Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Takashi Musha

Toshiyuki Matsuoka

Norio Minami

Kazutoshi Miyake

Masayuki Matsukura

Naoki Yoneda

Sachiyuki Hamano

Hiroki Ishihara

Nobuyuki Mori

Osamu Hiroshima

Richard S Clark

Tetsuya Kawahara

Mitsuaki Miyamoto

Fumihiro Ozaki

Kazuo Okano

Nobuaki Sato

Akiharu Kajiwara

Ieharu Hishinuma

Tsutomu Kawata

Masanobu Shinoda

Hiroshi Tanaka

Fumiyoshi Matsuura

Itaru Tsukada

Atsushi Kamada

Makoto Kotake

Taro Terauchi

Yoshimitsu Naoe

Shuichi Suzuki

Motoji Kogushi

Osamu Ito

Akifumi Kimura

Hiroko Kobayashi

Naoto Ono

Ken-ichi Chiba

Yoshiaki Oohashi

Syuhei Miyazawa

Ken-Ichi Chiba

A 2-iminoimidazole derivative represented by the formula: {wherein R, Rand Rrepresent hydrogen, optionally substituted Calkyl, etc.; Rrepresents hydrogen, Calkyl, Calkyloxycarbonyl, etc.; Yrepresents a single bond, &#x2014;CH&#x2014;, etc.; Yrepresents a single bond, &#x2014;CO&#x2014;, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R&#x2013;Rrepresent hydrogen, Calkyl, hydroxyl, Calkoxy, etc., and Rand Ror Rand Rmay bond together to form a 5- to 8-membered heterocycle], etc.}or salt thereof.

2-iminoimidazole derivatives (2)

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.

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Ibaraki, Japan

Takashi Musha