Wakunaga Seiyaku Kabushiki Kaisha

Shunsou Hatono

Akira Yazaki

Yuzo Hirao

Masaharu Yokomoto

Susumu Yoshida

A bile acid derivative of the following formula (I): ##STR1## wherein: X is a halogen atom; R.sub.1 is a hydrogen atom or a lower alkyl group; Y is ##STR2## (wherein n is an integer of from 0 to 5); each of R.sub.2 and R.sub.3 is a hydrogen atom or a hydroxyl group; R.sub.4 is a hydroxyl group, lower alkoxyl group, ##STR3## (wherein R.sub.5 is a hydrogen atom or a lower alkoxy group, R.sub.6 is a carboxyl group, benzyloxycarbonyl group or sulfonyl group, or a salt thereof, and m is an integer of from 1 to 4); the intermittent line, . . . , is an .alpha.-bond; and the wavy line,  , is an .alpha.- or .beta.-bond, and a salt thereof, and a process for production thereof. This bile acid derivative has carcinostatic activity and yet is of low toxicity. Accordingly, this compound can be used as a carcinostatic agent.

Bile acid derivatives, their salts and production thereof

A bile acid derivative having carcinostatic activity represented by the following formula (1): ##STR1## wherein each of R.sub.1 and R.sub.2 is a hydrogen atom or a hydroxyl group, R.sub.3 is a hydroxyl group, benzyloxyl group or --NH--CH.sub.2n R.sub.5 (wherein R.sub.5 is a carboxyl group or sulfonyl group, and n represents the integer of 1 or 2), X is a halogen atom, R.sub.4 is a hydrogen atom or XCH.sub.2 CH.sub.2 --,.chi. is an .alpha.-bond, and .chi. is an .alpha.- or .beta.-bond is produced by the steps (a) and (b), the steps (a), (b) and (c), or the steps (a), (b), (c) and (d) described below:

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Hiroshima, Japan

Shunsou Hatono