Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Alchemedicine, Inc.

Keigo Tanaka

Kazutaka Nakamoto

Itaru Tsukada

Katsura Hata

Satoshi Inoue

Kappei Tsukahara

Norio Murai

Koji Sagane

Naoaki Watanabe

Norihiro Ueda

Masayuki Matsukura

Shuji Shirotori

Mamiko Tsuchiya

Fuminori Ohba

Junko Kai

Shinya Abe

Toshimi Okada

Hironori Ikuta

Masashi Ito

Toru Haneda

Takao Saeki

Kaoru Ogawa

Toshihiro Horii

Daisuke Shinmyo

Satoshi Nagao

Hironobu Hiyoshi

Nobuyuki Kurusu

Eiichi Yamamoto

Tomoki Nishioka

Mamoru Yanagimachi

Jun Niijima

Nobuhisa Watanabe

Kazuki Miyazaki

Hiroyuki Sugumi

Hiroshi Azuma

Shinsuke Hirota

Seiji Yoshikawa

Tasuku Ishida

Yoshiaki Ohashi

Shuichi Suzuki

Daisuke Iida

Setsuo Funasaka

Yuzo Watanabe

Masayuki Miyano

Daisuke Ito

Wataru Itano

Takashi Fukuyama

Isao Ohashi

Takuma Minamisono

Raku Shinkyo

Yoshinobu Yamane

Yusuke Nakatani

Yuki Karoji

Yosuke Kaburagi

Nishioka Tomoki

An object of the present invention is to provide a compound having CK1δ inhibition activity and/or ALK5 inhibition activity and the like. The object thereof can be attained by a compound represented by the following formula (1): wherein

Heterocyclic compound as inhibitor of casein kinase 1-δ and/or activin receptor-like kinase 5

The present invention provides a compound represented by formula (1): or pharmaceutically acceptable salt thereof, wherein

ALDH2 activator

A compound represented by the formula (I) or a salt thereof: wherein a ring Z is a 5 to 6-membered heteroaromatic ring having one or two heteroatoms in the ring; Xis a hydrogen atom, a hydroxy group, a hydroxy Calkyl group, &#x2014;B(OH), a boronate ester group, a cyclic boronate ester group, a boranyl group, a cyclic boranyl group, &#x2014;BFM, &#x2014;Sn(R)(R)(R), a leaving group, a carboxy group, a formyl group, or &#x2014;NRR; and Xis a hydrogen atom or &#x2014;COR.

Hetero-fused cyclic compound

The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or &#x2014;CH&#x2014;; E represents a nitrogen-containing non-aromatic heterocycle; Rrepresents an alkoxy group or the like; Rrepresents a hydrogen atom or the like; and Rrepresents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and Ror Ris present on a nitrogen atom on the azetidine ring, the Ror Rdoes not represent a hydrogen atom.

Monocyclic pyridine derivative

A compound represented by Formula (1), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of paroxetine and has an improved CYP inhibitory effect: wherein Ris a hydrogen atom or Calkyl group.

Paroxetine derivative

An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R, R, X, Y, ring A, Z, Rand Rare as defined in the specification.

Heterocycles substituted pyridine derivatives and antifungal agent containing thereof

A compound represented by formula (1-1) or (1-2), or a pharmacologically acceptable salt thereof retains the principal therapeutic effect of sitaxentan and has an improved CYP inhibitory effect: wherein Ris a halogen atom, etc., Ris a methyl group, etc., Ris a Calkyl group, etc., and M is a group represented by: etc.

Sitaxentan derivative

A production method of a compound containing a primary, secondary, or tertiary aminomethyl aromatic ring of the present invention includes: using a fluoroboron compound or a dimer thereof, or solvates thereof, which are represented by a formula (I):Ra(Rb)N&#x2014;CH&#x2014;BFM&#x2003;&#x2003;(I)

Fluoroboron compound, aminomethylating agent for aromatic ring made of the same, and production method of compound containing aminomethyl aromatic ring using aminomethylating agent

Anti-fungal agent having excellent anti-fungal action physicochemical properties including safety and water solubility. Compound represented by formula (I), or salt thereof: wherein Rrepresents hydrogen, halogen, amino, R&#x2014;NH&#x2014; wherein Rrepresents Calkyl, hydroxy Calkyl, Calkoxy Calkyl, or Calkoxycarbonyl Calkyl, R&#x2014;(CO)&#x2014;NH&#x2014; wherein Rrepresents Calkyl group or Calkoxy Calkyl, Calkyl, hydroxy Calkyl, cyano Calkyl, Calkoxy, or Calkoxy Calkyl or a phosphonoamino group; Rrepresents hydrogen, Calkyl, amino, or a di Calkylamino group or a phosphonoamino group; one of X and Y is nitrogen while the other is nitrogen or oxygen; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom or 1 or 2 Calkyl groups; Z represents a single bond, a methylene group, an ethylene group, oxygen, sulfur, &#x2014;CHO&#x2014;, &#x2014;OCH&#x2014;, &#x2014;NH&#x2014;, &#x2014;CHNH&#x2014;, &#x2014;NHCH&#x2014;, &#x2014;CHS&#x2014;, or &#x2014;SCH&#x2014;; Rrepresents hydrogen or halogen or Calkyl, Ccycloalkyl, Caryl, a 5- or 6-member heteroaryl group or a 5- or 6-member nonaromatic heterocyclic group which may have 1 or 2 substituents; and Rrepresents hydrogen or halogen; provided that either Ror Rrepresents a phosphonoamino group.

Pyridine derivatives substituted by heterocyclic ring and phosphonoamino group, and anti-fungal agent containing same

Provided is a fluoroboron compound which is highly safe and stable and is capable of forming a cyclic ether-fused ring by the intramolecular alkoxymethylation reaction, or a salt thereof. The compound can be synthesized by the intramolecular alkoxymethylation reaction of a fluoroboron compound represented by the formula (I) or a salt thereof in the presence of a metal catalyst.  represents an aromatic ring; L represents a substituent such as a halogen atom; R represents a substituted or unsubstituted alkylene group having 1 or 2 carbon atoms; and M represents an alkali metal cation or the like, with the proviso that L and &#x2014;R&#x2014;OCHBFM are respectively located on contiguous carbon atoms on the aromatic ring, or in the case of a fused aromatic ring, on two carbon atoms adjacent to one carbon at the fused position).

Fluoroboron compound having aromatic ring or salt thereof, and method for producing compound having cyclic ether-fused aromatic ring using the same

The present inventors succeeded in isolating GWT1 (PfGWT1), which is one of the enzymes involved in GPI biosynthesis in the malaria parasite. In addition, the inventors revealed that degenerate mutant DNAs, with a lower AT content than the DNA encoding the PfGWT1 protein, can complement the phenotype of GWT1-deficient yeast. Based on the findings, the present invention provides the GWT1 protein of malaria parasites and the use of the protein in methods of screening for antimalarial drugs. The present invention also provides degenerate mutant DNAs encoding proteins involved in GPI biosynthesis, and which have a lower AT content than the original DNAs. The present invention also provides methods of screening for antimalarial drugs which use the degenerate mutant DNAs.

Methods of screening for compounds that inhibit the biosynthesis of GPI in malaria parasites

The present invention provides an antifungal agent which has excellent antifungal action, and which is also excellent in terms of its properties, and in particular its solubility in water and safety. The present invention discloses a compound represented by the following formula (I) or a salt thereof. wherein R, R, R, R, A, X, Y, and Z are defined in the specification.

Pyridine derivatives substituted with heterocyclic ring and &#x3b3;-glutamylamino group, and antifungal agents containing same

The present invention provides an antifungal agent that has excellent antifungal action, and is also excellent in terms of its properties, safety, and metabolic stability. The present invention discloses a compound represented by the following formula I or a salt thereof, and an antifungal agent comprising the compound or the salt: wherein Rrepresents a hydrogen atom, a halogen atom, an amino group, a Calkyl group, a Calkoxy group, or a C-alkoxy-C-alkyl group; Rrepresents a hydrogen atom or an amino group; X, Y, Z, and W independently represent a nitrogen atom, an oxygen atom, a sulfur atom, or &#x2014;CH&#x2014;, provided that at least two among X, Y, and W are nitrogen atoms; the ring A represents a 5- or 6-membered heteroaryl ring or a benzene ring; Q represents a methylene group, an oxygen atom, &#x2014;CHO&#x2014;, &#x2014;OCH&#x2014;, &#x2014;NH&#x2014;, &#x2014;NHCH&#x2014;, or &#x2014;CHNH&#x2014;; and Rrepresents a Calkyl group, a Ccycloalkyl group, a Caryl group, or a 5- or 6-membered heteroaryl group, each of which may have one or two substituents.

Pyridine derivative substituted by heteroaryl ring, and antifungal agent comprising the same

An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein Rrepresents a hydrogen atom, a halogen atom, an amino group, a Calkyl group, a Calkoxy group or a Calkoxy Calkyl group; Rrepresents a hydrogen atom, a Calkyl group, an amino group or a di Calkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 Calkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, &#x2014;CHO&#x2014;, &#x2014;OCH&#x2014;, &#x2014;NH&#x2014;, &#x2014;CHNH&#x2014;, &#x2014;NHCH&#x2014;, &#x2014;CHS&#x2014;, or &#x2014;SCH&#x2014;; Rrepresents a hydrogen atom, a halogen atom, a Calkyl group, a Ccycloalkyl group, a Caryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and Rrepresents a hydrogen atom or a halogen atom.

Growing community of inventors

Tsukuba, Japan

Keigo Tanaka