Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Tadashi Okabe

Keiko Takahashi

Noritaka Kitazawa

Atsushi Sasaki

Kazumasa Nara

Shinichi Hamaoka

Koki Kawano

Atsuhiko Kubota

Kohshi Ueno

Manabu Matsunaga

Norihiro Ueda

Yasuhiro Funahashi

Akihiko Tsuruoka

Yuji Yamamoto

Toru Haneda

Junichi Kamata

Takashi Owa

Taro Semba

Naoko Hata

Toshiaki Wakabayashi

Yoichi Ozawa

Makoto Komatsu

Teiji Kimura

Atsushi Kamada

Yuichi Suzuki

Noboru Yamamoto

Noako Tsukahara

Nobuhisa Watanabe

Hitoshi Harada

Ichiro Yoshida

Yoshiaki Ohashi

Naoko Tsukahara

Yuji Onizawa

Yasunobu Matsumoto

A compound represented by formula (1) or a pharmaceutically acceptable salt thereof has an inhibitory effect in the fractalkine-CX3CR1 pathway: wherein R represents a Calkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, a Ccycloalkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, or a Ccycloalkenyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group A, X represents a Calkyl group, Y and Z are the same or different from each other and each represents a halogen atom or a Calkyl group unsubstituted or having 1 to 3 substituents selected from Substituent Group B, n represents 0 or 1, Substituent Group A consists of halogen atoms, and Substituent Group B consists of halogen atoms.

Pyrrolidin-3-ylacetic acid derivative

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

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.

A novel compound of the formula:wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; RR, R, R, and Rrepresent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.

Quinoline derivatives

Condensed pyridine compounds represented by formula (I):wherein: Rand Rare, independently, hydrogen, lower alkyl, or lower alkoxy; Rrepresent an amino substituent; ring A is a benzene ring, pyridine ring, thiophene ring, or furan ring; and B represents a substituent containing a ring structure. Also, pharmaceutically acceptable salt and hydrates thereof. These compounds are clinically useful medicaments having serotonin antagonism, and in particular, for treating, ameliorating, or preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.

Growing community of inventors

Ibaraki, Japan

Tadashi Okabe