Adamantyl substituted oxindoles as pharmaceuticals agents

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 401/14 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) C07D 401/06 (2006.01) C07D 403/06 (2006.01) C07D 403/14 (2006.01)

Patent

CA 2206104

This invention relates to a novel compound of the formula Image IA or Image IB or pharmaceutically acceptable salts thereof, wherein preferred values are as follows: R1 is hydrogen, R2 is pyridin-4-ylmethyl, R3 is 4-pyridyl, R4 is 1- or 2-adamantyl, E1 and E2 are selected, independently, from hydrogen, halo, (C1-C3)alkyl, hydroxy, (C1-C3)alkoxy, nitro, trifluoromethyl, cyano, amino, (C1-C3)alkylamino and di[(C1-C3)alkyl]amino, and Het' and Het" are selected, independently, from 6 membered heterocyclic rings containing from one to four nitrogen atoms as part of the ring. The invention also relates to a pharmaceutical composition for treating cancer, which composition comprises a compound as described above, or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable carrier.

La présente invention concerne un nouveau composé de formule Image IA ou Image IB ou des sels pharmaceutiquement acceptables de ce dernier, dont les caractéristiques préférées sont les suivantes : R1 est un atome d'hydrogène, R2 correspond à un groupe pyridin-4-ylméthyle, R3 correspond à groupe 4-pyridyle, R4 correspond à un groupe 1- ou 2-adamantyle, E1 et E2 sont choisis, indépendamment, parmi l'hydrogène, un halogène, un alkyle en C1-C3, un hydroxy, un alcoxy en C1-C3, un nitro, un trifluorométhyle, un cyano, un amino, alkylamino en C1-C3 et un di[alkyle en C1-C3]amino, et Het' et Het" sont choisis, indépendamment, parmi des noyaux hétérocycliques à 6 atomes contenant de un à quatre atomes d'azote. L'invention concerne également une composition pharmaceutique pour traiter le cancer, laquelle composition comprend un composé décrit ci-dessus ou un sel pharmaceutiquement acceptable de ce dernier, combiné à un transporteur pharmaceutiquement acceptable.

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