Other

The University of Tokyo

Shionogi Company Limited

Tohoku University

Riken Corporation

Sekisui Medical Co., Ltd.

Tetsuo Nagano

Hirotatsu Kojima

Takayoshi Okabe

Kazuya Kikuchi

Nobuyuki Tanaka

Osamu Nureki

Hiroshi Nishimasu

Ryuichiro Ishitani

Yusuke Tateno

Junken Aoki

Kazuki Kiyose

Mitsuyasu Kawaguchi

Junji Yamane

Shigeyuki Yokoyama

Hirofumi Nakano

Akiko Tanaka

Manabu Katou

Shiro Kida

Tomoya Hirano

Masanao Abe

Hidenori Ichijo

Yasuhiko Kanda

Takao Fujisawa

Chiaki Fujikoshi

Keiko Tsuganezawa

Hitomi Yuki

Teruki Honma

Tsunehiko Higuchi

Hidehiko Nakagawa

Shin-Ichi Ikeda

Sakiko Aizawa

Kengo Homma

Eita Sasaki

Naomi Tsuburaya

Manabu Shimonishi

Masahide Odan

Norio Shiibata

Yoshiyuki Kioi

Seiichi Nakamura

Nae Saito

A compound represented by the following formula (1) is provided: wherein X represents a sulfur atom or &#x2014;CH&#x2550;CH&#x2014;; Ato Aeach independently represent a carbon atom or a nitrogen atom, and at least one of Ato Ais a nitrogen atom; Rrepresents any one of a 1,2,3,4-tetrahydroquinolyl group (or a 3,4-dihydro-1(2H)-quinolyl group), a 3,4-dihydro-4,4-dimethyl-1(2H)-quinolyl group, a 2,3,4,5-tetrahydro-1H-1-benzazepinyl group, or a substituent represented by the following formula (2): wherein Rrepresents a 2,3,4-trifluorophenyl group, a 4-iodophenyl group, a 2,3-difluorophenyl group, a 3,5-difluorophenyl group, a 5-fluoro-2-methylphenyl group, a 3-pentafluorosulfanylphenyl group, a 2,6-dimethylphenyl group, a 4-benzyloxyphenyl group, a 3,5-bis(trifluoromethyl)biphenyl group, a 4-tert-butylphenyl group, a 3-methoxyphenyl group, an unsubstituted or substituted pyridyl group, or an unsubstituted or substituted naphthyl group; Rrepresents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group optionally containing an oxygen atom and/or a double bond, or an unsubstituted or substituted aromatic lower alkyl group; Rrepresents a hydrogen atom, a lower alkyl group, a lower acyl group, or an unsubstituted or substituted aromatic lower alkyl group; and Rrepresents a hydrogen atom, or Rand Rmay bind to each other to form a ring.

Thieno[2,3-b]pyridine derivative, quinoline derivative, and use thereof

The present invention provides a compound of formula (1), wherein R, R, R, R, R, Rand Rare as defined in the description, which has an autotaxin inhibitory activity, a pharmaceutical composition comprising the compound as an active ingredient, and a method of prevention or treatment of a disease involving autotaxin, which is characterized by administering the compound. 

Fused pyrazole derivative having autotaxin inhibitory activity

A compound according to any one of formula (Ia) to (Ic), or its pharmaceutically acceptable salt: 

Pyrimidinone derivative having autotaxin-inhibitory activity

An anticancer agent comprising a compound represented by the formula (I) [Rrepresents hydrogen atom, hydroxyl group, a Calkoxy group and the like; Rand Rrepresents hydrogen atom, a halogen atom, a Calkyl group and the like; Rrepresents hydrogen atom, a Calkyl group, a Calkylsulfonyl group and the like; Rrepresents hydrogen atom or a substituent;represents a single bond or a double bond; Rand Rrepresents hydrogen atom, a Calkyl group and the like; Rrepresents hydrogen atom, a Calkyl group and the like; A represents &#x2014;O&#x2014;, &#x2014;S&#x2014;, or &#x2014;CH&#x2014;; D represents &#x2014;C&#x2550; or &#x2014;N&#x2550;; X represents methylene group, &#x2014;O&#x2014;, or &#x2014;CO&#x2014;; Q represents &#x2014;N&#x2550; or &#x2014;C(R)&#x2550;; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase. 

Anticancer agent

A compound represented by the following general formula (I): [wherein Rand Rrepresent a Calkyl group; R, Rand Rrepresent hydrogen atom, a Calkyl group, or an aryl group; Yand Yrepresent &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;Se&#x2014;, &#x2014;CH&#x2550;CH&#x2014;, &#x2014;C(R)(R)&#x2014;, or &#x2014;N(R)&#x2014; (wherein R, Rand Rrepresent hydrogen atom or a Calkyl group); A represents a Calkylene group; n and n' represent 0, 1 or 2; Zand Zrepresent a nonmetallic atom group required to form a benzo-condensed ring or a naphtho-condensed ring; Lto Lrepresent a methine group; and Mrepresents a counter ion in a number required for neutralizing electrical charge], which is useful as a fluorescent probe of which optical characteristics change depending on pH change.

Fluorescent probe

A fluorescent probe comprising a compound represented as (Fluorophore A)-S-(Fluorophore B) (Fluorophore A and Fluorophore B are fluorophores which emit fluorescence when they are irradiated with an excitation light of a wavelength of 600 to 950 nm, Fluorophore A has a property that it shows change of fluorescence characteristic before and after a specific reaction with an substance to be measured, and S represents a spacer which connects Fluorophore A and Fluorophore B), which compound shows substantial change in efficiency of fluorescence resonance energy transfer between Fluorophore A and Fluorophore B before and after the specific reaction with the objective substance, wherein Fluorophore A is represented by the following formula (AI): which uses and shows an excitation light wavelength/fluorescence wavelength in the near infrared region, lights of which region show superior biological tissue permeability, and enables measurement of an substance to be measured by the ratio method.

A fluorescent probe which specifically and efficiently traps nitrogen monoxide, zinc ion etc. to emit fluorescence is provided. A compound represented by the following general formula (I): [wherein Rand Rrepresent hydrogen atom, or a group represented by the following formula (A): (wherein Xto Xrepresent hydrogen atom, an alkyl group, or a protective group for amino group, and m and n represent 0 or 1); Rand Rrepresent hydrogen atom, a Calkyl group, or a Calkoxy group; Rto Rrepresent hydrogen atom, sulfo group, phospho group, a halogen atom, or a Calkyl group; Rand Rrepresent a Calkyl group; Zrepresents oxygen atom, sulfur atom, or &#x2014;N(R)&#x2014; (wherein Rrepresents hydrogen atom, or a Calkyl group); Yand Yrepresent &#x2014;C(&#x2550;O)&#x2014;, &#x2014;C(&#x2550;S)&#x2014;, or &#x2014;C(R)(R) (wherein Rand Rrepresent a Calkyl group); and Mrepresents a counter ion in a number required for neutralizing the charge].

A compound represented by the following formula (I): wherein Rand Rrepresent amino groups that substitute at adjacent positions on the phenyl ring, provided that either of Rand Rrepresents a mono(Calkyl)-substituted amino group and the other represents an unsubstituted amino group; and Rand Rindependently represent hydrogen atom or an acyl group, and an agent for measurement of nitrogen monoxide which comprises said compound.

Diaminofluorescein derivatives

Diaminorhodamine derivative

Diaminofluorescein derivative

A compound represented by the following general formula:

Diaminorhodamine derivatives

A compound useful for the measurement of nitrogen monoxide under a substantially neutral condition which is represented by the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 represent amino groups that substitute at adjacent positions on the phenyl ring; R.sup.3 and R.sup.4 independently represent a hydrogen atom or an acyl group; R.sup.5, R.sup.6, R.sup.7, and R.sup.8 independently represent a hydrogen atom, a C.sub.1-6 alkyl group, allyl group, or a halogen atom.

Growing community of inventors

Tokyo, Japan

Hirotatsu Kojima