Heterocyclylalkyl piperidine derivatives, their preparation...

C - Chemistry – Metallurgy – 07 – D

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C07D 409/14 (2006.01) A61K 31/4709 (2006.01) A61P 31/04 (2006.01) C07D 401/06 (2006.01) C07D 401/14 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2429311

The invention concerns heterocyclylalkyl piperidine derivatives of general formula (I), wherein X1, X2, X3, X4 and X5 are >C-R'1 to >C-R'5 or one at most represents N; R2 is COOH, alkyloxycarbonyl, cycloalkyloxycarbonyl, CN, -CONRaRb or R2 is CH2OH, alkyl substituted or R2 is -CF2-Rc, -C(CH3)2-Rc, -CO-Rc, -CHOH-Rc, -C(cycloalkyl)-Rc or -CH=CH-Rc; R3 is phenyl, heterocyclyl. alk-R< DEG >3; Y represents >CH-Re or a difluoromethylene, carbonyl, hydroxyiminomethylene, alkyloxyiminomethylene, cycloalkyloxyiminomethylene radical, or a cycloalkylene-1,1 radical; and n = 0 to 4 provided that the radicals or phenyl or heterocyclyl portions mentioned above can optionally be substituted, in the enantiomeric or diastereoisomeric forms or mixtures thereof, and/or as the case may be in their syn or anti form or mixture thereof and their salts.

Dérivés hétérocyclylalcoyl pipéridine de formule générale (I) pour lesquels: X1, X2, X3, X4 et X5 sont >C-R'1 à >C-R'5 ou bien l'un au plus représente N, R2 est COOH, alcoyloxycarbonyle, cycloalcoyloxycarbonyle, CN, -CONRaRb ou R2 est CH2OH, alcoyle substitué ou R2 est -CF2-Rc, -C(CH3)2-Rc, -CO-Rc, -CHOH-Rc, -C(cycloalcoyle)-Rc ou -CH=CH-Rc, R3 est phényle, hétérocyclyle, alk-R~3, Y représente >CH-Re ou un radical difluorométhylène, carbonyle, hydroxyiminométhylène, alcoyloxyiminométhylène, cycloalcoyloxyiminométhylène, ou un radical cycloalcoylène-1,1, et n = 0 à 4 étant entendu que les radicaux ou portions phényle ou hétérocyclyle mentionnés ci-dessus peuvent être éventuellement substitués, sous leurs formes énantiomères ou diastéréoisomères ou les mélanges de ces formes, et/ou le cas échéant sous leur forme syn ou anti ou leur mélange ainsi que leurs sels.

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