Eisai Company, Limited

Sachiyuki Hamano

Norio Minami

Kazutoshi Miyake

Hitoshi Oinuma

Masayuki Matsukura

Naoki Yoneda

Yoshiharu Daiku

Hiroki Ishihara

Toshihiko Naito

Kenichi Nomoto

Nobuyuki Mori

Takashi Hasegawa

Toshiyuki Matsuoka

Tadanobu Takamura

Takashi Musha

Osamu Hiroshima

Hachiro Sugimoto

Shinichi Kitamura

Takaharu Nakamura

Toshiji Igarashi

Tadao Shoji

Yoshikage Nakajima

Tamotsu Kanazawa

Shin-ichi Kitamura

Takeru Kaneko

Mitsumasa Shino

Takeshi Uzuo

A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.

Benzenesulfonamide derivatives

The biphenylmethane derivative having the formula (I) is useful to prevent and treat hypertension and cardiac failure. ##STR1## in which R1 is hydrogen, an alkyl, a cycloalkyl, a halogenated alkyl, --S--R7, --SO2--R7, --C.tbd.C--R7 or --(CH2)p--OR7, R7 being hydrogen, an alkyl, a cycloalkyl or a halogenated alkyl, p being zero or 1, --A1=A2--A3=A4-- is --CH=CH--CH=CH--, --N=CH--CH=CH--, --CH=N--CH=CH--, --CH=CH--N=CH--, --CH=CH--CH=N-- or --CH=N--CH=N--, R2 and R3 are each hydrogen, a halogen, a lower alkyl, a lower alkoxy, a carbamoyl or cyano, R4 is hydrogen or a lower alkyl, R5 is 1H-tetrazol-5-yl, carboxyl (--COOH) or a carboxylic ester and R6 is hydrogen, a halogen, hydroxyl or a lower alkoxy, or a pharmacologically acceptable salt thereof.

Biphenylmethane derivative and pharmacological use

The biphenylmethane derivative having the formula (I) is useful to prevent and treat hypertension and cardiac failure. ##STR1## in which R1 is hydrogen, an alkyl, a cycloalkyl, a halogenated alkyl, --S--R7, --SO2--R7, --C.tbd.C--R7 or --(CH2)p--OR7, R7 being hydrogen, an alkyl, a cycloalkyl or a halogenated alkyl, p being zero or 1, --A1.dbd.A2--A3.dbd.A4-- is --CH.dbd.CH--CH.dbd.CH--, --N.dbd.CH--CH.dbd.CH--, --CH.dbd.N--CH.dbd.CH--, --CH.dbd.CH--N.dbd.CH--, --CH.dbd.CH--CH.dbd.N-- or --CH.dbd.N--CH.dbd.N--, R2 and R3 are each hydrogen, a halogen, a lower alkyl, a lower alkoxy, a carbamoyl or cyano, R4 is hydrogen or a lower alkyl, R5 is 1H-tetrazol-5-yl, carboxyl (--COOH) or a carboxylic ester and R6 is hydrogen, a halogen, hydroxyl or a lower alkoxy, or a pharmacologically acceptable salt thereof.

The biphenylmethane derivative having the formula (I) is useful to prevent and treat hypertension and cardiac failure. ##STR1## in which R1 is hydrogen, an alkyl, a cycloalkyl, a halogenated alkyl, --S--R7, --SO2--R7, --C.tbd.C--R7 or --(CH2)--OR7, R7 being hydrogen, an alkyl, a cycloalkyl or a halogenated alkyl, p being zero or 1, --A1.dbd.A2--A3.dbd.A4-- is CH.dbd.CH--CH.dbd.CH--, --N.dbd.CH--CH.dbd.CH--, --CH.dbd.N--CH.dbd.CH--, --CH.dbd.CH--N.dbd.CH--, --CH.dbd.CH--CH.dbd.N-- or --CH.dbd.N--CH.dbd.N--, R2 and R3 are each hydrogen, a halogen, a lower alkyl, a lower alkoxy, a carbamoyl or cyano, R4 is hydrogen or a lower alkyl, R5 is 1H-tetrazol-5-yl, carboxyl (--COOH) or a carboxylic ester and R6 is hydrogen, a halogen, hydroxyl or a lower alkoxy, or a pharmacologically acceptable salt thereof.

Solid oral preparation containing a pyrrolidine derivative with a

Derivatives of theophylline substituted at the 7 position with various substituents containing a homopiperazine nucleus. The compounds can be prepared reacting theophylline or reactive intermediate containing same with a homopiperazine compound. The compounds exhibit antihistaminic activity and vasodilating activity.

Theophylline derivatives

There are disclosed theobromine derivatives wherein theobromine is substituted at the 1 position with substituted piperazino, homopiperazino and piperidino groups, and pharmacologically acceptable acid addition salts thereof. The compounds exhibit vasodilating and psychotropic and analgesic activities.

Theobromine derivatives

Derivatives of 2-substituted-cyclohexane-1,3-diones possessing antihypertensive activity.

Cyclohexane derivatives, process for preparation thereof and medicines

New furo[2, 3d]pyrimidine derivatives of the general formula: ##STR1## wherein R.sub.1 represents a lower alkyl, a lower alkenyl or an aralkyl group, and R.sub.2 represents a lower alkyl, unsubstituted phenyl, carboxyl, methylsulphonyl, methoxycarbonyl or a nitro-substituted phenyl group, or the corresponding pharmacologically acceptable acid addition salts. The new compounds exhibit the outstanding anti-ulcer, anti-inflammatory and anti-edema effects.

Furo[2, 3d]pyrimidine derivatives and anti-ulcer containing the same

Bis-(meta-amidinophenoxy)-compounds and pharmacologically acceptable acid addition salts thereof, having excellent antifungal, antibacterial and anti-trichomonal activities.

Bis-(meta-amidinophenoxy)-compounds and pharmacologically acceptable

New 4-aminopyrimidium derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.2 each represents a hydrogen atom or a lower alkyl group, and R.sub.3 and R.sub.4 each represents a hydrogen or halogen atom, a lower alkyl, a lower alkoxyl, a lower alkoxycarbonyl, a lower alkylsulfonyl, nitro or amino group, and X represents a halogen atom, as well as a process for the preparation thereof. The compounds are useful as anti-inflammatory, analgesic agents without producing gastrointestinal trouble.

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Kanagawa, Japan

Sachiyuki Hamano