Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Esai Co., Ltd.

Norihiro Ueda

Kappei Tsukahara

Yoshihiko Kotake

Kyosuke Kitoh

Toru Haneda

Shigeru Souda

Shuhei Miyazawa

Naoyuki Shimomura

Tatsuo Watanabe

Jun Niijima

Takeshi Nagasu

Nozomu Koyanagi

Hiroshi Yoshino

Kentaro Yoshimatsu

Tsuneo Wakabayashi

Keigo Tanaka

Itaru Tsukada

Kazutaka Nakamoto

Katsura Hata

Naoaki Watanabe

Toshihiko Kaneko

Seiichiro Nomoto

Katsuya Tagami

Hisashi Shibata

Makoto Okita

Manabu Murakami

Masatoshi Fujimoto

Kiyoshi Oketani

Makoto Asada

Hideaki Fujisaki

Toshimi Okada

Koji Sagane

Mamiko Tsuchiya

Fuminori Ohba

Junko Kai

Atsumi Iijima

Yasuhiro Funahashi

Akihiko Tsuruoka

Keiko Takahashi

Yuji Yamamoto

Tadashi Okabe

Hiroyuki Sugumi

Kazumasa Nara

Junichi Kamata

Takashi Owa

Taro Semba

Shinichi Hamaoka

Toshiaki Wakabayashi

Naoko Hata

Yoichi Ozawa

Naoko Tsukahara

Takashi Yamanaka

Ieharu Hishinuma

Tsutomu Kawata

Junichi Nagakawa

Junsaku Nagaoka

Kaname Miyamoto

Hidetoshi Kawashima

Naoko Nagaoka

Noako Tsukahara

Hiroaki Nomura

Shinya Abe

Satoshi Inoue

Masayuki Matsukura

Hirovuki Sugumi

The present invention provides isolated DNA encoding a GWT1 protein having activity to confer resistance of a fungus against a compound of formula Ia, and wherein a defect of a function of the GWT1 protein leads to a decrease in the amount of a glycosylphosphatidylinositol (GPI)-anchored protein in the cell wall of a fungus.

Fungal cell wall synthesis gene

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

A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, fungal genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. These genes encode proteins participating in fungal cell wall synthesis. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.

A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed. Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.

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

Sulfonamide-containing heterocyclic compounds

Sulfonamide-containing indole compounds

Pyridine derivatives useful for preventing or treating peptic ulcers, pharmaceutical preparations and methods of treating peptic ulcers are described.

Pyridine derivatives having anti-ulcerative activity

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).

Growing community of inventors

Tsukuba, Japan

Norihiro Ueda