Astellas Pharma Gmbh

Michihito Kageyama

Susumu Watanuki

Takashi Kamikubo

Hiroyuki Moritomo

Fukushi Hirayama

Yuji Koga

Jun Takasaki

Takao Okuda

Jiro Fujiyasu

Toshio Uemura

Ryushi Seo

Kazuhiro Ikegai

Eisuke Nozawa

Keisuke Matsuura

Tatsuya Zenkoh

Ryotaro Ibuka

Disclosed are quinolone derivatives characterized in that these have lower alkyl, cycloalkyl or the like at the 1-position; &#x2014;N(R)C(O)-lower alkylene-COR, lower alkylene-COR, lower alkenylene-COR, &#x2014;O-lower alkylene-COR, &#x2014;O-(lower alkylene which may be substituted with &#x2014;COR)-aryl or &#x2014;O-lower alkenylene-COR(wherein Ris H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof, has excellent P2Y12 inhibitory activity. The quinolone derivatives have excellent platelet aggregation inhibitory activity. A method of using the compounds is also disclosed.

Quinolone derivative or pharmaceutically acceptable salt thereof

[Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.

Amide compound

Provided are quinolone derivatives having a lower alkyl or cycloalkyl at the 1-position; &#x2014;N(R)C(O)-lower alkylene-COR, lower alkylene-COR, lower alkenylene-COR, &#x2014;O-lower alkylene-COR, &#x2014;O-(lower alkylene which may be substituted with &#x2014;COR)-aryl or &#x2014;O-lower alkenylene-COR(wherein Ris H or lower alkyl) at the 3-position; halogen at the 6-position; and amino group substituted with a substituent group having a ring structure at the 7-position, respectively, or pharmaceutically acceptable salts thereof. Pharmaceutical composition containing the quinolone derivatives and methods of using the compositions are provided.

Growing community of inventors

Tokyo, Japan

Michihito Kageyama