Toyama Chemical Co., Ltd.

Taisho Pharmaceutical Co., Ltd.

Fujifilm Corporation

Fujifilm Toyama Chemical Co., Ltd.

National Institute of Advanced Industrial Science and Technology

Tadashi Tanaka

Hiroki Urabe

Taro Kiyoto

Fumihito Ushiyama

Toshiya Noguchi

Yasuhiro Tsutsui

Junichi Ando

Masataka Fujino

Yasunobu Ushiki

Kentaro Furuya

Yasuko Kawaguchi

Hiromasa Horikiri

Mai Motono

Mai Yokotani

Daisuke Nakagawa

Hisaaki Chaki

Tohru Natsume

Yukihiko Aikawa

Hironori Kotsubo

Tatsuya Murakami

Shunichi Shiozawa

Shuichi Hirono

Takayuki Yamakawa

Issei Doi

Yusuke Okubo

Keiko Makita

Daisuke Kubo

Yoshitake Konishi

Kazunori Saeki

It is an object of the present invention to provide an antitumor agent, which is further excellent as a treatment agent used in the prevention and/or therapy of tumor associated with a bromodomain, and also to provide a bromodomain inhibitor, which is useful as a treatment agent for diseases or states associated with a bromodomain. An antitumor agent and a bromodomain inhibitor, comprising a compound represented by the following formula, have an excellent bromodomain inhibitory activity and are useful as treatment agents in the prevention and/or therapy of tumor associated with a bromodomain, and the like: 

Antitumor agent and bromodomain inhibitor

A compound represented by the general formula, or a salt thereof, has exceptional CXCL10 inhibitory activity and is useful as a treatment agent for the prevention and/or treatment, etc., of diseases involving overproduction of CXCL10. In the formula: Ris a Calkyl group, etc.; Ris a hydrogen atom, etc.; Ris a halogen atom, etc.; Z, Z, and Zare CH, etc.; Xis CONH, etc.; ring A is a phenyl group, etc.; Ris a halogen atom, etc.; and m is an integer of 0-5. 

Nitrogen-containing heterocyclic compound

Crystals of 5-cyclopropyl-2-((1-(3-fluorobenzyl)-1H-indol-5-yl)amino)nicotinic acid having diffraction peaks at diffraction angles (2&#x3b8;) of 12.2&#xb1;0.2, 17.2&#xb1;0.2, 19.4&#xb1;0.2, 24.1&#xb1;0.2, and 27.1&#xb1;0.2&#xb0; or diffraction angles (2&#x3b8;) of 12.9&#xb1;0.2, 15.5&#xb1;0.2, 21.2&#xb1;0.2, 21.7&#xb1;0.2, and 25.9&#xb1;0.2&#xb0; in powder x-ray diffraction have excellent stability, are easy to handle, and are useful as a drug substance of pharmaceuticals to be used in treatments such as the prevention or treatment of diseases involving keratinocyte hyperproliferation.

Crystals of 5-cyclopropyl-2-((1-(3-fluorobenzyl)-1H-indol-5-yl)amino)nicotinic acid

A novel amine derivative expressed by general formula (1) (in the formula: G, G, and Gare the same or different and represent CH or a nitrogen atom; Rrepresents a chlorine atom, an optionally-substituted Ccycloalkyl group, or the like; Rrepresents &#x2014;COOR(in the formula, Rrepresents a hydrogen atom or a carboxyl protective group), or the like; Rrepresents a hydrogen atom, or the like; and Rrepresents an optionally-substituted condensed bicyclic hydrocarbon group, an optionally-substituted bicyclic heterocyclic group, or the like), or a salt thereof is useful in procedures such as the treatment or prevention of conditions related to excessive keratinocyte proliferation.

Amine derivative or salt thereof

A nitrogen-containing heterocyclic compound or pharmaceutically acceptable salt thereof represented by the general formula: which have a potent antibacterial activity and a high safety. Thus, the compounds are useful as antibacterial agents against gram-positive bacteria, gram-negative bacteria and drug resistant bacteria.

Quinolinones and quinoxalinones as antibacterial composition

Disclosed is a compound represented by the general formula: wherein Rrepresents an aryl or heterocyclic group which may be substituted or the like; Xrepresents a C-Calkylene group or the like; X, Xand Xindependently represent NH, a bond or the like; Xrepresents a lower alkylene group, a bond or the like; Yrepresents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z, Z, Z, Z, Zand Zindependently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z, Z, Zand Zrepresents a nitrogen atom, or a salt thereof, which is useful as an antibacterial agent.

Heterocyclic compound or salt thereof and intermediate thereof

Quinoxalinones as antibacterial composition

Disclosed is a compound represented by the general formula: [wherein Rrepresents an aryl or heterocyclic group which may be substituted or the like; Xrepresents a C-Calkylene group or the like; X, Xand Xindependently represent NH, a bond or the like; Xrepresents a lower alkylene group, a bond or the like; Yrepresents a bivalent alicyclic hydrocarbon residue which may be substituted or a bivalent alicyclic amine residue which may be substituted; and Z, Z, Z, Z, Zand Zindependently represent a nitrogen atom, a group represented by the formula: CH, or the like, provided that at least one of Z, Z, Zand Zrepresents a nitrogen atom] or a salt thereof, which is useful as an antibacterial agent.

A benzophenone derivative represented by the following formula: wherein

Benzophenone derivatives or salts thereof

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Toyama, Japan

Tadashi Tanaka