Anti-helicobacter acyl derivatives of azolones

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 249/12 (2006.01) A61K 31/495 (2006.01) C07D 233/70 (2006.01) C07D 401/00 (2006.01) C07D 401/04 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/00 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2193490

The invention is concerned with the compounds having formula (I), the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y is CH or N; R1, R2 and R3 each independently are hydrogen or C1-4alkyl; R4 and R5 each independently are hydrogen, halo, C1- 4alkyl, C1-4alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R6 is hydrogen; or R6 is phenyl optionally substituted with halo; pyridinyl; furanyl; thienyl; 3-chlorobenzo[b]thien-2-yl; trifluoromethyl; C1-4alkyloxycarbonyl; dihalophenylcyclopropanyl; C3- 6cycloalkyl; adamantyl; C2-6alkenyl optionally substituted with halophenyl; or C1-4alkyl optionally substituted with halo, phenyl, halophenyl, dihalophenyl, phenyloxy, piperidinyl, pyrrolidinyl, piperazinyl, C1-4alkylpiperazinyl, C1- 4alkyl-carbonylpiperazinyl, C1-4alkyloxycarbonylpiperazinyl, phthalimino, amino, mono- or di(C1-20)alkylamino or C3-6cycloalkylamino; Z is C=O or CHOH; and (1) is a radical of formula (a-1), (a-2), (a-3), (a-4), (a-5), (a-6), or (a-7). Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.

L'invention concerne des composés de formule (I), leurs sels d'addition pharmaceutiquement acceptables et leurs formes stéréochimiquement isomériques. Dans cette formule, Y est CH ou N; R?1¿, R?2¿ et R?3¿ sont chacun indépendamment hydrogène ou alkyle C¿1-4?;R?4¿ et R?5¿ sont chacun indépendamment hydrogène, halo, alkyle C¿1-4?, alkyloxy C¿1-4?, hydroxy, trifluorométhyle, trifluorométhyloxy, ou difluorométhyloxy; R?6¿ est hydrogène; ou bien R?6¿ est phényle éventuellement substitué avec halo; pyridinyle; furanyle; thienyle; 3-chloro-benzo[b]thien-2-yl; trifluorométhyle; alkoxycarbonyle C¿1-4?; dihalophénylcyclopropanyle; cycloalkyle C¿3-6?; adamantyle; alcényle C¿2-6? éventuellement substitué avec halophényle; ou bien alkyle C¿1-4? éventuellement substitué avec halo, phényle, halophényle, dihalophényle, phényloxy, pipéridinyle, pyrrolidinyle, pipérazinyle, alkylpipérazinyle C¿1-4?, alkylcarbonylpiperazinyle C¿1-4?, phtalimino, amino, mono- ou di(C¿1-20?)alkylamino ou cycloalkylamino C¿3-6?; Z est C=O ou CHOH; et (1) est un radical de formule (a-1), (a-2), (a-3), (a-4), (a-5), (a-6), ou bien (a-7). L'invention concerne également des compositions comprenant lesdits composés, des procédés pour les préparer et l'utilisation de ces composés comme médicament.

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