Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Toru Haneda

Norihiro Ueda

Yasuhiro Funahashi

Junichi Kamata

Akihiko Tsuruoka

Keiko Takahashi

Yuji Yamamoto

Tatsuo Watanabe

Yoshihiko Kotake

Kyosuke Kitoh

Tadashi Okabe

Kazumasa Nara

Takashi Owa

Taro Semba

Shinichi Hamaoka

Naoko Hata

Toshiaki Wakabayashi

Yoichi Ozawa

Naoko Tsukahara

Jun Niijima

Masayuki Matsukura

Takeshi Nagasu

Nozomu Koyanagi

Hiroshi Yoshino

Kentaro Yoshimatsu

Hiroshi Obaishi

Junji Matsui

Noako Tsukahara

Satoshi Inoue

Hiroaki Nomura

Keigo Tanaka

Kazuki Miyazaki

Tomohiro Matsushima

Kazutaka Nakamoto

Yoshio Fukuda

Atsumi Yamaguchi

Katsuji Nakamura

Fusayo Mimura

Sachi Suzuki

Ken-ichi Nomoto

Shinya Abe

Yasuyuki Suzuki

Itaru Tsukada

Katsura Hata

Naoaki Watanabe

Itaru Arimoto

Takako Yoshiba

Kenji Matsui

Ken-Ichi Nomoto

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 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

The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them, wherein in the formula, B means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated; K means a single bond, &#x2014;CH&#x2550;CH&#x2014; or &#x2014;(CRR)&#x2014; (wherein Rand Rare the same as or different from each other and each means hydrogen atom or a C1-C4 alkyl group; and mmeans an integer of 1 or 2); Rmeans hydrogen atom or a C1-C6 alkyl group; Z means a single bond or &#x2014;CO&#x2014;NH&#x2014;; and R means a C6-C10 aryl ring or 6- to 10-membered heteroaryl ring which may have a substituent and in which a part of the ring may be saturated, respectively.

Integrin expression inhibitor

The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): (wherein X represents an oxygen atom, a sulfur atom or &#x2014;NH&#x2014;, Rrepresents a hydrogen atom, a halogen atom, a cyano group, an amino group or a substituent, and Rand Rindependently represent a hydrogen atom, a halogen atom, a hydroxyl group or a substituent, except for a case in which Rand Rare both hydrogen atoms), and an antifungal agent containing the above compound.

Antifungal agent containing pyridine derivative

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.

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.)],

Sulfonamide-containing heterocyclic compounds

Sulfonamide-containing indole compounds

Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have excellent antitumor activity and are represented by the following general formula (I) and processes for producing the same are provided. The present sulfonamide derivatives or a sulfonic ester derivatives are represented by the following general formula (I): ##STR1## wherein G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- and --R.sup.1 represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from among the following; ##STR2## rings A and B each represent an unsaturated 5- or 5 -membered ring; X represents N(R.sup.2) wherein R.sup.2 represents hydrogen or lower alkyl, or NHCO; Y represents 0, S(O).sub.n, C(R.sup.3) (R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10) C(O), N.dbd.CR.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15); Z represents nitrogen or C(R.sup.16); and n represents 0, 1 or 2, R.sup.3 to R.sub.13, R.sup.15 and R.sup.16 each represent hydrogen or lower alkyl, and R.sup.14 represents hydrogen, lower alkyl or lower acyl.

Tricyclic heterocyclic sulfonamide and sulfonic ester derivatives

A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).

A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a hydroxyl or amino group;

Condensed pyrimidine derivative

A novel pyrimidine derivative having an excellent antitumor activity, which is represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a hydroxyl or amino group; R.sup.2 represents a phenylene, pyridinediyl, thiendiyl, furandiyl or thiazoldiyl group, --CO.sub.2 R.sup.5 and --CO.sub.2 R.sup.6 may be the same or different from each other and each represents a carboxyl group or a carboxylic acid ester, the part ##STR2## A represents an oxygen atom, a group represented by the formula: ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different from each other and each represents a hydrogen or halogen atom or a hydrocarbon group which may be substituted, or alternatively R.sup.3 and R.sup.4 may be united to form an alkylidene group which may be substituted) or a group represented by the formula: ##STR4## (wherein R.sup.70 represents a hydrogen atom or a hydrocarbon group), and n is an integer of 1 to 3, provided that the compound in which R.sup.1 represents oxygen, and hydrogen is attached to nitrogen at 3-position is included in the above shown definition, a process for preparation the same, and an antitumor drug containing the same.

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Ushiku, Japan

Toru Haneda