Eisai Company, Limited

Hitachi, Ltd.

Hitachi Video Engineering, Incorporated

Eisai Chemical Co., Ltd.

Norio Minami

Fumihiro Ozaki

Kazutoshi Miyake

Hitoshi Oinuma

Toshiaki Ogawa

Yasuhiro Kabasawa

Keiji Ishibashi

Motosuke Yamanaka

Nobuyuki Mori

Tadao Shoji

Tomonori Hoshiko

Shizumasa Kijima

Yoshiharu Daiku

Kenichi Nomoto

Kohei Sawada

Takanori Kawamura

Hideyuki Adachi

Isao Yamatsu

Hiroshi Katoh

Yuichi Inai

Kimio Hamamura

Youji Yamagishi

Megumi Ikemori

Kenji Hayashi

Masayuki Matsukura

Toshiji Igarashi

Naoki Yoneda

Sachiyuki Hamano

Hiroki Ishihara

Noriyasu Hirose

Takashi Hasegawa

Chiaki Seki

Toshiyuki Matsuoka

Kohtarou Kodama

Takashi Musha

Kouzou Morita

Hiroshi Inoue

Takashi Yoshimura

Noriyoshi Iwata

Yuh Horikawa

Osamu Hiroshima

Toshio Matsunami

Hideto Ohara

Makoto Komatsu

Yoshimasa Machida

Isao Fukushima

Naoyuki Shimomura

Noritaka Kitazawa

Akiharu Kajiwara

Yoshiharu Yamanishi

Satoshi Nagato

Kohshi Ueno

Kozo Akasaka

Toshikazu Shimizu

Masahiro Yonaga

Yoshikage Nakajima

Masataka Ueno

Yuki Komatsu

Toshinobu Kunii

Kunizo Higurashi

Yuithi Inai

Mikio Takeda

Atsushi Nagaoka

Satoru Tanaka

Tomishige Yatsugi

Koichiro Ueda

Isao Nakagawa

Yoshimi Iso

Satoshi Katayama

Ken Furukawa

Hiroshi Shionoya

Yoji Yamagishi

Isao Akitake

Hiroshi Shirai

Mitsuya Sato

Tadashi Takamiya

Hiroshi Toeda

Hiroshi Nishimura

Yuuki Komatsu

Isao Yamatu

Masayuki Mathukura

A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof:

Biphenyl derivatives

A process is provided for the preparation of .alpha.-tocopherol. According to the process, a condensation reaction between trimethylhydroquinone and a specific phytol derivative or isophytol is conducted in the presence of any one of the following solvents:

Process for the preparation of .alpha.-tocopherol

A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.

Processes for the preparation of hydroquinone and benzoquinone

A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field. ##STR1##

Butenoic or propenoic acid derivative

The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];

Thioformamide 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 present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like]; Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.

Thioformamide derivatives having hypotensive activity

A butenoic acid compound of the following formula: ##STR1## in which Z is O, S, vinylene or azomethyne, A is an alkylene group and J is phenyl group, is a useful in treating heart disease.

Butenoic acid 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.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

Norio Minami