Astellas Pharma Gmbh

Tacurion

Kazuyoshi Obitsu

Hiroyuki Koshio

Souichirou Kawazoe

Takahiro Akiba

Kiichi Sato

Shun Hirasawa

Akio Miyafuji

Junji Itoh

Masaaki Hirano

Fukushi Hirayama

Yuji Koga

Keizo Sugasawa

Eiji Kawaminami

Isao Kinoyama

Shunichiro Matsumoto

Kei Ohnuki

Toshiyuki Kusayama

Hiroshi Nagata

Hideki Kubota

Masaki Abe

Takao Okuda

Ken-Ichi Suzuki

Susumu Watanuki

Ryutaro Wakayama

Ken-ichi Suzuki

Koichiro Harada

The present invention provides a method for producing a 4,4,7-trifluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound which has an superior agonistic activity to an arginine vasopressin V2 receptor and is useful as an active ingredient for a pharmaceutical composition for preventing and/or treating urinary frequency, urinary incontinence, enuresis, central diabetes insipidus, nocturia, nocturnal enuresis, or the like; and useful intermediates for use in the methods. The production method of the present invention is suitable for the industrial production of a medicament, because of a smaller number of steps, a higher yield, and a lower cost, as compared with the methods in the related art.

Method for producing 4,4,7-trifluoro-1,2,3,4-tetrahydro-5H-1-benzazepine compound and intermediate used in the method

Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like. In addition, since the compound of the invention is excellent in metabolic stability in human and also is less in drug interaction, it has more desirable properties as a medicament to be used for the aforementioned diseases.

Benzimidazolylidene propane-1,3-dione derivative or salt thereof

Benzimidazolylidene propane-1,3 dione derivative or salt thereof

A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.

2-Acylaminothiazole derivative or salt thereof

2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of megakaryocytic colonies and which are useful for treating thrombocytopenia are provided.

2-acylaminothiazole derivative or salt thereof

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Tokyo, Japan

Kazuyoshi Obitsu