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US 8,507,483 B2Granted
1H-pyrimidin-2-one derivatives, preparation thereof and pharmaceutical use thereof as inhibitors of AKT (PKB) phosphorylation
AssigneeSanofi
InventorsVictor Certal, Bruno Filoche-Rommé, Frank Halley, Karl Andreas Karlsson, Fabienne Thompson
Life of this patent
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Abstract
The invention relates to the novel products of formula (I): in which Z represents —O—, —NH or Nalk; n represents 0 to 4; R1 represents Hal, hydroxyl, alkyl or alkoxy; the alkyl and alkoxy radicals being optionally substituted; R2 and R3 represent H, Hal or alkyl optionally substituted with one or more halogen atoms; R4 represents H; these products being in all the isomer forms and the salts, as medicaments, in particular as inhibitors of AKT(PKB) phosphorylation.
Claims14
A compound of formula (I):
- in which:
- Z represents —O—, —NH, or Nalk;
- n represents an integer from 0 to 4;
- R1 represents a halogen atom or a hydroxyl, alkyl or alkoxy radical;
- the alkyl and alkoxy radicals being optionally substituted with an NRxRy group
- R2 and R3, which may be identical or different, represent a hydrogen atom, a halogen atom, or an alkyl radical optionally substituted with one or more halogen atoms;
- R4 represents a hydrogen atom;
- NRxRy being such that Rx represents a hydrogen atom or an alkyl radical and Ry represents a hydrogen atom or an alkyl radical;
- or Rx and Ry form, with the nitrogen atom to which they are attached, a cyclic radical containing from 3 to 10 ring members and optionally one or more other heteroatoms chosen from O, S, NH and N-alkyl, this cyclic radical being optionally substituted with one or more radicals, which may be identical or different, chosen from halogen atoms and alkyl, hydroxyl, oxo, alkoxy, NH2, NHalk and N(alk)2 radicals;
- all the above alkyl (alk) and alkoxy radicals being linear or branched and containing from 1 to 6 carbon atoms,
- said compound of formula (I) being in all the possible racemic, enantiomeric and diastereoisomeric isomer forms, and also the addition salts with inorganic and organic acids or with inorganic and organic bases, of said compound of formula (I).
8 more elements
Dependencies are inferred from the claim text.