Sankyo Company, Limited

Masao Arakawa

Masakatsu Kaneko

Hideo Nakao

Masami Fukushima

Bunji Shimizu

Fusaaki Shimizu

Shigeo Iwasaki

Michio Namikoshi

Tsuneo Baba

Shigenobu Okuda

Acylated derivatives of rhizoxin and of rhizoxin-2-ene may be prepared by reacting rhizoxin or rhizoxin-2-ene with an acid or reactive derivative thereof. They have excellent anti-tumor activity.

Rhizoxin esters and salts, their pharmaceutical use as anti-tumor agents

5-Fluorouracil compounds having a glycoside substituent connected to the 5-fluorouracil nucleus through a bridging oxygen atom; and having anti-tumor activity.

5-Fluorouracil derivatives and process for preparing thereof

Nitrosourea derivatives represented by the formula ##STR1## wherein A represents a group of the formula B--Y-- in which B is an unsaturated 5- or 6-membered heterocyclic group which has the as hetero atom at least one nitrogen atom, an unsaturated 9-membered heterocyclic group which has as the hetero atom at least one nitrogen atom and a bicyclic fused ring or an unsaturated 10-membered heterocyclic group which has as the hetero atom at least one nitrogen atom and a bicyclic fused ring, the heterocyclic groups optionally having alkyl, alkoxy, hydroxyl, amino, hydroxyalkyl or halogen as ring substituent and Y represents a group of the formula --(CH.sub.2).sub.m -- in which m is an integer of 1 or 2, the group optionally having alkyl as a substituent; A group of the formula ##STR2## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 may be the same or different and each represents a hydrogen atom or an alkyl group; or a group of the formula ##STR3## in which R's may be the same or different and each represents a halogen atom or an alkyl group, n is an integer of 0 to 3 inclusive and Z is an ethylene group which may be substituted with alkyl; and X represents a halogen atom and acid addition salts thereof. The Compounds of the present invention are prepared from the corresponding 2-halogeno-ethylurea derivatives by means of conventional nitrosation procedures and useful as an antileukemic drug for various types of leukemia.

Nitrosourea derivative

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Hiromachi, Japan

Masao Arakawa