Water-soluble SHPs as novel alkylating agents

   
   

The present invention relates to compounds according to the structure (I): ##STR1## Where R is --CH.sub.3 or --CH.sub.2 CH.sub.2 Cl; R' is C.sub.1 -C.sub.7 alkyl or --CH.sub.2 CH.sub.2 Cl; R.sub.2 or R.sub.4 is OPO.sub.3 H.sub.2, NO.sub.2, OCO(Glu-OH), NHCO(Glu-OH), NHR.sub.7 and unassigned groups of R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are, independently H, F, Cl, Br, I, OH, OPO.sub.3 H.sub.2, OCH.sub.3, CF.sub.3, OCF.sub.3, NO.sub.2, CN, SO.sub.2 CH.sub.3, SO.sub.2 CF.sub.3, COCH.sub.3, COOCH.sub.3, SCH.sub.3, SF.sub.5, NH.sub.2, NHR.sub.7, N(CH.sub.3).sub.2, OPO.sub.3 H.sub.2, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R.sub.2, R.sub.3, R.sub.4, R.sub.5 or R.sub.6 are other than H, the other two of unassigned groups of R.sub.2, R.sub.3, R.sub.4, R.sub.5 or R.sub.6 are H. R.sub.7 is H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

La actual invención se relaciona con los compuestos según la estructura (i): ## del ## STR1 Donde está -- CH.sub.3 o -- cl R de CH.sub.2 CH.sub.2; R ' es C.sub.1 - C.sub.7 alkyl o -- cl de CH.sub.2 CH.sub.2; R.sub.2 o R.sub.4 es OPO.sub.3 H.sub.2, NO.sub.2, OCO(Glu-OH), NHCO(Glu-OH), NHR.sub.7 y los grupos no asignados de R.sub.2, de R.sub.3, de R.sub.4, de R.sub.5 y de R.sub.6 son, independientemente H, F, cl, Br, I, OH, OPO.sub.3 H.sub.2, OCH.sub.3, CF.sub.3, OCF.sub.3, NO.sub.2, CN, SO.sub.2 CH.sub.3, SO.sub.2 CF.sub.3, COCH.sub.3, COOCH.sub.3, SCH.sub.3, SF.sub.5, NH.sub.2, NHR.sub.7, N(CH.sub.3).sub.2, OPO.sub.3 H.sub.2, o un grupo alkyl C1-C7 a condición de que cuando cualesquiera dos de grupos no asignados de R.sub.2, de R.sub.3, de R.sub.4, de R.sub.5 o de R.sub.6 están con excepción de H, los otros dos de grupos no asignados de R.sub.2, R.sub.3, R.sub.4, R.sub.5 o R.sub.6 son H. R.sub.7 son H o polyglutamyl según lo descrito. El ácido fosfórico y el ácido glutamic pueden ser un ácido libre o farmacéutico una sal aceptable de eso.

 
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