| 摘要 |
The invention comprises compounds of formula R1.Q.CO.Q1.R in which R1 represents a group (X.CH2CH2)2N-Ar-, X representing a chlorine or bromine atom and Ar representing a p-phenylene group, Q and Q1 each represent an oxygen atom, a sulphur atom or an -NH- group and may be the same or different, and R represents a sugar residue, an aryl group different from R1 or a lower (i.e. 1-4 carbon atom) alkyl group, said aryl or lower alkyl group being substituted by a saltforming group; and their derivatives in which the salt-forming group is converted into a salt or ester. In examples, the sugar residue is D-galactose and 1,2:3,4-di-O-isopropylidene-D-galactose, and the salt forming group carboxyl, phenolic hydroxy, amino and dialkylamino; derivatives obtained are alkyl esters, and salts, for example methiodide, S-benzylthiouronium and picrate salts. Methods of preparation referred to are the reaction of compounds R1.QH and OCN.R (Q1=NH); of compounds R1.Q.CO.halogen and H2N.R (Q1=NH); of compounds R1.QH and halogen.COOR (Q1=O); of compounds R1.QH and Cl.CO.S.R (Q1=S); and of compounds R.SH and R1.NCO, R1.O.CO.Cl or R1.S.CO.Cl (Q1=S). p - N,N - Diethylaminophenyl isocyanate hydrochloride is prepared by the action of phosgene on the corresponding aniline. In the Provisional Specification X represents any halogen atom. Pharmaceutical compositions comprise one or more of the compounds of the invention dissolved in a compatible fluid carrier, for injection. Intramuscular and interperitoneal administration are mentioned. The compounds have anti-tumour activity. |
