Other

Ajinomoto Co., Ltd.

The Nissin Sugar Manufacturing Co., Ltd.

Nippon Universal Pharmaceutical Co., Ltd.

Tetsuo Suami

Takashi Hisamatsu

Tomoya Machinami

Kunisuke Izawa

Kazuo Ohishi

Tsuyoshi Shiio

Seiichi Nishi

Shuichi Oki

Masao Sako

Yushi Itoh

Platinum complexes of cis-diaminocyclohexanol or cis-diaminocyclohexane, with the exclusion of platinum complexes of 2-deoxystreptamine, having high anti-tumor activity, low toxicity, water-solubility and exhibiting no cross-resistance to cis-platin.

Platinum complexes and uses therewith

6-Iodoethylated starch and process for preparing the same are disclosed. The 6-idodethylated starch contains one iodine attached per 5 glucose units. Said compound is useful as a contrast agent for X-ray examination, especially for opacifying the vascular os lymphatic vessel. Said compound is produced by reacting 6-hydroxyethylated starch with N-iodosuccinimide in the presence of triphenylphosphine.

6-iodoethylated starch and process for preparing the same

Novel nitrosourea derivatives are provided which possess a high level of inhibitory activity against leukemia and tumors and which are therefore useful for pharmaceutical purposes. The compounds have the structure represented by formula (I): ##STR1## wherein R.sub.0 represents --OH or --OC.sub.m H.sub.2m+1 where m is an integer of 1 to 3 and one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represents ##STR2## where X is ##STR3## or an alkylene group of 1 to 3 carbon atoms, n is an integer of 1 to 3 and Y is the group on the .alpha.-carbon atom of an .alpha.-amino acid and each of the remaining three represents --OH; or wherein R.sub.0 represents ##STR4## and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent --OH; or by formula (II): ##STR5## wherein X and n have the same meanings as above; and p is an integer of 1 to 5.

Nitrosourea derivatives

Nitrosourea derivatives are provided which possess a high level of inhibitory activity against leukemia and tumors and which are therefore useful for pharmaceutical purposes. The compounds have the structure represented by formulae (I), (II) and (III): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.4 may be the same or different and each represent a hydrogen atom or an alkyl, aryl, aralkyl, alkanoyl or a heterocyclic group; R.sup.3 represents the residual group on the .alpha.-carbon atom of an .alpha.-amino acid; n represents 2 or 3; X represents a halogen atom selected from chlorine, fluorine and bromine; and Ac represents an alkanoyl group.

Novel nitrosourea derivatives of sucrose having a structure expressed by the general formula: ##STR1## wherein A.sup.1 and A.sup.2 denote a group of OR or ##STR2## either A.sup.1 or A.sup.2 represents a group of ##STR3## and R shows a hydrogen atom or acyl group, and a method of manufacturing said derivatives. Said novel nitrosourea derivatives of sucrose have antitumor activity.

Nitrosourea derivatives of sucrose

5,6-Dideoxyneamine, useful as an antimicrobial agent, and a process for preparing 5,6-dideoxyneamine.

Neamine derivatives and process for preparing the same

Novel nitrosourea derivatives are provided which possess a high level of inhibitory activity against leukemia and tumors and other are therefore useful for pharmaceutical purposes. The compounds have the structure: ##STR1## wherein one of X and Y represents a hydroxyl and another of them represents a group --NHCONNOCH.sub.2 CH.sub.2 Cl; R represents a hydrogen, alkyl or aryl; and .about. represents a single bond which may be in the .alpha.- or .beta.-stereochemical configuration and are prepared by nitrosating a corresponding urea compound with a nitrosating agent in a manner known per se.

Novel nitrosourea derivatives

Novel nitrosourea compounds are provided which possess a high level of inhibitory activity against leukemia and tumors with a low toxicity and which are therefore useful for pharmaceutical purposes. The compounds have the chemical structure: ##STR1## wherein .about. represents a single bond which may be in the .alpha.- or .beta.-position and are prepared by nitrosating a urea compound of the formula: ##STR2## with a nitrosating agent in a manner known per se.

Nitrosourea pentose compounds

New nitrosourea derivatives are provided, which possess a high inhibitory activity against the leukemia and tumors with a low toxicity and which are useful for pharmaceutical purposes. The compounds have the formula ##STR1## wherein A represents a glycosyl group, a monovalent residue of methyl glucoside or of alditol, a N-substituted carbamoyloxyalkyl group or a hydroxy-substituted cyclohexyl group when n is 1, or A represents a tetravalent residue of ribostamycin when n is 4 and R represents a lower alkyl or halo-alkyl group and are prepared by treating a compound of the formula ##STR2## with a nitrosating agent.

Novel nitrosourea derivatives are provided which possess a high inhibitory activity against the leukemia and tumors with a low toxicity and a good stability against humidity and which are useful for pharmaceutical purposes. The compounds have the structure: ##STR1## wherein R.sup.1 represents hydroxyl or alkanoyloxy containing 2-4 carbon atoms; R.sup.2 represents hydrogen or alkanoyl containing 2-4 carbon atoms; R.sup.3 represents alkanoyl containing 2-4 carbon atoms; and R.sup.4 represents alkyl or halo-substituted alkyl containing 1-4 carbon atoms.

Novel inosadiamine derivatives of the formula ##STR1## exhibit high effectiveness against various mammalian tumor systems.

Antitumor agents

5,6-Epineamine represented by the formula (I) ##STR1## and a process for preparing 5,6-epineamine of the formula (I) above which comprises hydrolyzing the epoxy group of a compound of the formula (II) ##STR2## wherein R.sup.1 represents a protective group for an amino group and R.sup.2 represents a protective group for a hydroxyl group, and removing the protective groups for the amino and hydroxyl groups.

5,6-Epineamine and process for preparing the same

Aminocyclitol derivatives, 5-deoxyneamine and 6-deoxyneamine, having antimicrobial activities against various antibiotic-resistant microorganisms, a process for producing 5-deoxyneamine and 6-deoxyneamine and intermediates useful in producing the aminocyclitol derivatives.

Aminocyclitol derivatives and process for producing the same

New nitrosourea derivatives are provided, which possess a high inhibitory activity against the leukemia and tumors with a low toxicity and which are useful for pharmaceutical purposes. The compounds have the formula ##STR1## WHEREIN A represents a glycosyl group, a monovalent residue of methyl glucoside or of alditol, a N-substituted carbamoyloxyalkyl group or a hydroxy-substituted cyclohexyl group when n is 1, or A represents a tetravalent residue of ribostamycin when n is 4 and R represents a lower alkyl or halo-alkyl group and are prepared by treating a compound of the formula ##STR2## WITH A NITROSATING AGENT.

Growing community of inventors

Tokyo, Japan

Tetsuo Suami