Astellas Pharma Gmbh

Other

Ludwig Institute for Cancer Research Limited

Imperial Cancer Research Technology, Ltd.

Kotobuki Pharmaceutical Co Ltd

Yamanouchi Pharmaceutical Company Ltd.

Kotobuki Pharmaceuticals Co., Ltd.

Hiroyuki Kaizawa

Minoru Okada

Masahiko Hayakawa

Mitsuaki Ohta

Koyo Matsuda

Mayumi Yamano

Tomonobu Koizumi

Ken-Ichi Kawaguchi

Hiroyuki Moritomo

Ryushi Seo

Kazuyuki Tsuchiya

Kenichi Kawaguchi

Satoshi Yamamoto

Hirofumi Yamamoto

Kazunori Kamijo

Mari Sugita

Akira Kanai

Yusuke Inagaki

Hajime Takamatsu

Kentaro Enjo

Hiroshi Morikawa

Masashi Hiramoto

Akihiro Ishihata

Junichi Kazami

Tadaatsu Hanadate

Hideki Kubota

Takashi Furutani

Kazuhiko Take

Eiji Kawaminami

Hidenori Azami

Kazuyuki Sakamoto

Isao Kinoyama

Masakazu Imamura

Yuta Fukuda

Takatoshi Kanayama

Yutaka Kondoh

Tatsuhisa Takahashi

Nobuaki Taniguchi

Kazuyuki Kuramoto

Takaho Nomura

Takenori Kimura

Noriko Ishikawa

Makoto Takeuchi

Noriyuki Kawano

Issei Tsukamoto

Tomofumi Takuwa

Masahiro Iwata

Kiyoshi Yahiro

Miki Kobayashi

Atsushi Ukai

The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

Pyridine derivative

Substituted imidazo[1,5-a]quinoxalin-4-one compounds of formula (I) described herein exhibit PDE9-inhibitory action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.

Substituted imidazo[1,5-A]quinoxalin-4-ones are useful for preventing or treating storage dysfunction, voiding dysfunction and bladder/urethral diseases

The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.

Pyrazoloquinoline 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 optically substituted lower alkyl, etc.

Substituted amide compound

Substituted imidazo[1,5-a]quinoxalin-4-ones are useful as phosphodiesterase 9 inhibitors.

Substituted imidazo[1,5-a]quinoxalin-4-ones as phosphodiesterase 9 inhibitors

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.

Substituted imidazo[1,5-a]quinoxalin-4(5H)-ones are useful as PDE9 inhibitors.

Substituted imidazo[1,5-a]quinoxalin-4(5H)-ones as PDE9 inhibitors

The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

Fused heteroaryl derivatives

The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.

N-phenyl-(2R,5S)dimethylpiperazine derivative

N-phenyl-(2R,5S) dimethylpiperazine derivative

The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein

Phenylpyridinecarbonylpiperazinederivative

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Tsukuba, Japan

Hiroyuki Kaizawa