Astellas Pharma Gmbh

Other

Takatoshi Kanayama

Tatsuhisa Takahashi

Kentaro Sato

Jun Maeda

Takahiro Ishii

Takashi Sugane

Akio Kakefuda

Chikashi Saitoh

Jotaro Suzuki

Chisato Kanai

Fumie Narazaki

Hiroyuki Kaizawa

Tomoyuki Saito

Ryushi Seo

Kazuhiko Take

Eiji Kawaminami

Takafumi Shimizu

Kazuyuki Sakamoto

Shunichiro Matsumoto

Yuta Fukuda

Yutaka Kondoh

Kazuyuki Kuramoto

Shigeo Matsui

Daisuke Suzuki

Hiroaki Tanaka

Shingo Yamasaki

Hideki Kubota

Kazuhiro Yokoyama

Kazushi Watanabe

Satoshi Hayashibe

Nobuyuki Shiraishi

Hiroaki Hoshii

Naoto Katoh

Junya Ohmori

Chiharu Mori

[Problem] To provide a compound useful as a MTand/or MTreceptor agonist. [Solution] The present inventors have studied on MTand/or MTreceptor agonists, and have confirmed that indole compounds have the activity. As a result, the present invention is accomplished. That is, a compound represented by formula (I) or a salt thereof according to the present invention has a MTand/or MTreceptor agonistic activity and has a low ability of migrating into central nervous system. Therefore, the compound or a salt thereof can be used as a peripheral MTand/or MTreceptor agonist, and therefore can be used as a therapeutic and/or prophylactic agent for urinary incontinence, particularly stress urinary incontinence and mixed urinary incontinence. 

Indole compound

The present invention relates to indole carboxamide compounds of formula (I) or a salt thereof wherein R, R, R, R, R, R, Rand Rhave the meanings as indicated herein, and are MT1 and/or MT2 receptor agonists useful for treating and/or preventing urological diseases.

Indole carboxamide derivative

A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula:  In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or &#x2014;(CRR)&#x2014;; n is 1, 2, 3, or 4; Rand Rare hydrogen, etc.; Yto Yare each CRor N; each Ris hydrogen, etc.; Rand Rare hydrogen, etc.; m is 1, 2, or 3; Ris hydrogen, etc.; and Ris an optically substituted lower alkyl, etc.

Substituted amide compound

A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or &#x2014;(CRR)&#x2014;; n is 1, 2, 3, or 4; Rand Rare hydrogen, etc.; Yto Yare each CRor N; each Ris hydrogen, etc.; Rand Rare hydrogen, etc.; m is 1, 2, or 3; Ris hydrogen, etc.; and Ris an optionally substituted lower alkyl, etc.

Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. A novel compound or a salt thereof, which is characterized in that it has an amino group and R(lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3 -dihydro-1-benzofuran, 2,3-dihydro-1-benzothiophene, indoline ring, or the like, and has Rand R(the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.

Aminoindane derivative or salt thereof

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.

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Tokyo, Japan

Takatoshi Kanayama