Phthalazinone derivatives

Details Phthalazinone derivatives Phthalazinone derivatives

C - Chemistry, Metallurgy

07

D

C07D 237/32 (2006.01) A61K 31/50 (2006.01) A61K 31/502 (2006.01) A61P 31/20 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2423279

The use of a compound of the formula: (see above formula) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; R C is represented by -L-R L, where L is of formula: -(CH2)n1-Q n2-(CH2)n3- wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH or C(=O) ; and R L is an optionally substituted C5-20 aryl group; and R N is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, and C5-20 aryl, hydroxy, ether, nitro, amino, amido, thiol, thioether, sulfoxide and sulfone. Novel compounds, and their use as pharmaceuticals, are also disclosed.

L'invention concerne l'utilisation d'un composé de la formule (I) ainsi que l'utilisation d'isomères, de sels, de solvants, de formes chimiquement protégées et de promédicaments de celui-ci, dans la préparation d'un médicament destiné à inhiber l'activité de la PARP, dans laquelle, A et B de la formule (I) représentent un cycle aromatique fusionné et facultativement substitué ; R¿c ?est représenté par - L-R¿l?, L ayant la formule : (CH¿2?)¿n1?-Q¿n2?- (CH¿2?)¿n3? dans laquelle n¿1, ?n¿2 ?et n¿3 ?sont chacun choisis parmi 0, 1, 2 et 3 et la somme de n¿1, ?n¿2 ?et n¿3 ?fait 1, 2 ou 3 ; Q est choisi parmi O, S, NH, ou C (=O) et R¿l ?peut, le cas échéant, être un groupe aryle C¿5-20 ?facultativement substitué; R¿n? est choisi parmi hydrogène, alkyle C¿1-7? facultativement substitué, hétérocyclyle C¿3-20?, aryle C¿5-20?, hydroxy, éther, nitro, amino, amido, thiol, thioéther, sulfoxyde et sulfone. L'invention porte également sur de nouveaux composés ainsi que sur leur utilisation en tant que produits pharmaceutiques.

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