Abstract: A process for preparing a 3-dihalobenzyl-2,4-quinazolinedione derivative represented by the formula (V): (wherein X1, X2, X3 are independently a halogen atom, and A is an alkylene group), which comprises: reacting a dihalobenzyl derivative represented by the formula (III): (wherein X2 and X3 are each as defined above, and L is an acid residue) with a 2,4-quinazolinedione derivative having a carboxyalkyl group represented by the formula (I): (wherein X1 and A are each as defined above) to selectively substitute a hydrogen atom of an imino group at the 3-position of the derivative (1). The above process enables the efficient preparation of the compounds of the above formula (V) useful as inhibitors against aldose reductases, makes it possible to secure the safety and hygiene of workers, and can facilitate waste disposal to reduce the expenses, thus being industrially extremely advantageous.

Abstract: New nucleoside derivatives possessing strong anti-tumor activity with low toxicity, represented by the general formula: ##STR1## wherein (A-CO-- is a residue of a saturated straight or branched chain fatty acid, B is a nitrogen-containing group, Q is a substituent of the fatty acid, Z and Z' each is H or OH with the proviso that both of Z and Z' are not OH, and n is zero or an integer of at least 1, as well as physiologically acceptable salts thereof. These nucleoside derivatives are prepared by introducing the nitrogen-containing acyl group directly in one step or indirectly in two steps into the 5'-position of 5-fluorouridine, 2'-deoxy-5-fluorouridine or 1-.beta.-D-arabinofuranosyl-5-fluorouracil and splitting off any protective group and optionally converting the free compound into a physiologically acceptable salt thereof or vice versa.

Abstract: .alpha.-Cyanoamine compounds represented by the following formula or an acid addition salt thereof ##STR1## WHEREIN R.sub.1 is a halogen atom or lower alkoxy group, R.sub.2 and R.sub.3 are a hydrogen atom or lower alkoxy group, R.sub.4 is a hydrogen atom or lower alkyl group, R.sub. 5 is a hydrogen atom, --COOR.sub.6 (R.sub.6 is lower alkyl group), ##STR2## (R.sub.7 is lower alkoxy group, m is a numeral 0-3), --R.sub.8 --COOR.sub.9 (R.sub.8 is lower alkylene group, R.sub.9 is lower alkyl group), ##STR3## (R.sub.10 and R.sub.11 are a hydrogen atom or lower alkyl group, or R.sub.10 and R.sub.11 jointly form alkylene group), or ##STR4## (R.sub.1 to R.sub.4 are the same as defined above) and n is a numeral 2 or 3; but it is excluded when R.sub.5 is hydrogen atom or --COOR.sub.6 (R.sub.

Abstract: .alpha.-Cyanoamine compounds represented by the following formula or an acid addition salt thereof ##SPC1##Wherein R.sub.1 is a halogen atom or lower alkoxy group, R.sub.2 and R.sub.3 are a hydrogen atom or lower alkoxy group, R.sub.4 is a hydrogen atom or lower alkyl group, R.sub.5 is a hydrogen atom, -COOR.sub.6 (R.sub.6 is lower alkyl group), ##SPC2##(R.sub.7 is lower alkoxy group, m is a numeral 0-3), --R.sub.8 --COOR.sub.9 (R.sub.8 is lower alkylene group, R.sub.9 is lower alkyl group), ##EQU1## (R.sub.10 and R.sub.11 are a hydrogen atom or lower alkyl group, or R.sub.10 and R.sub.11 jointly form alkylene group), or ##SPC3##(R.sub.1 to R.sub.4 are the same as defined above) and n is a numeral 2 or 3; but it is excluded when R.sub.5 is hydrogen atom or --COOR.sub.6 (R.sub.