C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/255
C07D 239/36 (2006.01) C07D 405/06 (2006.01)
Patent
CA 1160226
Abstract . Substituted pyrimidin-2-ones, the salts thereof, processes for their preparation, pharmaceutical compositions containing them and a method therefor Compounds of the general formula:- Image . I (wherein X represents a halogen atom or a trifluoromethy; group; Rl represents an optionally substituted C6-10 carbocyclic aromatic group; and R2 represents a hydrogen atom or a lower alkyl, C7-16 aralkyl or C6-10 aryl group or the group CORla, in which Rla is as defined for Rl, Rl and Rla being the same ordifferent) 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 whilst the abnormal cells are in a phase susceptible to attack and whilst 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 electxophilic 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.
381712
Phillipps Gordon H.
Williamson Christopher
Fetherstonhaugh & Co.
Glaxo Group Limited
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