Astellas Pharma Gmbh

Kotobuki Pharmaceutical Co Ltd

Mitsubishi Denki Kabushiki Kaisha

Sanyo Electric Co., Ltd.

Kotobuki Pharmaceuticals Co., Ltd.

Kenichi Kawaguchi

Hiroyuki Kaizawa

Akira Kanai

Yusuke Inagaki

Hajime Takamatsu

Kentaro Enjo

Masashi Hiramoto

Akihiro Ishihata

Kazuyuki Tsuchiya

Hiroshi Morikawa

Junichi Kazami

Tadaatsu Hanadate

Akira Suga

Toru Watanabe

Minoru Okada

Masahiko Hayakawa

Takashi Furutani

Ryushi Seo

Keizo Sugasawa

Hidenori Azami

Isao Kinoyama

Masakazu Imamura

Shunichiro Matsumoto

Tomoaki Abe

Nobuaki Taniguchi

Takashi Shin

Masayuki Tanahashi

Takenori Kimura

Tetsuya Yamamoto

Takeyuki Nagashima

Eiji Kawaminami

Hironori Harada

Hisao Hamaguchi

Hiroshi Suzuki

Sunao Imada

Yorinobu Yoshisato

Seiji Suzuki

Tomoyoshi Imaizumi

Kazuyuki Kuramoto

Mitsuaki Okumura

Kohei Inamura

Hideyuki Watanabe

Kazuhiko Takahashi

Takaho Nomura

Hiroki Ishioka

Takaho Matsuzawa

Yuichiro Ichiyama

Tomohiro Yoshinari

[Problem] To provide a compound useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer. [Means for resolution] The present inventors have studied about a compound that is useful as an active ingredient of a pharmaceutical composition for treating pancreatic cancer and have found that a quinazoline compound has an excellent degradation-inducing action on a G12D mutant KRAS protein and a G12D mutant KRAS inhibition activity and can be used as a therapeutic agent for pancreatic cancer, thus completing the present invention. The quinazoline compound or a salt thereof of the present invention can be used as a therapeutic agent for pancreatic cancer.

Quinazoline compound for inducing degradation of G12D mutant KRAS protein

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

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-(bi-cyclic pyridylmethyl)-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.

Bicyclic pyridine compound

The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent 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-(pyridylmethyl)-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 derivatives

[Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action. [Means for Solution] A novel azolecarboxamide compound in which a thiazole ring or an oxazole ring is bonded to a benzene ring, a pyridine ring, a pyridazine ring, a thiophene ring, a pyrazole ring or a pyrrole ring through carboxamide, or a salt thereof is confirmed to have a potent trkA receptor inhibitory activity, and found to be capable of being used as a therapeutic and/or prophylactic agent which is excellent in efficacy and safety for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, thereby completing the present invention.

Azolecarboxamide compound or salt thereof

Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.

Azolecarboxamide derivative

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

A navigation device in that on each of fixed information having a long update period and update information having a short update period which compose the user service information stored in a navigation device whether or not the user service information is newest, is determined, and the newest information corresponding to at least one of the fixed information and the update information which are determined to be not newest by the determination is acquired from an information supply server, thus, in almost all cases, only the update information is acquired from the information supply server, so it acquires the desired user service information in a short time, and therefore, low communication expenses.

Navigation device, information supplying server and information service system using the same

A superconductor device comprises a Schottky barrier region S.sub.B for selectively passing injected carriers and a collector barrier region L.sub.B for selectively blocking leakage carriers. The Schottky barrier region is formed in a low permittivity region .epsilon..sub.L between the first operating region (B) made of superconductor material and the second operating region (C) made of either semiconductor material or metallic material. A resonance region R is formed in the low permittivity region .epsilon..sub.L.

Superconductor device

Growing community of inventors

Tokyo, Japan

Kenichi Kawaguchi