process for preparing the same.

17.beta.-ethynylsteroids and process for preparing same

Novel 6-oxygenated corticoid 17.alpha.-carbonates are disclosed. These compounds have strong topical anti-inflammatory activity which are accompanied by extremely weak systemic adverse reaction. The present compounds are useful for the treatment of acute and chronic eczema, eczema seborrhoicorum, contact dermatitis, atopic dermatitis, asthma, etc.

6-oxygenated corticoid 17.alpha.-carbonates and process for production

There is disclosed novel intermediates, i.e. acyloxysteroids, which are useful for the preparation of corticoids such as hydrocortisone and prednisolone, and a process for producing the same.

Acyloxysteroids and process for producing same

A 4,6-dien-3-one steroid is produced by brominating an enolic ether of a 4-en-3-one steroid in a water-containing organic solvent which is substantially free from acetic acid and sodium acetate to give a 6-bromosteroid and then dehydrobrominating the 6-bromosteroid in a medium which contains dimethylformamide or N-methylpyrrolidone and 1 to 9% by volume of water.

Growing community of inventors

Machida, Japan

Issei Nitta