Astellas Pharma Gmbh

Astella Pharma Inc.

Akio Kakefuda

Chikashi Saitoh

Kentaro Sato

Jun Maeda

Hiroyuki Koshio

Takahiro Ishii

Takashi Sugane

Takatoshi Kanayama

Tatsuhisa Takahashi

Jotaro Suzuki

Fumie Narazaki

Chisato Kanai

Takashi Furutani

Akio Kamikawa

Issei Tsukamoto

Kentaro Enjo

Seijiro Akamatsu

Masaaki Hirano

Tatsuya Niimi

Minoru Yasuda

Ippei Sato

Kazushi Watanabe

Yutaka Kondoh

Ryutaro Wakayama

Masanao Sanagi

Tomohiko Yamaguchi

Kenichi Suzumura

Yasushi Amano

As a result of studies on compounds having a selective inhibitory activity against 17&#x3b2;HSD type 5, the present inventors have confirmed that a {1-[(indol-2-yl)carbonyl]piperidyl}alkanol derivative has a potent selective inhibitory activity against 17&#x3b2;HSD type 5. The invention has been completed based on these findings. The compound of the present invention can be used as an agent for treating and/or an agent for preventing diseases associated with 17&#x3b2;HSD type 5, such as benign prostatic hyperplasia and prostate cancer, without accompanying adverse effects due to a decrease in testosterone.

Piperidine derivative

A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound

To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17&#x3b2;HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17&#x3b2;HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.

17&#x3b2;HSD type 5 inhibitor

A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.

4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or salt thereof

4,4-difluoro-1,2,3,4-tetrahydro-5h-1-benzazepine derivative or salt thereof

To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof.

1,4,5.6-tetrahydroimidazo[4,5-d]diazepine derivatives or salts thereof

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Tokyo, Japan

Akio Kakefuda