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US 2008/0287461 A1Published application
Pyridinone Derivatives Against Malaria
AssigneeGlaxo Group Limited
InventorsJose Maria Fiandor Roman, Jose Maria Bueno Calderon, Araceli Mallo Rubio
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Abstract
4-pyridone derivatives of Formula (1) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
Claims17
A compound represented by the following Formula I:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- Het represents a 6-membered monocyclic heteroaromatic ring containing at least one nitrogen atom, wherein Het is substituted through a carbon atom with one group Z, wherein Z represents:
- i) a phenyl or methylenedioxyphenyl group, either of which is optionally substituted with one or more RX groups;
- ii) a —OC1-6alkylphenyl group, wherein the phenyl portion is optionally substituted with one or more RX groups;
- iii) a C1-10alkyl, a-Oaryl, a-C1-6alkylaryl, a-C2-6alkenylaryl or a-C2-6alkynylaryl group, wherein any aryl portion is optionally substituted with one or more RX group;
- RX represents halogen, cyano, —NRARA, C1-6alkyl, C1-6alkoxy or C1-6alkylS(O)m—;
- m represents 0-2;
- R1 represents halogen, hydrogen, or cyano;
- R2 represents hydrogen, hydroxy, —C(O)RY, —C(O)OH or C1-6alkyl optionally substituted by halogen, hydroxy, —C(O)OH, —C(O)RY or —NRARB;
- RA and RB independently represent hydrogen or C1-6alkyl;
- RY represents C1-6alkoxy or C1-6alkyl;
- and
- R3 and R4 are independently C1-6alkyl.
11 more elements
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Dependencies are inferred from the claim text.