Astellas Pharma Gmbh

Yoh Terada

Shunichiro Hachiya

Masanori Miura

Ippei Sato

Daisuke Kaga

Kazuhiro Terai

Koji Kato

Hiroyuki Moritomo

Ryushi Seo

Taisuke Takahashi

Yoshimasa Imamura

Makoto Oku

Masanao Sanagi

Takashi Kamikubo

Koji Nagai

Nobuaki Shindo

Takao Okuda

Kazuhiro Ikegai

Susumu Watanuki

Kousei Yoshihara

Keisuke Matsuura

Takashi Shin

Masamichi Mori

Isao Takahashi

Nobuaki Shindou

Ryotaro Ibuka

Nobuaki Amino

Noboru Yamaji

Mai Isomura

Hana Mukai

Masatoshi Taniguchi

Ken-ichi Suzumura

Mitsuo Amase

The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: 

Tetrahydrobenzothiophene compound

[Problem] To provide a compound that has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. [Means for Solution] The present inventors conducted their studies on a compound that has an NPT-IIb inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. As a result, they created an aminoalkyl-substituted N-thienylbenzamide derivative which has NPT-IIb inhibitory action, thereby completing the present invention. The aminoalkyl-substituted N-thienylbenzamide derivative of the present invention has an NPT-IIb inhibitory action and can be used as an agent for preventing and/or treating hyperphosphatemia.

Aminoalkyl-substituted N-thienylbenzamide derivative

To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).

Piperidine derivative or salt thereof

[Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).

Pyrrolidine derivative or salt thereof

The present invention relates to a novel compound which is useful as an agent for prevention and treatment of diseases associated with HDAC, in particular, tumor or cell proliferative diseases. The depsipeptide compound or its pharmaceutically acceptable salt of the present invention has a good HDAC inhibitory activity and an inhibitory activity of cell proliferation against human cancer cells and, therefore, is useful in treatment and improvement of diseases and pathogenic conditions associated with histone acetylation, in particular, tumor or cell proliferative diseases.

Depsipeptide compound

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Chuo-ku, Japan

Yoh Terada