Yamanouchi Pharmaceutical Company Ltd.

Other

Ludwig Institute for Cancer Research Limited

Imperial Cancer Research Technology, Ltd.

Astellas Pharma Gmbh

Ferring B.v.

Ferring-research Limited

Mitsuaki Ohta

Keiji Miyata

Minoru Okada

Masahiko Hayakawa

Hiroyuki Kaizawa

Koyo Matsuda

Mayumi Yamano

Tomonobu Koizumi

Ken-Ichi Kawaguchi

Hiroyuki Moritomo

Isao Yanagisawa

Takeshi Suzuki

Akira Matsuhisa

Graeme Semple

Masato Satoh

Michael Szelke

Akito Nishida

Tokuo Koide

Hamish Ryder

Hiroyuki Ito

Hiroyuki Koshio

Junya Ohmori

Kiyoshi Iwaoka

David Alan Kendrick

Jun-ya Ohmori

Noriko Ishikawa

Masaaki Hirano

Takashi Kamikubo

Eiji Kawaminami

Isao Kinoyama

Masakazu Imamura

Akira Toyoshima

Nobuaki Taniguchi

Hirotsune Itahana

Yoji Miyazaki

Hideki Anan

Hiroshi Koutoku

Kenichi Kazuta

Naoki Imanishi

Eisuke Nozawa

Masato Ishii

Kiyohiro Samizu

The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

Fused heteroaryl derivatives

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

The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo&lsqb;1,2-a&rsqb;pyridin-3-yl) derivatives or salts thereof exhibit an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity, and are thus useful as medicaments, especially as PI3K inhibitors and antitumor agents.

Imidazopyridine derivatives

A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein (a) R.sup.1 is --CH.sub.2 CHOH(CH.sub.2).sub.a R.sup.4 or a ketone group --CH.sub.2 CO(CH.sub.2).sub.a R.sup.5 in which a is 0 or 1 and R.sup.4 and R.sup.5 are selected from alkyl and cycloalkyl groups and saturated heterocyclic groups optionally substituted at a hetero-atom; (b) R.sup.2 and R.sup.3 are independently selected from aromatic carbocyclic and heterocylic residues; and (c) W and X are selected independently from halogen and hydrogen atoms and alkyl and alkoxy groups. These compounds are gastrin and/or CCK-B receptor antagonists. ##STR1##

Benzodiazepin derivatives useful as CCK-receptor antagonists

5-HT.sub.3 receptor agonist, novel thiazole derivative and intermediate

Process of preparing benzodiazepine compounds useful as antagonists of

Benzodiazepine derivatives useful as CCK-receptor antagonists

A novel thiazole derivative represented by general formula (I), which has a selected agonistic activity for 5-HT.sub.3 receptor, a pharmaceutical composition thereof, and a process for producing the same. In the said formula, R.sup.1 represents hydrogen or lower alkoxy; R.sup.2 and R.sup.3 are such that R.sup.2 represents hydrogen and R.sup.3 represents a group, --Y--Het, wherein Y represents a single bond or lower alkylene and Het represents a nitrogenous heterocyclic group, or alternatively R.sup.2 and R.sup.3 are combined together to form a group, --(CH.sub.2).sub.m --NR.sup.4 --(CH.sub.2).sub.n --, wherein m and n are each 1 or 2 and R.sup.4 represents lower alkyl; and X represents --NH--, --NHC(.dbd.O)NH--, --C(.dbd.O)NH-- or --NHC(.dbd.O)--.

Thiazole derivatives

Growing community of inventors

Ibaraki, Japan

Mitsuaki Ohta