Novel nitrosourea compounds and process for preparing the same

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 22, 536 53, 536 18, A61K 3170, C07H 1312, A61K 3173

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042410525

ABSTRACT:
A nitrosourea compound of the formula: ##STR1## wherein R.sup.1 is an alicyclic group having 3 to 6 carbon atoms, phenyl, phenyl substituted with one to substituents selected from halogen, lower alkyl, lower alkoxy, hydroxy and nitro, or a heteromonocyclic group selected from oxiranyl, tetrahydrofuryl, 1,3-dioxolanyl, 1,4-dioxanyl, morpholino, tetrahydro-S,S-dioxo-thienyl, furyl, thienyl and pyridyl; R.sup.2 is aldopentofuranosyl, aldo-pentopyranosyl, aldo-hexopyranosyl or O-aldo-hexopyranosyl-(1.fwdarw.4)-aldo-hexopyranosyl; and A is a single bond or straight or branched alkylene having one to 3 carbon atoms, is prepared by nitrosation of a compound of the formula: ##STR2## wherein R.sup.1, R.sup.2 and A are the same as above. Said nitrosourea compound is useful as an anti-tumor or anti-leukemic agent however, effectiveness in human beings has not yet been demonstrated.

REFERENCES:
patent: 3577406 (1971-05-01), Hessler
patent: 4086415 (1978-04-01), Suami et al.
patent: 4156777 (1979-05-01), Kimura
patent: 4157439 (1979-06-01), Suami
Noller "Chemistry of Organic Compounds," W. B. Saunders Co., Philadelphia, Pa., 1965, p. 598.

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