Ishihara Sangyo Kaisha, Ltd.

Kenji Kon

Hideo Sugi

Nobutoshi Yamada

Sadanori Mizukoshi

Hiroshi Okada

Fuminori Kato

Hiroyuki Mori

Taiji Katayama

Masamitsu Tsukamoto

The present invention provides a substituted benzoylurea derivative having the formula (I), ##STR1## (wherein Q is a --R.sub.1 N(Z.sub.2)Z.sub.3 group or a --R.sub.2 N(Z.sub.4)COR.sub.1 N(Z.sub.2)Z.sub.3 group, R.sub.1 and R.sub.2 are respectively an alkanediyl group which may be substituted with a lower alkylthio group or a phenyl group, Z.sub.1, Z.sub.2, Z.sub.3 and Z.sub.4 are respectively a hydrogen atom or a lower alkyl group, R.sub.1 and Z.sub.2 may be bonded with each other to form a heterocyclic ring with an adjacent nitrogen atom, X is a halogen atom, a lower alkyl group or a CF.sub.3 group, and Y is a halogen atom) or its salt, effective as an antitumor agent; a method for producing the same; an antitumor composition containing the same; and an intermediate product for producing the same.

Substituted benzoylurea derivatives or their salts

An immuno-suppressive agent containing, as an effective component, an, enopyranose derivative of the following formula (I) or its salt: ##STR1## wherein R.sup.1 is a hydrogen atom, alkyl which may be substituted, alkenyl, alkynyl, --OSO.sub.2 R.sup.7, a halogen atom, --OCOR.sup.7, --NHCOR.sup.8, alkoxy, phenyl which may be substituted or a saccharose residue, R.sup.2 is a hydrogen atom or alkyl, R.sup.3 is a hydrogen atom or a halogen atom, R.sup.4 is a hydrogen atom, --COR.sup.9, silyl which may be substituted or alkyl which may be substituted, one of R.sup.5 and R.sup.6 is hydroxyl, alkoxy which may be substituted, a saccharose residue, cycloalkyloxy which may be substituted or --OCOR.sup.10 and the other is a hydrogen atom or alkyl which may be substituted, or R.sup.4 and R.sup.5 together form a single bond, while R.sup.6 is a hydrogen atom or alkyl which may be substituted, each of R.sup.7, R.sup.9 and R.sup.10 is alkyl or phenyl which may be substituted, R.sup.8 is alkyl, phenyl which may be substituted or benzyloxy, X is a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted, pyridyl which may be substituted, furanyl which may be substituted, thienyl which may be substituted, formyl, --COR.sup.11, --C(W.sup.1)W.sup.2 R.sup.11 or --SO.sub.2 R.sup.11, R.sup.11 is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted, or a polycyclic heterocycle group which may be substituted, W.sup.1 is an oxygen atom or a sulfur atom, W.sup.2 is an oxygen atom, a sulfur atom or --NH--, Y is a hydrogen atom, alkyl which may be substituted, alkenyl which may be substituted or alkynyl which may be substituted.

Immuno-suppressive agent

Exo-3',4'-O-benzylidene-3'-dimethylchartreusin (exo-BDMC) or its salts and 3'-demethylchartreusin (3'-DMC) or its salts are provided according to the present invention. Exo-BDMC and its salts are useful for antitumorous agents and antibacterial agents. 3'-DMC and its salts are useful as starting materials for producing exo-BDMC.

Exo-3',4'-O-benzylidene-3'-demethylchartreusin and its salts

This invention relates to a novel chartreusin derivative of the general formula (I): ##STR1## and a salt thereof. This chartreusin derivative and a salt thereof have an excellent antitumor activity, which is exhibited even when the site of cancer inoculation and the site of drug administration are different. This invention further relates to an antitumorous composition containing the above-mentioned compound as active ingredient. This invention furthermore relates to a process for producing the above-mentioned chartreusin derivative or salt thereof.

Chartreusin derivatives and salts thereof

This invention relates to a novel chartreusin derivative of the general formula (I): ##STR1## and a salt thereof. This chartreusin derivative and a salt thereof have an excellent antitumor activity, which is exhibited even when the site of cancer inoculation and the site of drug administration are different. This invention further relates to a antitumorous composition containing the above-mentioned compound as active ingredient. This invention furthermore relates to a process for producing the above-mentioned chartreusin derivative or salt thereof.

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Moriyama, Japan

Kenji Kon