C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 413/00 (2006.01)
Patent
CA 2570183
This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R6)-, -S-, -S(O)-, or -S(O2)-; R1 is selected from the group consisting of aryl and heteroaryl; R2 is selected from the group consisting of alkyl, -C(O)-Y, -X-C(O)-Y, -alkylene-X-C(O)-Y, -alkylene-C(O)-Y, -alkylene-cycloalkylene-X-C(O)-Y, -alkylene-cycloalkylene-C(O)-Y, - cycloalkylene-alkylene-X-C(O)-Y, -cycloalkylene-alkylene-C(O)-Y, - cycloalkylene-X-C(O)-Y, -cycloalkylene-C(O)-Y, -alkylene-cycloalkylene- alkylene-X-C(O)-Y, -alkylene-cycloalkylene-alkylene-C(O)-Y, aryl, and heteroaryl; R3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R4 and R5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR8R9, -N(R6)-(CH2)b-NR8R9, aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of Formula II and Formula III: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
L'invention concerne des inhibiteurs de gamma secrétase de formule I: L est -O-, -N(R6)-, -S-, -S(O)-, or -S(O2)-; R1 appartient au groupe qui comprend aryle et hétéroaryle; R2 appartient au groupe qui comprend alkyle, -C(O)-Y, -X-C(O)-Y, -alkylène-X-C(O)-Y, -alkylène-C(O)-Y, -alkylène-cycloalkylène-X-C(O)-Y, -alkylène-cycloalkylène-C(O)-Y, -cycloalkylène-alkylène-X-C(O)-Y, -cycloalkylène-alkylène-C(O)-Y, -cycloalkylène-X-C(O)-Y, -cycloalkylène-C(O)-Y, -alkylène-cycloalkylène-alkylène-X-C(O)-Y, -alkylène-cycloalkylène-alkylène-C(O)-Y, aryle, et hétéroaryle; R3 appartient au groupe qui comprend aryle, hétéroaryle, alkyle, cycloalkyle, arylalkyle, arylcycloalkyle, hétéroarylalkyle, hétéroarylcycloalkyle, arylhétérocycloalkyle, et alcoxyalkyle; chaque R4 et R5 est pris indépendamment dans le groupe qui comprend H et alkyle; et Y appartient au groupe qui comprend -NR8R9, -N(R6)-(CH2)b-NR8R9, aryle, hétéroaryle, alkyle, cycloalkyle, arylalkyle, arylcycloalkyle, hétéroarylalkyle, hétéroarylcycloalkyle, et arylhétérocycloalkyle; ou Y appartient au groupe qui comprend les formules II et III. Un ou plusieurs composés de formule I, ou des formulations comprenant de tels composés, peuvent être utiles, par exemple pour traiter la maladie d'Alzheimer.
Bara Thomas A.
Clader John W.
Josien Hubert B.
Li Hongmei
Pissarnitski Dmitri
Norton Rose Canada S.e.n.c.r.l.,s.r.l./llp
Schering Corporation
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