Astellas Pharma Gmbh

Taisuke Takahashi

Hiroaki Tanaka

Kenji Negoro

Hajime Takamatsu

Jun Maeda

Takanori Koike

Kazuhiro Yokoyama

Hiroyuki Koshio

Ryushi Seo

Takafumi Shimizu

Shunichiro Hachiya

Norio Asai

Yoh Terada

Makoto Oku

Masanao Sanagi

Karl Bruce Thor

Yasuhito Nagai

Keiko Kawabata

Takashi Kamikubo

Yusuke Inagaki

Issei Tsukamoto

Kazuhiro Ikegai

Kousei Yoshihara

Michinori Akaiwa

Hisashi Mihara

Takashi Shin

Keisuke Matsuura

Ryotaro Ibuka

Hideyoshi Fuji

Hana Mukai

[Problem] To provide a compound which is useful as an active ingredient for a pharmaceutical composition for preventing or treating urine storage dysfunction, voiding dysfunction, lower urinary tract dysfunction, and the like. [Means for Solution] The present inventors have found that a thiazole derivative substituted with pyrazinylcarbonylamino at the 2-position is an excellent muscarinic Mreceptor-positive allosteric modulator and is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic Mreceptor, thereby completing the present invention. 2-Acylaminothiazole derivative or a salt thereof of the present invention is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic Mreceptor, for example voiding dysfunction such as underactive bladder.

2-acylaminothiazole derivative or salt thereof

A compound which is useful as an active ingredient for a pharmaceutical composition for treating urine storage dysfunction, voiding dysfunction, lower urinary tract dysfunction, and the like. The present inventors have found that a 2-aminothiazole derivative has an excellent muscarinic Mreceptor-positive allosteric modulator activity and is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic Mreceptor, thereby completing the present invention. 2-aminothiazole derivative or a salt thereof of the present invention is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic Mreceptor, for example voiding dysfunction such as underactive bladder.

2-aminothiazole derivative or salt thereof

Provided is a compound which is useful as an agent for treating or preventing 5-HTreceptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. The present inventors have investigated compounds having a 5-HTreceptor agonist activity and have found that the benzazepine compounds of the present invention have an excellent 5-HTreceptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HTreceptor agonist activity and can be used as an agent for treating or preventing 5-HTreceptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.

Benzazepine compound

Thiazole derivatives having pyrazine-2-carbonylamino substituted at the 2-position of the following formula (I): are excellent muscarinic Mreceptor positive allosteric modulators, and are useful for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic Mreceptor. The 2-acylaminothiazole derivatives and salts thereof can be used for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic Mreceptor, for example, voiding dysfunctions such as underactive bladder.

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

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Tokyo, Japan

Taisuke Takahashi