Kyowa Hakko Kogyo Co., Ltd.

Millennium Pharmaceuticals Limited

Kyowa Hakko Kirin Co., Limited

Kyowa Hakko Kogyo K.k.

Yuji Nomoto

Michio Ichimura

Kenji Matsuno

Shoji Oda

Shinichi Ide

Eiji Tsukuda

Tetsuji Ohno

Robert M Scarborough

Anjali Pandey

Junko Sasaki

Takao Nakajima

Yoshisuke Nakasato

Noriaki Uesaka

Shigeki Fujiwara

Masamori Sugawara

Junko Irie

Haruki Takai

Shin-ichi Uchida

Koji Yamada

Kazuhiro Kubo

Hiroshi Kase

Tadashi Hirata

Satoshi Nakanishi

Daisuke Machii

Hideaki Kusaka

Kimihisa Ueno

Yoshihisa Ohta

Yasuo Onoda

Iwao Kinoshita

Tomoko Ishikawa

Ken Nagashima

Kotaro Takasaki

Hiroshi Yano

Akira Ogawa

Shin-ichi Ide

Chiharu Nakagawa

Shin-Ichi Uchida

Method of treating central nervous systems disease by administering wherein n is an integer of from 0 to 3; Ris a 5-membered aromatic heterocyclic group containing at least one oxygen atom; Ris &#x2014;COR(wherein Ris aryl); Ris hydrogen or lower alkyl; and Rrepresents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R, R, Rand Rare individually optionally substituted.

Thiazole derivatives

Wherein n is an integer of from 0 to 3; Ris a 5-membered aromatic heterocyclic group containing at least one oxygen atom; Ris &#x2014;COR(wherein Ris aryl); Ris hydrogen or lower alkyl; and Rrepresents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R, R, Rand Rare individually optionally substituted. 

The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

Quinazoline derivatives as kinase inhibitors

Nitrogenous heterocyclic compounds

(Wherein n is an integer of from 0 to 3; Ris substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; Ris halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, &#x2014;COR, or the like; Rand Rmay be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, &#x2014;COR, or the like) For example, provided are adenosine Areceptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like. 

The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomeruloscierosis.

A condensed purine derivative represented by Formula (I):wherein X&#x2014;Y-Z represents RN&#x2014;C&#x2550;O or N&#x2550;C&#x2014;W, Rrepresents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, Vrepresents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, Vrepresents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when Vrepresents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X&#x2014;Y-Z represents RN&#x2014;C&#x2550;O and Rrepresents a substituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted alicyclic heterocyclic group, a halogen atom, a lower alkylthio group, &#x2014;NRR, &#x2014;COH, a lower alkoxycarbonyl group, &#x2014;COHal, &#x2014;CONRRor &#x2014;CHO, Vmay represent a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group; or a pharmacologically acceptable salt thereof.

Fused purine derivatives

The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

Nitrogenous heterocylic compounds

Nitrogen-containing heterocyclic compounds

1,3 diazines with platelet-derived growth factor receptor inhibitory activity

Growing community of inventors

Shizuoka, Japan

Yuji Nomoto