Other

Yamanouchi Pharmaceutical Company Ltd.

Ludwig Institute for Cancer Research Limited

Imperial Cancer Research Technology, Ltd.

Astellas Pharma Gmbh

Koyo Matsuda

Minoru Okada

Masahiko Hayakawa

Mitsuaki Ohta

Hiroyuki Kaizawa

Mayumi Yamano

Ken-Ichi Kawaguchi

Tomonobu Koizumi

Hiroyuki Moritomo

Noriki Ito

Yuichi Iizumi

Kiyoshi Iwaoka

Noriko Ishikawa

Tsukasa Ishihara

Masahiko Isaka

Seiichi Hashimoto

Teruhiko Shimokawa

Satomi Nishijima

Hiroshi Moritani

Hirotoshi Kakuta

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

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

Pharmaceutical compositions having a cholesterol-lowering effect which comprises as the active ingredient a compound having a PPAR (peroxisome proliferator-activated receptor)&dgr; activating effect or a PPAR&dgr;- and PPAR&ggr;-activating effect or a pharmaceutically acceptable salt thereof; pharmaceutical compositions wherein the cholesterol-lowering effect is an LDL-cholesterol-lowering effect; and a method for identifying a compound having a cholesterol-lowering effect characterized by measuring the PPAR&dgr;-activating effect or the PPAR&dgr;- and PPAR&ggr;-activating effect thereof. Means for Solution: It is found out that a compound exerting an excellent cholesterol-lowering effect on higher animals such as humans and ape has an effect of activating PPAR&dgr; or PPAR&dgr; and PPAR&ggr;. Also, a method for identifying a compound having an excellent cholesterol-lowering effect was found, wherein the desired compound can be quickly and efficiently screened from among a number of compounds by measuring the PPAR&dgr;-activating effect or the PPAR&dgr;- and PPAR&ggr;-activating effect.

Medicinal compositions with cholesterol-lowering effect

Quinuclidine derivative having tricyclic hetero condensed ring

Urea derivatives of the general formula (I) ##STR1## and salts thereof, pharmaceutical compositions containing the same, and methods for producing the same are-disclosed. The urea derivatives of the general formula (I) and salts thereof are novel compounds having the acyl-CoA cholesterol acyltransferase (ACAT) inhibiting activity.

Urea derivatives and salts thereof

Urea derivatives of the general formula (I) ##STR1## and salts thereof, pharmaceutical compositions containing the same, and methods for producing the same are disclosed. The urea derivatives of the general formula (I) and salts thereof are novel compounds having the acyl-CoA cholesterol acyltransferase (ACAT) inhibiting activity.

Urea derivatives and salts thereof in method for inhibiting the ACAT

Growing community of inventors

Tsukuba, Japan

Koyo Matsuda