Daiichi Pharmaceutical Co., Ltd.

Daiichi Sankyo Company, Limited

Hitoshi Ohki

Makoto Takemura

Kenichi Kimura

Hisashi Takahashi

Rie Miyauchi

Youichi Kimura

Katsuhiro Kawakami

Masahiro Ota

Nobuyuki Suzuki

Hiroyuki Naito

Yoshihiro Shibata

Akio Ejima

Satoru Ohsuki

Yasusi Ueda

Masahiro Ikeda

Kazuyuki Sugita

Satoru Miyauchi

Shinji Matuura

Toshiyuki Nakanishi

Tooru Okayama

Hideaki Watanabe

Toshiyuki Takeda

Hidekazu Inoue

Yuichi Tominaga

Katsuhiro Kobayashi

Takeshi Jimbo

Daisuke Fukatsu

Junya Kawai

Haruko Kawato

Norikazu Matsuhashi

Keijiro Kobayashi

Akitake Yamaguchi

Kosuke Takeuchi

Chie Makino

Tadashi Toki

Provided is a novel compound or a salt thereof inhibiting MTHFD2 and useful for treating a disease caused by overexpression of MTHFD2, a disease involved in overexpression of MTHFD2 and/or a disease associated with overexpression of MTHFD2. Solution Provided is a sulfonamide derivative having a coumarin skeleton represented by the following formula (I) and having various substituents: wherein R, R, R, R, R, Rand Rare the same as defined in the specification,and a salt thereof.

Sulfonamide derivative having coumarin skeleton

Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R, R, R, R, R, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.

Pyridone derivatives

To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.

Crystal of a free tricyclic pyrazolopyrimidine derivative

A pyrazolopyrimidine compound represented by formula (1) that inhibits the function of HSP90 as a chaperone protein and that has antitumor activity, a medicament comprising a compound represented by formula (1), a pharmaceutical composition comprising a compound represented by formula (1), and a method for treating cancer using a compound represented by formula (1). 

Tricyclic pyrazolopyrimidine derivatives

Cis-substituted fluoromethylpyrrolidine derivative

Tricyclic amine derivatives

This invention provides compounds having antitumor effect, namely a compound represented by the following formula (I) or (Ia) having various substituents in which G and G are condensed tricyclic heterocyclic rings or salts thereof, and a compound represented by the following formula (Ib) having various substituents or salts thereof.

Pyrazole derivatives and salts thereof

Pyrazole derivatives

The present invention provides an antibacterial compound useful as medicines, animal drugs, fisheries drugs or antibacterial preservatives and to an antibacterial agent or preparation which contains the same, more particularly a compound which possesses high safety and excellent activity against a broad range of bacterial species including quinolone-resistant strains. A quinolone derivative of the following formula (I) which has a group derived from the heterocyclic spiro-compound at the 7-positioned R and the halogenocyclopropyl group at the N -position, prefereably a compound of pure isomer, and an antibacterial agent containing the derivative compound.

Heterocyclic spiro-derivative

A quinolone derivative represented by formula (I):

Cycloalkylaminomethylpyrrolidine derivatives

An antimicrobial drug having excellent antimicrobial activity and high safety is disclosed, which comprises as an active ingredient, a quinolone derivative having a substituted aminocycloalkylpyrrolidine as a substituent and which is further substituted with various substituents, represented by formula (I), its salts and hydrates thereof:

Substituted aminocycloalkylpyrrolidine derivatives and cis-substituted aminocycloalkylpyrrolidine derivatives

The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I):

An antimicrobial drug having excellent antimicrobial activity and high safety is disclosed, which comprises as an active ingredient, a quinolone-derivative having a substituted aminocycloalkylpyrrolidine as a substituent and which is further substituted with various substituents, represented by formula (I), its salts and hydrates thereof: ##STR1## wherein Q is represented by formula (II) or (IV). ##STR2## Also disclosed is a quinolone derivative where R.sup.4 and the substituent on the pyrrolidine ring of the following formula: ##STR3## are located at the cis-configuration; and Q is represented by the formula: ##STR4##

Substituted aminocycloalkylpyrrolidine derivatives and cis-substituted

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Tokyo, Japan

Hitoshi Ohki