Kyorin Pharmaceutical Co., Ltd.

Teijin Pharma Limited

Kohei Ohata

Mitsuhito Shibasaki

Hiroyasu Takahashi

Yoshifumi Saito

Kosuke Tsuda

Yasumichi Fukuda

Yoshikazu Asahina

Koji Murakami

Kiyoshi Fujii

Kazuya Yokota

Toshiyuki Matsui

Shinji Kobayashi

Masanori Yamamoto

Masanori Takadoi

Tomohiro Ide

Hiroyuki Watanabe

Fumiyoshi Kobayashi

Kanji Komatsu

Megumi Kamiya

Kentaro Umei

Mikako Kawashima

Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect. The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. 

Urea derivative or pharmacologically acceptable salt thereof

The present invention provides a urea compound or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea compound or the pharmacologically acceptable salt thereof and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like. 

The present invention provides a urea derivative or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea derivative or the pharmacologically acceptable salt thereof, and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like. 

Summary Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. Solving Means The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).

Bicycloester derivative

A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, Rrepresents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C-Calkyl group, or a C-Calkoxy group, Rrepresents a C-Ccycloalkylsulfanyl group, a C-Ccycloalkylsulfinyl group, or a C-Ccycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).

Glucokinase activator

Novel bicycloester derivatives and pharmaceutically acceptable salts thereof have high DPP-IV inhibitory activity. The novel bicycloester derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[N-(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).

Growing community of inventors

Shimotsuga-gun, Japan

Kohei Ohata