C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 231/56 (2006.01) A61K 31/415 (2006.01) A61P 25/00 (2006.01) C07D 401/12 (2006.01)
Patent
CA 2358586
A class of 4-oxo-tetrahydroindazole-3-carboxamides is disclosed. The compounds bind selectively to GABAA .alpha.-5 receptors, and are useful in therapy where cognition enhancement is required, for example in the treatment of Alzheimer's disease. The compounds are represented by formula (I) wherein R1 and R4 are independently chosen from hydrogen, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C2-6 haloalkenyl and C2-6 haloalkynyl; R2 is hydrogen or C1-6 alkyl; and Ar is phenyl, a 5-membered heterocyclic group containing 1,2,3 or 4 heteroatoms chosen from N, O and S, no more than one of which is O or S, or a 6-membered heterocyclic group containing one or two nitrogen atoms, each of which groups Ar is unsubstituted or substituted by from one to three groups independently chosen from halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C1-6 alkoxy, C2-6 alkenyloxy, C2-6 alkynylnoxy, C3-7 cycloalkoxy, C1-6 haloalkyl, C2-6 haloalkenyl, C2-6 haloalkynyl, amino, C1-6 alkylamino, di(C1-6)alkylamino, hydroxy, hydroxy C1-6 alkyl, cyano, nitro, amino C1-6 alkyl, C1-6 alkylaminoC1-6 alkyl, di(C1-6 alkyl)aminoC1-6alkyl or C1-6alkoxycarbonylaminoC1-6alkyl.
La présente invention concerne une classe de 4-oxo-tétrahydroindazole-3-carboxamides. Ces composés, qui se lient sélectivement au récepteurs GABA¿A? .alpha.-5, conviennent particulièrement pour les thérapies demandant une meilleure cognition, notamment dans le cas de la maladie d'Alzheimer. Ces composés sont représentés par la formule générale (I). Dans cette formule, R?1¿ et R?4¿ appartiennent chacun en ce qui le concerne au groupe des hydrogène, halogène, C¿1-6? alkyle, C¿2-6? alcényle, C¿2-6? alkynyle, C¿1-6? haloalkyle, C¿2-6? haloalcényle et C¿2-6? haloalkynyle; R?2¿ est hydrogène ou C¿1-6? alkyle; et Ar est phényle, un groupe hétérocyclique à 5 segments contenant 1, 2, 3 ou 4 hétéroatomes choisis entre les N, O et S, où il ne doit y avoir qu'un seul O ou S, ou un a groupe hétérocyclique à 6 segments contenant un ou deux atomes d'azote, chaque groupe Ar étant non substitué ou substitué par un à trois groupes choisis indépendammenent parmi les halogène, C¿1-6? alkyle, C¿2-6? alcényle, C¿2-6? alkynyle, C¿3-7? cycloalkyle, C¿1-6? alcoxy, C¿2-6? alkényloxy, C¿2-6? alkynylnoxy, C¿3-7? cycloalcoxy, C¿1-6? haloalkyle, C¿2-6? haloalcényle, C¿2-6? haloalkynyle, amino, C¿1-6? alkylamino, di(C¿1-6?)alkylamino, hydroxy, hydroxy C¿1-6? alkyle, cyano, nitro, amino C¿1-6? alkyle, C¿1-6? alkylamino C¿1-6?alkyle, di(C¿1-6?alkyl)aminoC¿1-6?alkyle ou C¿1-6?alcoxycarbonylaminoC¿1-6?alkyle.
Bryant Helen Jane
Chambers Mark Stuart
Merck Sharp & Dohme Limited
Ogilvy Renault
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