Astellas Pharma Gmbh

Seldar Pharma Inc.

Kotobuki Pharmaceutical Co Ltd

Itsuro Shimada

Kyoichi Maeno

Hiroyuki Hisamichi

Norio Seki

Tsukasa Ishihara

Takafumi Shimizu

Tomofumi Takuwa

Noriko Ishikawa

Yutaka Kondoh

Takahiro Matsuya

Takanori Koike

Akio Kamikawa

Kazuhiko Iikubo

Kazuo Kurosawa

Hartmut Greiner

Hiroshi Tomiyama

Susumu Yamaki

Takashi Sugane

Wataru Hamaguchi

Tomoaki Abe

Kazushi Watanabe

Takahiro Nigawara

Junji Miyata

Takeshi Suzuki

Yoshinori Iwai

Kazuyuki Kuramoto

Shigeki Kunikawa

Tomoyoshi Imaizumi

Takahiko Tobe

Michinori Akaiwa

Keisuke Arakawa

Takanobu Araki

Yoshiki Satake

Masashi Shimazaki

Tetsuya Kimizuka

Atsuyuki Kohara

Takuma Morita

Michael Arlt

Masaaki Hirano

Hirofumi Yamamoto

Takashi Furutani

Kenichi Onda

Hiroyuki Mano

Nobuaki Shindo

Eiji Kawaminami

Takatoshi Soga

Sadao Kuromitsu

Hisao Hamaguchi

Shunichiro Matsumoto

Isao Kinoyama

Kei Ohnuki

Tatsuhisa Takahashi

Takashi Shin

Toshiyuki Kusayama

Hiroki Fukudome

Maiko Iida

Shigetoshi Kikuchi

Nobuaki Shindou

Kazuhiko Osoda

Yukihiro Takemoto

Hideki Sakagami

[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

To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

Tetrahydroisoquinolin-1-one derivative or salt thereof

Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.

Diamino heterocyclic carboxamide compound

Compounds of formula (I): in which the variables are defined herein, are useful for the treatment of cancer in patients which express the EGFR T790M mutation.

Pyrazinecarboxamide compound

[Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). [Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.

The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, lung cancer, non-small cell lung cancer, small cell lung cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive cancer, EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive lung cancer, or EML4-ALK fusion polynucleotide-positive and/or mutant EGFR polynucleotide-positive non-small cell lung cancer, etc.

Di(arylamino)aryl compounds

It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by &#x2014;SO&#x2014;Rin a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.

Propane-1,3-dione derivative or salt thereof

The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

Triazole derivative

Growing community of inventors

Tokyo, Japan

Itsuro Shimada