Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Masahiro Yasuda

Hitoshi Harada

Shuhei Miyazawa

Masato Ueda

Yoshihiko Kotake

Osamu Asano

Nobuyuki Yasuda

Seiichi Kobayashi

Hisashi Shibata

Junichi Nagakawa

Takayuki Hida

Yasuhiro Kabasawa

Daisuke Iida

Kokichi Harada

Makoto Nakagawa

Kazuo Hirota

A compound having excellent adenosine receptor (A, A, Areceptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, Rand R, same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an aromatic hydrocarbon cyclic group, an acyl group or an alkylsulfonyl group, which groups may be substituted (except the hydrogen atom); Rrepresents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, a nitrogen atom, an oxygen atom or a sulfur atom, which groups may be substituted (except the hydrogen atom, the halogen atom and the cyano group); Rrepresents an aromatic hydrocarbon cyclic group which may be substituted, and Rrepresents an aromatic hydrocarbon cyclic group which may be substituted.

Pyrimidine compound and medicinal composition thereof

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

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Ibaraki, Japan

Masahiro Yasuda