Substituted pyrimidin-2-ones, the salts thereof, pharmaceutical compositions containing them and a method therefor
US4650800A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 19, 1983 |
| Grant date | Mar 17, 1987 |
| Priority date | — |
| Expiry date | May 19, 2003 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D413/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Compounds of the general formula: ##STR1## wherein X represents a halogen atom or a trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group and Het represents an optionally substituted C-attached 5-7 membered aromatic heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused ring 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.