Eisai Company, Limited

Yasuhiro Kabasawa

Fumihiro Ozaki

Keiji Ishibashi

Toshiaki Ogawa

Norio Minami

Hideyuki Adachi

Takanori Kawamura

Hitoshi Oinuma

Takashi Hasegawa

Shigeru Souda

Kohtarou Kodama

Megumi Ikemori

Nobuhisa Watanabe

Hiroki Ishihara

Nobuyuki Mori

Hiroshi Katoh

Hideto Ohara

Kazutoshi Miyake

Masayuki Matsukura

Kazuki Miyazaki

Satoshi Katayama

Yasutaka Takase

Katsuhiro Moriya

Kohtaro Kodama

Manabu Shirato

Shinya Abe

Shuhei Miyazawa

Masato Ueda

Yoshihiko Kotake

Osamu Asano

Hitoshi Harada

Nobuyuki Yasuda

Masahiro Yasuda

Mayu Shibazaki

The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A, A, and Areceptors), particularly, compounds represented by the general formula (1), salts thereof, or solvates of both: (1) wherein Rand Rare each independently hydrogen, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, Ccycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a Caromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, Cacyl, or Calkylsulfonyl; Ris hydrogen, Calkyl, Calkenyl, or Calkynyl; Ris a Caromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and Ris a Caromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).

Pyrimidone compounds and pharmaceutical compositions containing the same

The present invnetion provides a remedy for erectile dysfunction. The active ingredient thereof is a fused pyridazine compound represented by the following formula (I) or a pharmacologically acceptable salt thereof:

Remedy for erection failure comprising fused pyridazine compound

Fused pyridazine compounds

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

To provide a novel cyclohexane derivative, a cyclohexane derivative is defined by the formula (I) or a pharmacologically acceptable salt thereof: ##STR1## (wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents hydrogen or lower alkyl; R.sup.3 represents optionally substituted aryl or optionally substituted heteroaryl; X represents oxygen or sulfur; and Y represents a group represented by the formula: ##STR2## or the like). The compound of the present invention is useful as a preventive and therapeutic agent for diseases against which a potassium channel opening action is efficacious.

Cyclohexane derivatives

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 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.

To provide a cyclohexane derivative defined by the formula (I) or a pharmacologically acceptable salt thereof: ##STR1## (wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents hydrogen or lower alkyl; R.sup.3 represents optionally substituted aryl or optionally substituted heteroaryl; X represents oxygen or sulfur; and Y represents a group represented by the formula: ##STR2## or the like). The compound of the present invention is useful as a preventive and therapeutic agent for diseases against which a potassium channel opening action is efficacious.

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

A butenoic acid compound is defined by the following formula: ##STR1## in which Z is O,S, vinylene or azomethyne, A is an alkylene and J is phenyl or etc. It is useful to treat the heart desease.

A butenoic acid compound is defined by the following formula: ##STR1## in which Z is O,S, vinylene or azomethyne, A is an alkylene and J is phenyl or etc. It is useful to treat the heart disease.

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Ibaraki, Japan

Yasuhiro Kabasawa