Astellas Pharma Gmbh

Eisuke Nozawa

Hiroshi Shibata

Ryushi Seo

Yuji Koga

Tsubasa Watanabe

Kazuhiko Ohne

Takeshi Hanazawa

Keisuke Matsuura

Ryo Mizoguchi

Tatsuya Zenkoh

Ippei Sato

Takao Okuda

Kazuhiro Ikegai

Shunichiro Hachiya

Susumu Watanuki

Kyoichi Maeno

Hiroyoshi Yamada

Yoshimasa Imamura

Kenichiro Imamura

Toshio Kurosaki

Hirotsune Itahana

Ayako Moritomo

Michihito Kageyama

Maiko Iida

Shinobu Akuzawa

Koichiro Harada

Ryotaro Ibuka

Takaho Matsuzawa

Hiroki Ishioka

Tohru Ugawa

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.

Amide compound

An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.

Imidazopyridine compounds

[Problem] A pharmaceutical composition for treating or preventing various cardiovascular diseases, which have sGC activities based on improvement of cGMP signals, is provided. [Means for Solution] It was found that imidazo[1,2-a]pyridine compounds having a carbamoyl group at the 3-position and a particular cyclic group at the 8-position via a methyleneoxy group, or a salt thereof have sGC activation, and are useful as active ingredients of pharmaceutical compositions for treating or preventing various sGC-related cardiovascular diseases, in particular, peripheral arterial diseases, intermittent claudication, critical limb ischemia, hypertension, and pulmonary hypertension, thereby completing the present invention.

[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.

[Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HTreceptor and 5-HTreceptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HTreceptor and 5-HTreceptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HTreceptor and 5-HTreceptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.

Acylguanidine derivative or salt thereof

Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.

Ornithine derivative

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Tokyo, Japan

Eisuke Nozawa