Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Kazumasa Nara

Akihiko Tsuruoka

Tadashi Okabe

Shinichi Hamaoka

Norihiro Ueda

Yasuhiro Funahashi

Keiko Takahashi

Yuji Yamamoto

Toru Haneda

Junichi Kamata

Takashi Owa

Taro Semba

Toshiaki Wakabayashi

Naoko Hata

Atsushi Kamada

Yoichi Ozawa

Noritaka Kitazawa

Atsushi Sasaki

Itaru Tsukada

Toshihiko Naito

Katsura Hata

Noako Tsukahara

Yumiko Kaku

Manabu Yanagisawa

Toshio Toyosawa

Shinya Abe

Mitsuo Nagai

Osamu Asano

Jun Niijima

Tomohiro Matsushima

Shuji Shirotori

Takahisa Sakaguchi

Eiichi Yamamoto

Naoko Tsukahara

Kazunori Wakasugi

Shinichi Tsukuba Res Lab Eisai Co Ltd Hamaoka

Tadashi c/o Tsukuba Research Laboratories Okabe

Crystals, amorphous substances, salts, and hydrates of a salt of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl)phenyl]terephthalamic acid having PDE4 inhibitory action are provided. These compounds are useful for treating allergic diseases such as atopic dermatitis.

Crystals, amorphous substances or salts of methyl N-[3-(6,7-dimethoxy-2-methylaminoquinazolin-4-yl) phenyl] terephthalamic acid

The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Rand Rare the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R&#x2033; represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

Selective estrogen receptor modulator

The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like;&#x2003;&#x2003;(I-1)formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Rand Rare the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R&#x2033; represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

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

A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent,wherein Rrepresents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R, R, Rand Rmay be the same or different and each represents hydrogen or fluorine; and Rrepresents hydrogen or fluorine.

Process for preparing phenoxypyridine derivatives

The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like;formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Rand Rare the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R&#x2033; represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.

Sulfonamide-containing heterocyclic compounds

Sulfonamide-containing indole compounds

A compound represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 denote a halogen atom or hydrogen atom; R.sup.3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for --S--, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmaceutical composition suitable for use as an antifungal agent.

Antifungal agents, processes for the preparation thereof, and

A compound represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 denote a halogen atom or hydrogen atom; R.sup.3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for --S--, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmacetical composition suitable for use as an antifungal agent.

Antifungal agents, and compositions

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Tsukuba, Japan

Kazumasa Nara