Phthalazinone derivatives as inhibitors of parp-1

Details Phthalazinone derivatives as inhibitors of parp-1 Phthalazinone derivatives as inhibitors of parp-1

C - Chemistry, Metallurgy

07

D

C07D 237/32 (2006.01) A61K 31/502 (2006.01) A61P 35/00 (2006.01) C07D 401/10 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2691459

A compound of the formula (I): wherein: R represents one or more optional substituents on the fused cyclohexene ring; X can be NR X or CR X R Y; if X= NR X then n is 1 or 2 and if X= CR X R Y then n is 1; if X= NR X, then R X is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted ester, optionally substituted acyl, and optionally substituted sulfonyl groups; if X = CR X R Y then R X is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted sulfonamino, optionally substituted ether, optionally substituted ester, optionally substituted acyl, optionally substituted acylamido, and optionally substituted sulfonyl groups and R.gamma. is selected from H, hydroxy, optionally substituted amino, or R x and R.gamma. may together form an optionally substituted spiro- C3-7 cycloalkyl or heterocyclyl group; R C1 and R C2 are both hydrogen, or when X is CR X R Y, R C1, R C2, R x and R y, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo. The compounds act as inhibitors of poly(APD-ribose)synthase, PARP-1.

L'invention concerne un composé représenté par la formule (I): dans laquelle: R représente un ou plusieurs substituants facultatifs sur le noyau cyclohexène fusionné ; Y peut être NRX ou CRXRY ; si X = NRX, alors n vaut 1 ou 2 et si X = CRXRY, alors n vaut 1 ; si X = NRX, alors RX est choisi dans le groupe constitué par H, alkyle en C1-20 facultativement substitué, aryle en C5-20 facultativement substitué, hétérocyclyle en C3-20 facultativement substitué, amido facultativement substitué, thioamido facultativement substitué, ester facultativement substitué, acyle facultativement substitué et les groupes sulfonyle facultativement substitués ; si X = CRXRY, alors Rx est choisi dans le groupe constitué par H, alkyle en C1-20 facultativement substitué, aryle en C5-20 facultativement substitué, hétérocyclyle en C3-20 facultativement substitué, amido facultativement substitué, thioamido facultativement substitué, sulfonamino facultativement substitué, éther facultativement substitué, ester facultativement substitué, acyle facultativement substitué, acylamido facultativement substitué, et des groupes sulfonyle facultativement substitués, et R? est choisi parmi H, hydroxy, amino facultativement substitué, ou Rx et R? peuvent former ensemble un groupe spiro-cycloalkyle en C3-7 ou hétérocylyle facultativement substitué ; RC1 et RC2 sont tous deux hydrogène, ou lorsque X est CRXRY, RC1, RC2, Rx et Ry, conjointement avec les atomes de carbone auxquels ils sont attachés, peuvent former un noyau aromatique fusionné facultativement substitué ; et R1 est choisi parmi H et halo. Les composés agissent en tant qu'inhibiteurs de la poly(APD-ribose)synthase, PARP-1.

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