Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Esai Co., Ltd.

Shuhei Miyazawa

Naoyuki Shimomura

Shigeru Souda

Shinya Abe

Isao Yamatsu

Hiroyuki Yoshimura

Hisashi Shibata

Tetsuya Kawahara

Koukichi Harada

Kazuo Okano

Osamu Asano

Takashi Yamanaka

Yoshimasa Machida

Mitsuaki Miyamoto

Kouichi Katayama

Kenzo Muramoto

Norihiro Ueda

Richard S Clark

Tsuneo Wakabayashi

Kazuo Hirota

Hideaki Fujisaki

Toshihiko Kaneko

Yorihisa Hoshino

Kouji Yamada

Tsutomu Kawata

Hiroshi Obaishi

Kiyoshi Oketani

Satoshi Katayama

Hajime Tsunoda

Junsaku Nagaoka

Takashi Mori

Yoshimori Sakuma

Seiichiro Nomoto

Katsuya Tagami

Makoto Okita

Manabu Murakami

Masatoshi Fujimoto

Junichi Nagakawa

Hitoshi Harada

Nobuhisa Watanabe

Takaaki Kameyama

Shigeki Hibi

Masato Ueda

Mitsuo Nagai

Kouichi Kikuchi

Masanori Mizuno

Tsutomu Yoshimura

Hiromasa Suzuki

Takeshi Suzuki

Ieharu Hishinuma

Atsuhiko Kubota

Takashi Inoue

Kenichi Chiba

Nobuyuki Yasuda

Ryoichi Hashida

Kaname Miyamoto

Toru Horie

Hidetoshi Kawashima

Naoko Nagaoka

Masahiro Yasuda

Kenichi Kusube

Fumihiro Ozaki

Yoshihiko Kotake

Norio Karibe

Kazuki Miyazaki

Hideyuki Adachi

Masanobu Shinoda

Itaru Tsukada

Atsushi Kamada

Hiroki Ishihara

Hiroshi Shirota

Tadashi Nagakura

Yoshimitsu Naoe

Kohtarou Kodama

Daisuke Iida

Hiroki Terauchi

Seiichi Kobayashi

Takayuki Hida

Yasuhiro Kabasawa

Kokichi Harada

Makoto Nakagawa

Hirsohi Shirota

Richar S Clark

Naoyuki Kimomura

Yorohisa Hoshino

Kotaro Kodama

A novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases is provided, which has an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where Rand Rmay be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; Rrepresents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R, R, Rand Rrepresent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and Wrepresents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.

Benzimidazole compound

A compound represented by the following general formula (1), or a salt or hydrate thereof: [Formula 1] wherein Rrepresents a C1-C6 alkyl group or C2-C6 alkynyl group which may be substituted, or a phenyl group which may be substituted, Rrepresents a hydrogen atom or a C1-C6 alkyl group, Rrepresents methyl or ethyl group, Rrepresents a C1-C6 alkyl group, Rrepresents a hydrogen atom, provided that a compound wherein Ris a C1-C6 alkyl group unsubstituted or substituted with a halogen atom and Ris a hydrogen atom is excluded.

Imidazopyridine compound

An object of the present invention is to provide a novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases, having an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by 

The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine Areceptor antagonism, preferably an adenosine Areceptor antagonism, or a salt thereof.

Medicinal compositions promoting bowel movement

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

A class of substituted compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), wherein R is selected from hydrido, halo, alkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R and R are one more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R and R is substituted with alkysulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.

2-aminopyridine compounds and use thereof as drugs

Phthalazine compounds and therapeutic agents for erectile dysfunction

Phthalazine derivatives and remedies for erectile dysfunction

Pyridine derivatives useful for preventing or treating peptic ulcers, pharmaceutical preparations and methods of treating peptic ulcers are described.

Pyridine derivatives having anti-ulcerative activity

To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## �wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, &gt;N--R.sup.6 or&gt;CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc-; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.

Aminobenzoic acid derivatives

Pyridine derivatives useful for preventing or treating peptic ulcers, pharmaceutical preparations and methods of treating peptic ulcers are disclosed.

To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## �wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, &gt;N--R.sup.6 or &gt;CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.

A pyridine compound having the formula is disclosed and useful to treat the peptic ulcer. ##STR1## wherein R.sup.1 and R.sup.2 which may be the same or different are each a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogenated lower alkyl group, or a halogen atom, R.sup.3 and R.sup.4 which may be the same or different are each a hydrogen atom or a lower alkyl group, X is a group represented by the formula --S--, a group represented by the formula ##STR2## or a group represented by the formula ##STR3## and n is an integer of 1 to 6, provided that R.sup.3 and R.sup.4 are not simultaneously hydrogen atoms when n is 1.

Pyridine derivative and therapeutic agent for ulcer comprising the same

To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## [wherein R.sup.1 represents a group represented by the formula ##STR2## etc., {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, &gt;N--R.sup.6 or &gt;CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5].

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Ibaraki, Japan

Shuhei Miyazawa