Astellas Pharma Gmbh

Takahiro Nigawara

Masahiko Hayakawa

Junji Sato

Shigeru Yoshida

Hiroyuki Moritomo

Takanori Koike

Susumu Yamaki

Kenji Negoro

Itsuro Shimada

Kenichi Onda

Fumiyuki Shirai

Yutaka Nakajima

Yasuhiro Yonetoku

Sunao Imada

Keita Nakanishi

Tomoaki Abe

Kazushi Watanabe

Kazuhiko Iikubo

Shigeki Kunikawa

Tomoyoshi Imaizumi

Kazuyuki Kuramoto

Shohei Shirakami

Keisuke Arakawa

Michinori Akaiwa

Daisuke Sasuga

Takanobu Araki

Takahide Ohishi

Yoshiki Satake

Yuji Takasuna

Naohiro Aoyama

Kaori Kubo

Masashi Shimazaki

Akira Kanai

Mitsuaki Okumura

Nobuaki Amino

Yoshiyuki Kido

Keisuke Maki

[Problem] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.

Quinazoline compound

On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. It was found that a nitrogen-containing bicyclic heterocyclic compound has an excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has an cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.

Nitrogen-containing bicyclic aromatic heterocyclic compound

[Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.

Phenylacetamide compounds of the formula having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide have an excellent glucokinase activation action.

Substituted pyrazine compounds

The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom within said ring is optionally substituted with one or more groups selected from the group consisting of lower alkyl, &#x2014;O-(lower alkyl), halogen atom, carboxyl, &#x2014;CO-(lower alkyl), and carbamoyl, Rrepresents: (1) phenyl substituted with at least three halogen atoms, which may have at least one additional substituent, or (2) cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl, each of which is optionally substituted; and Rrepresents a group represented by formula (II) or an optionally substituted cyclic amino: wherein Rand Rmay be identical or different and each represents &#x2014;H, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, phenyl, heteroaryl, non-aromatic heterocyclyl, or &#x2014;O-(lower alkyl), each of which is optionally substituted.

Pyrimidine derivative condensed with a non-aromatic ring

There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingredient. These compounds exhibit excellent promoting activity on insulin secretion and activity against hyperglycemia. Hence, the pharmaceutical compositions comprising such compounds as active ingredients, based on these actions, are useful for treating and/or preventing insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes), insulin-resistant diseases, obesity, and the like.

Aromatic-ring-fused pyrimidine derivative

Growing community of inventors

Tokyo, Japan

Takahiro Nigawara