Astellas Pharma Gmbh

Takashi Shin

Ryushi Seo

Hidenori Azami

Shunichiro Matsumoto

Akira Suga

Toru Watanabe

Keizo Sugasawa

Kenichi Kawaguchi

Tomoaki Abe

Kei Ohnuki

Masayuki Tanahashi

Masaaki Hirano

Takashi Kamikubo

Yuki Sawada

Hirofumi Yamamoto

Takeyuki Nagashima

Takanori Koike

Tomoyuki Saito

Itsuro Shimada

Eiji Kawaminami

Hironori Harada

Isao Kinoyama

Hisao Hamaguchi

Shunichiro Hachiya

Hiroyuki Hisamichi

Taisuke Takahashi

Kousei Yoshihara

Kazuyuki Kuramoto

Tatsuhisa Takahashi

Yoh Terada

Keisuke Matsuura

Makoto Oku

Toshiyuki Kusayama

Masanao Sanagi

Takaho Nomura

Kazuhiko Osoda

Takaho Matsuzawa

Shigetoshi Kikuchi

Hana Mukai

Compounds of formula (I) and salts thereof: wherein the variables are defined herein, are useful for the treatment of breast cancer.

Bicyclic nitrogen-containing aromatic heterocyclic amide compound

[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

It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by &#x2014;SO&#x2014;Rin a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.

Propane-1,3-dione 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

Takashi Shin