Yamanouchi Pharmaceutical Company Ltd.

Astellas Pharma Gmbh

Nobuaki Taniguchi

Akira Matsuhisa

Akihiro Tanaka

Minoru Okada

Hiroyuki Koshio

Takeyuki Yatsu

Masakazu Imamura

Isao Kinoyama

Ken-ichiro Sakamoto

Masahiko Hayakawa

Hiroyuki Kaizawa

Takashi Furutani

Kenichi Kawaguchi

Atsuki Yamazaki

Takenori Kimura

Masaaki Hirano

Takashi Kamikubo

Hiroyuki Moritomo

Mitsuaki Ohta

Eiji Kawaminami

Akira Toyoshima

Yoji Miyazaki

Kiyohiro Samizu

Eisuke Nozawa

Hiroshi Koutoku

The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.

N-phenyl-(2R,5S)dimethylpiperazine derivative

N-phenyl-(2R,5S) dimethylpiperazine derivative

This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.

Cyanophenyl derivative

This invention relates to nitrogen-containing aromatic 5-membered ring-condensed benzazepine derivatives represented by the general formula (I) ##STR1## (symbols in the formula have the following meanings; ring B: a nitrogen-containing aromatic 5-membered ring having at least 1 nitrogen atom and optionally one oxygen or sulfur atom, which may optionally have substituent(s), R.sup.1 and R.sup.2 : these may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group which may optionally be substituted by lower alkyl group(s), or a lower alkoxy group,

Condensed benzazepine derivative and pharmaceutical composition thereof

Benzazepine derivatives represented by the following general formula (I) useful as arginine vasopressin antagonists or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and difluorobenzazepinone derivatives represented by the following general formulae (II) and (III) which are useful as production intermediates of the compound (I). ##STR1##

Benzazepine derivative, pharmaceutical composition thereof, and

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Tsukuba, Japan

Nobuaki Taniguchi