Taiho Pharmaceutical Company Limited

Hideki Kazuno

Tetsuji Asao

Tsutomu Sato

Masakazu Fukushima

Shingo Yano

Junichi Yamashita

Yukio Tada

Norihiko Suzuki

Tomohiro Emura

Tomonobu Mutsumi

Toshihiro Sakamoto

Hitomi Kondo

Tomohiro Yamamoto

Akira Matsuda

Motoaki Tanaka

Tetsuya Sugimoto

Makoto Nomura

Masato Washinosu

The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof: wherein R, R, R, L, L, L, A, X, and m are as described in the specification.

Phenol compound or salt thereof

An indazole compound represented by the following Formula (I) or a salt thereof: wherein X, R, R, ring A, L, L, L, and Rare as defined in this specification.

Indazole compound or salt thereof

Crystal Form I of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting powder X-ray peaks at two or more angles selected from the group consisting of 11.6&#xb0;, 17.2&#xb0;, 17.8&#xb0;, 23.3&#xb0;, 27.1&#xb0;, and 29.3&#xb0; as a diffraction angle (2&#x3b8;&#xb1;0.2&#xb0;).

Stable crystal form of tipiracil hydrochloride and crystallization method for the same

An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4 (1H,3H)-pyrimidinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4 (1H,3H)-pyrimidinedione hydrochloride exhibiting characteristic peaks at angles of 11.6&#xb0;, 17.2&#xb0;, 17.8&#xb0;, 23.3&#xb0;, 27.1&#xb0;, and 29.3&#xb0; as a diffraction angle (2&#x3b8;&#xb1;0.1&#xb0;) in powder X-ray diffraction.

An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting characteristic peaks at angles of 11.6&#xb0;, 17.2&#xb0;, 17.8&#xb0;, 23.3&#xb0;, 27.1&#xb0;, and 29.3&#xb0; as a diffraction angle (2&#x3b8;&#xb1;0.1&#xb0;) in powder X-ray diffraction.

The invention relates to novel uracil derivatives having excellent inhibiting effects on human derived thymidine phosphorylates and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators and antitumor agents containing such novel compounds, and a process for their preparation and use are described. The novel uracil derivative compounds are represented by the general formula (1&prime;):

Uracil derivatives and antitumor effect potentiator and antitumor agent containing the same

The invention relates to novel uracil derivatives having excellent inhibiting effects of human derived thymidine phosphorylase and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators, antitumor agents containing such novel compounds, and a process for their preparation and use is described. The novel compounds satisfy the general formula (1): ##STR1##

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Ibaraki, Japan

Hideki Kazuno