Substituted pyrimidin-2-ones, the salts thereof, processes for t

Details Substituted pyrimidin-2-ones, the salts thereof, processes for t Substituted pyrimidin-2-ones, the salts thereof, processes for t

1983-05-27

1987-01-13

Hollrah, Glennon H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544316, 544318, A61K 31505, C07D23936

Patent

active

046365095

ABSTRACT:
Compounds of the general formula: ##STR1## (wherein X represents a halogen atom or a trifluoromethyl group; R.sup.1 represents an optionally substituted C.sub.6-10 carbocyclic aromatic group; and R.sup.2 represents a hydrogen atom or a lower alkyl, C.sub.7-16 aralkyl or C.sub.6-10 aryl group or the group COR.sup.1a, in which R.sup.1a is as defined for R.sup.1, R.sup.1 and R.sup.1a being the same or different) and where an acidic or basic group is present, the salts thereof have been found to possess excellent metaphase arresting ability and are of use in combating abnormal cell proliferation. Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cytotoxic drug to be administered while the abnormal cells are in a phase susceptible to attack and while the normal cells are in a non-susceptible phase.
The compounds of the invention are prepared by alkylation, deprotection of a protected keto group, oxidation or electrophilic halogenation.
Pharmaceutical compositions containing the compounds of formula I, and where appropriate, the physiologically compatible salts thereof; and methods for the use of the compounds are described and claimed.

REFERENCES:
patent: 4395406 (1983-06-01), Gacek et al.
patent: 4399140 (1983-08-01), Gacek et al.

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