Thienopyridone derivatives as amp-activated protein kinase (ampk) activators
AssigneeMerck Patent Gesellschaft
InventorsDaniel Cravo, Franck Lepifre, Sophie Hallakou-Bozec, Christine Charon
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Abstract
The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).
Claims15
A compound of the formula (I)
- in which:
- R1 denotes H, A, OA, OH, Hal, NO2, COOA, COOH, CHO, COA, CONH2, CONHA, CONA2, CN, SO2A, SO2NH2, Ar or Het,
- R2, R3 each, independently of one another, denote Ar or Het,
- Ar denotes phenyl, naphthyl, each of which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by A, Hal, OA, OH, CHO, COA, NH2, NHA, NA2, NO2, COOA, COOH, CONH2, CONA, CONA2, SO2A, CN, C(═NH)NH2, C(═NH)NHOH and/or Het,
- Het denotes a mono- or bicyclic unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be mono-, di- or trisubstituted by Hal, A, Ar′, OA, OH, CHO, COA, COOH, COOA, CN, NO2, NH2, NHA, NA2, CONH2, CONHA and/or CONA2,
- A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7H atoms may be replaced by OH, F, Cl and/or Br, or
- denotes cycloalkyl having 3-7 C atoms,
- Hal denotes F, Cl, Br or I,
- and pharmaceutically usable derivatives, salts, solvates and stereoisomers thereof, including mixtures thereof in all ratios,
- excluding compounds of the formula (I) where
- —R1=H ;
- R2=phenyl;
- R3=3-methoxyphenyl
- —R1=H ;
- R2=R3=phenyl
- —R1=H , R2=phenyl, R3=2-thiazoyl.
Medicaments comprising at least one compound of formula (I), and/or pharmaceutically usable salts and stereoisomers thereof, including mixtures thereof in all ratios, and optionally excipients and/or adjuvants.
Dependencies are inferred from the claim text.