Astellas Pharma Gmbh

Ryo Mizoguchi

Eisuke Nozawa

Noritaka Hamada

Hiroshi Shibata

Noriyuki Kawano

Satoshi Miyamoto

Yuji Koga

Tsubasa Watanabe

Takashi Sugane

Kazuhiko Ohne

Takao Okuda

Shunichiro Hachiya

Takahiko Tobe

Takeshi Hanazawa

Toshio Kurosaki

Junya Ohmori

Takenori Kimura

Yuji Awamura

Makoto Kasai

Hiroki Ishioka

Kuniyuki Sano

Takaaki Sakaida

Yu Iwakawa

Tohru Ugawa

A compound which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy is provided.

Amide compound

[Problem] A pharmaceutical composition for treating or preventing various cardiovascular diseases, which have sGC activities based on improvement of cGMP signals, is provided. [Means for Solution] It was found that imidazo[1,2-a]pyridine compounds having a carbamoyl group at the 3-position and a particular cyclic group at the 8-position via a methyleneoxy group, or a salt thereof have sGC activation, and are useful as active ingredients of pharmaceutical compositions for treating or preventing various sGC-related cardiovascular diseases, in particular, peripheral arterial diseases, intermittent claudication, critical limb ischemia, hypertension, and pulmonary hypertension, thereby completing the present invention.

Imidazopyridine compounds

Anytime obtained is uniform crystal of N-(4-fluorophenyl)-N'-phenyl-N&#x2033;-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound A) and/or N,N&#x2032;-bis (4-fluorophenyl)-N&#x2033;-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound B) as a medicament or a starting material for the preparation of the medicament, and provided are a fumarate of the compound A and/or the compound B having excellent stability and a novel crystal thereof. A salt of the compound A and/or the compound B with fumaric acid enables uniform crystal to be anytime obtained, and thus, it is a compound that is very useful as a medicament or a starting material for the preparation of the medicament having excellent stability.

Salt of 1,3,5-triazine-2,4,6-triamine derivative

Object Provided are &#x3b2;-form crystal, &#x3b3;-form crystal, and &#x3b1;-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance. Means for Resolution A solving means includes &#x3b2;-form crystal of 4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole, which shows an endothermic peak at 145 to 150&#xb0; C. according to a differential scanning calorimeter analysis (DSC analysis) and shows X-ray powder diffraction peaks at 9.8, 11.1, 12.8, 13.3, 17.1, 20.2, 21.2 and 22.3 in 2&#x3b8;(&#xb0;), and the like.

Crystals of benzoxadiazole derivative

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Tokyo, Japan

Ryo Mizoguchi