Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Masayuki Matsukura

Keigo Tanaka

Kazutoshi Miyake

Kazuki Miyazaki

Satoshi Inoue

Kazutaka Nakamoto

Hiroki Ishihara

Shinya Abe

Naoki Yoneda

Junichi Kamata

Norio Murai

Shuji Shirotori

Shigeru Souda

Akihiko Tsuruoka

Keiko Takahashi

Tomohiro Matsushima

Yoshio Fukuda

Norio Minami

Tatsuo Watanabe

Fumihiro Ozaki

Yasuhiro Funahashi

Hiroshi Obaishi

Junji Matsui

Sachiyuki Hamano

Toru Haneda

Nobuyuki Mori

Toshiyuki Matsuoka

Takashi Musha

Osamu Hiroshima

Shigeto Negi

Nobuhisa Watanabe

Toshiaki Ogawa

Hideyuki Adachi

Yuji Yamamoto

Yasuhiro Kabasawa

Keiji Ishibashi

Yoshiharu Daiku

Yasutaka Takase

Kenichi Nomoto

Masanori Mizuno

Makoto Kaino

Tadanobu Takamura

Kohtaro Kodama

Atsumi Yamaguchi

Katsuji Nakamura

Naoya Kishi

Koichi Nose

Fusayo Mimura

Sachi Suzuki

Ken-ichi Nomoto

Fusayo Yoshida

Keizoh Satoh

Mikio Tomimatsu

Yasuyuki Suzuki

Toshihiko Kaneko

Norihiro Ueda

Yoshinori Takahashi

Jun Niijima

Ichiro Yoshida

Itaru Tsukada

Katsura Hata

Kohei Sawada

Naoaki Watanabe

Hiroshi Katoh

Takashi Yoshinaga

Kiyoaki Kobayashi

Hiroyuki Suzuki

Mutsuko Tabata

Tatsuhiro Onogi

Eiichi Yamamoto

Itaru Arimoto

Takako Yoshiba

Takuma Minamisono

Kenji Matsui

Miyuki Ohkubo

Ken-Ichi Nomoto

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

The present invention provides compounds that have excellent antifungal action, and are also excellent in terms of properties, such as solubility in water and safety. The compounds are represented by formula (I): The present invention is also directed to a pharmaceutical composition comprising the compound, an antifungal agent comprising the compound as an active ingredient, and a method for preventing or treating a fungal disease by administering the compound.

Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same

Compounds represented by the following general formula: wherein Ais an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xis &#x2014;O&#x2014;, &#x2014;S&#x2014;, etc.; Yis an optionally substituted Caryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tis a group represented by the following general formula: (wherein Eis a single bond or &#x2014;N(R)&#x2014;), Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, etc. and Zrepresents a Calkyl group, a Calicyclic hydrocarbon group, a Caryl group, etc.), salts thereof or hydrates of the foregoing.

Nitrogen-containing aromatic derivatives

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.

There is provided a heterocycle-substituted pyridine derivative's salt or a crystal thereof. The present invention provides an acid addition salt of 3-(3-(4-(pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-yl amine or a crystal thereof as well as process for producing the same.

Heterocycle-substituted pyridine derivative's salt or crystal thereof

The present invention provides an antifungal agent represented by the formula: [wherein Arepresents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; Xrepresents a group represented by the formula &#x2014;NH&#x2014;C(&#x2550;O)&#x2014;, a group represented by the formula &#x2014;C(&#x2550;O)&#x2014;NH&#x2014;, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that Amay have 1 to 3 substituents, and E has one or two substituents].

Antifungal agent containing heterocyclic compound

Compounds represented by the following general formula: [wherein Ais an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xis &#x2014;O&#x2014;, &#x2014;S&#x2014;, etc.; Yis an optionally substituted Caryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tis a group represented by the following general formula: (wherein Eis a single bond or &#x2014;N(R)&#x2014;, Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, etc. and Zrepresents a Calkyl group, a Calicyclic hydrocarbon group, a Caryl group, etc.)], salts thereof or hydrates of the foregoing.

A compound represented by the general formula: wherein Xrepresents a nitrogen atom or a group represented by the formula &#x2014;CR&#x2550;; Xrepresents a nitrogen atom or a group represented by the formula &#x2014;CR&#x2550;; Y represents an oxygen atom or the like; Rrepresents a Calkoxy group, an optionally substituted Caryloxy group, a group represented by the formula &#x2014;NRRor the like; Rrepresents a hydrogen atom, an optionally substituted Calkyl group, or the like; R, R, R, R, R, R, Rand Reach independently represent a hydrogen atom, a halogen atom, an optionally substituted Calkyl group, or the like; Rrepresents a group represented by the formula &#x2014;NRRor the like; and R, R, Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, or the like,a salt thereof, or a hydrate of the foregoing.

Compounds represented by the following general formula: [wherein Ais an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xis &#x2014;O&#x2014;, &#x2014;S&#x2014;, etc.; Yis an optionally substituted Caryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tis a group represented by the following general formula: (wherein Eis a single bond or &#x2014;N(R)&#x2014;, Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, etc. and Zrepresents a Calkyl group, a Calicyclic hydrocarbon group, a Caryl group, etc.)],

A compound represented by the general formula: wherein Xrepresents a nitrogen atom or a group represented by the formula &#x2014;CR&#x2550;; Xrepresents a nitrogen atom or a group represented by the formula &#x2014;CR&#x2550;; Y represents an oxygen atom or the like; Rrepresents a Calkoxy group, an optionally substituted Caryloxy group, a group represented by the formula &#x2014;NRRor the like; Rrepresents a hydrogen atom, an optionally substituted Calkyl group, or the like; R, R, R, R, R, R, Rand Reach independently represent a hydrogen atom, a halogen atom, an optionally substituted Calkyl group, or the like; Rrepresents a group represented by the formula &#x2014;NRRor the like; and Rand Reach independently represent a hydrogen atom, an optionally substituted Calkyl group, or the like, a salt thereof, or a hydrate of the foregoing.

Piperidine compound and pharmaceutical composition thereof

Fused pyridazine compounds

Growing community of inventors

Tsukuba, Japan

Masayuki Matsukura