Japan Tobacco Inc.

Yoshikazu Hori

Shinichi Kikuchi

Hiroyuki Abe

Tetsuya Iida

Toshiyuki Sakai

Mitsuru Takahashi

Masahiro Sakata

Takayuki Yamaguchi

Shinji Yata

Hisashi Kawasaki

Yoshihisa Koga

Takayuki Yamasaki

Wataru Kondo

Kazuhide Hayakawa

Takayuki Yoshida

Hironori Kurachi

Masahiro Tamaru

Toyomichi Nanayama

Steven Wade Andrews

Julia Haas

Takuya Matsuo

Takashi Inaba

Ellen Ruth Laird

Makoto Shiozaki

Takashi Watanabe

Akira Suma

Tatsuya Matsumoto

Nicole M Littmann

Katsutaka Yasue

Atushi Sakai

Andrew M Fryer

Takafumi Matsuo

Yuichi Shinozaki

Hiroto Imai

Tamotsu Negoro

Hidekazu Ozeki

The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.

Pyrimidine compound and medical use thereof

To provide a compound having an excellent inhibitory effect on vanilloid receptor subtype 1 (VR1) activity which is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, acute pain, chronic pain, neuropathic pain, rheumatoid arthritis pain, neuralgia, etc. and a pharmaceutical composition containing the compound. The object has been attained by a condensed benzamide compound represented by the following formula (the symbols in the formula have the same meanings defined in the specification) or its salt: 

Condensed benzamide compounds and inhibitors of vanilloid receptor subtype 1 (VR1) activity

A 3,4-dihydrobenzoxazine compound of the present invention is represented by the following formula [1] (wherein X is a nitrogen atom or CR; Ris a hydrogen atom or a halogen atom; Ris a C1-6 alkoxy group which may be substituted with the same or different 1 to 5 substituents selected from a halogen atom and a hydroxyl group; and Ris a halogen atom. However, Ris a halogen atom when X is CR). This compound is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, etc. 

3,4-dihydrobenzoxazine compounds and inhibitors of vanilloid receptor subtype 1 (VRI) activity

The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein Ris &#x2014;(CH)&#x2014;X&#x2014;(CH)-Aetc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and Ais a substituted Chydrocarbon ring group, etc.; Rand Rare the same or different and each is a hydrogen atom, &#x2014;(CH)&#x2014;X&#x2014;(CH)-A, etc., wherein p and q are the same or different and each is 0 to 6, Xis a single bond, etc. and Ais an optionally substituted Chydrocarbon ring group, etc.; Ris &#x2014;COR, etc., wherein Ris a hydrogen atom, etc.; and Rand Rare the same or different and each is a hydrogen atom, &#x2014;(CH)&#x2014;X&#x2014;(CH)&#x2014;R, etc., wherein m12 and m12 are the same or different and each is 0 to 6, Xis a single bond, etc. and Ris a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.

Cyclopropane compounds and pharmaceutical use thereof

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Takatsuki, Japan

Yoshikazu Hori