Chugai Seiyaku Kabushiki Kaisha

Takehiro Okada

Kazuo Hattori

Satoshi Niizuma

Toshiyuki Tsukaguchi

Osamu Kondoh

Satoshi Tanida

Miyako Masubuchi

Masaki Shibata

Miyuki Yoshida

Kohei Koyama

Hiroyuki Eda

Kenji Tatsuno

The present invention provides a compound of the formula (I) or a pharmaceutically acceptable salt thereof: 

1-(2H)-isoquinolone derivative

The present invention provides: a compound represented by the following formula (I): [wherein Yand Yrepresent a hydrogen atom or a halogen atom; either one of Yand Yrepresents &#x2014;NRR, and the other represents a hydrogen atom or a halogen atom; X represents an aryl group or a heteroaryl group that may be substituted; Rrepresents a hydrogen atom, or a Calkyl group that may be substituted; and Rrepresents a Calkyl group that is substituted with one or more substituents, &#x2014;COOR, &#x2014;COR, &#x2014;COSR, &#x2014;CONRR, &#x2014;NRR, or &#x2014;C&#x2550;NRR; or Rand R, together with a nitrogen atom to which they are bonded, may form a 4- to 10-membered hetero ring containing at least one nitrogen atom (wherein the hetero ring may be substituted with one or more substituents selected from Group C)], a prodrug thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical, a pharmaceutical composition, or the like, which comprises the compound.

The present invention provides a compound having high antitumor activity, which is useful for therapeutic and preventive agents effective for proliferative diseases such as cancer; a production method thereof; an intermediate compound useful for such production; and a pharmaceutical composition comprising such a compound. The present invention provides a compound represented by the formula (1): wherein X represents an aryl group or heteroaryl group which may be substituted, Cy represents a 4- to 7-membered monocyclic heterocyclic ring or a 8- to 10-membered condensed heterocyclic ring which may be substituted, and Z represents O, S, or NRa; or a prodrug thereof; or a pharmaceutically acceptable salt thereof; and a pharmaceutical and a pharmaceutical composition which comprise the compound.

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Kamakura, Japan

Takehiro Okada