Kyowa Hakko Kirin Co., Limited

Kyowa Hakko Kogyo Co., Ltd.

Kyowa Kirin Co., Ltd.

Kimihisa Ueno

Keisuke Yamamoto

Seiji Aratake

Michihiko Suzuki

Tomohiro Tamura

Takeshi Kuboyama

Arata Yanagisawa

Satoshi Nakanishi

Kazuki Hemmi

Katsuya Kobayashi

Rina Nakamura

Keiji Uehara

Hiroyuki Ishida

Tsutomu Akama

Kenji Uchida

Masaji Kasai

Hiromitsu Saito

Katsushige Gomi

Etsuo Ohshima

Yuji Nomoto

Ichiro Miki

Hitoshi Arai

Masahiro Matsubara

Shun-ichi Ikeda

Hideaki Kusaka

Yoshihisa Ohta

Shintaro Hosoe

Kozo Yao

Koji Suzuki

Koji Yanagawa

Yasushi Shida

Motoki Miyama

Tsutomu Matsumura

Hiroshi Ishida

Yukihito Tsukumo

Uichiro Kimura

Kotaro Takasaki

Hiroshi Yano

Akinori Hamaguchi

Maasa Motosawa

Takahiro Kabeya

Daisuke Nakashima

Chiharu Nakagawa

Akira Ogawa

Miho Iwase

Shinya Fujii

Takashi Sato

Ari Kawabe

Mirai Mizutani

Daisuke Harada

Yosuke Yamaura

The invention provides a pyridone compound represented by the following formula (I) [wherein, Rrepresents cycloalkyl optionally having substituent(s) and the like, Rrepresents a hydrogen atom and the like, Rrepresents hydroxy and the like, and Rrepresents the following formula (R-1) (wherein, Rand Rare the same or different and each represents a hydrogen atom and the like), and the like], or a pharmaceutically acceptable salt thereof, which is useful as a prophylactic and/or therapeutic agent for skin diseases, and the like. 

Pyridone compound

The invention provides a method of activating PPAR &#x3b3; and a method of treating or preventing a disease associated with PPAR &#x3b3; by administering a tricyclic compound having a PPAR &#x3b3; agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R-Rare the same or different and each represents hydrogen or the like, V represents a single bond or the like, Rand Rare the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like: 

Tricyclic compound

A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, Ris a hydrogen atom and the like, X is the formula (b3) wherein Ris a hydrogen atom and the like, and the like, A is the formula (a18) wherein Ris a hydrogen atom and the like, and Rand Rare the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR&#x3b3; agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided. 

Dibenzooxepin derivative

Provided is an agent for the prevention and/or treatment of a skin disease containing, as an active ingredient, a pyrazolopyrimidine derivative represented by the formula (I) (wherein each symbol is as defined in the specification), or a pharmacologically acceptable salt thereof, and the like.

Agent for prevention and/or treatment of skin diseases

Provided is a tricyclic compound having a PPAR &#x3b3; agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R-Rare the same or different and each represents hydrogen or the like, V represents a single bond or the like, Rand Rare the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like: 

The present invention provides a PPAR &#x3b3; agonist comprising, as an active ingredient, a tricyclic compound represented by the formula (I) (wherein Rrepresents lower alkyl optionally having substituent(s) or the like, Rand Rare the same or different and each represents lower alkyl optionally having substituent(s) or the like, Rand Rare the same or different and each represents a hydrogen atom or the like, Q-Q-Qrepresents CH&#x2550;CH&#x2014;CH&#x2550;CH or the like, Y represents a single bond or the like, Z-Zrepresents C&#x2550;CR(wherein Rrepresents a hydrogen atom or the like), or the like, and A represents &#x2014;COOH or the like), or a pharmaceutically acceptable salt thereof and the like.

Tricyclic compounds

[wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; Rrepresents &#x2014;NRR(wherein Rand Rmay be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); Rrepresents the above Formula (II), Formula (IV) or the like; A represents a single bond, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;SO&#x2014;, &#x2014;OC(&#x2550;O)&#x2014; or the like; and Rrepresents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like] Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided. These have anti-inflammatory activities or modulation activities on the functions of TARC and/or MDC and are useful for treating and/or preventing a disease which is related to T cells, such as an allergic disease, an autoimmune disease or transplant rejection.

Bicyclic pyrimidine derivatives

A condensed purine derivative represented by Formula (I):wherein X&#x2014;Y-Z represents RN&#x2014;C&#x2550;O or N&#x2550;C&#x2014;W, Rrepresents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, Vrepresents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, Vrepresents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when Vrepresents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X&#x2014;Y-Z represents RN&#x2014;C&#x2550;O and Rrepresents a substituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted alicyclic heterocyclic group, a halogen atom, a lower alkylthio group, &#x2014;NRR, &#x2014;COH, a lower alkoxycarbonyl group, &#x2014;COHal, &#x2014;CONRRor &#x2014;CHO, Vmay represent a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group; or a pharmacologically acceptable salt thereof.

Fused purine derivatives

5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.6 are taken together to form a heterocyclic group containing the nitrogen atom in the ring), lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, lower alkoxycarbonyl, lower alkanoyl, adizo, cyano, substituted or unsubstituted carbamoyl or lower alkylthiothiocarbonyl: or pharmaceutically acceptable salts thereof.

5-aminoflavone derivatives

Growing community of inventors

Shizuoka, Japan

Kimihisa Ueno