Parp modulators and treatment of cancer

Details Parp modulators and treatment of cancer Parp modulators and treatment of cancer

C - Chemistry, Metallurgy

07

D

C07D 295/00 (2006.01) C12P 13/00 (2006.01)

Patent

CA 2612979

The invention relates to a method of modulating poly(ADP-ribose)polymerase-l (PARP-I) activity in a mammal comprising administering to a mammal an effective amount of an organic aromatic compound having from 4 to about 35 carbon atoms, wherein said organic aromatic compound is capable of binding the arginine-34 moiety located in Zinc finger- 1 of the PARP-I enzyme and wherein said organic aromatic compound has electron donating capabilities such that it's .tau.r-electron system will interact with the positively charged (cationic) guanidinium moiety of the specific arginine-34 residue of the Zinc- 1 finger of PARP-I and does not contain benzamide or lactam substituents. In particular, substituted benzopyrones and substituted indoles and their pharmaceutical compositions containing such compounds that modulate the activity of PARP-I, are described. The invention is also directed to the composition of matter, kits and methods for their therapeutic and/or prophylactic use in treating diseases and disorders described herein, by administering effective amounts of such compounds. Preferably, the compositions and methods provided herein inhibit PARP activity.

L'invention concerne une méthode de modulation de l'activité de la poly(ADP-ribose)polymérase-l (PARP-I) chez un mammifère consistant à administrer à un mammifère une quantité efficace d'un composé aromatique organique présentant entre 4 et environ 35 atomes de carbone, ledit composé aromatique organique pouvant se lier à la fraction 34 de l'arginine située dans le doigt de zinc 1 de l'enzyme PARP-I et ledit composé aromatique organique présentant des capacités de donneur d'électrons de sorte que son système de .pi.-électrons interagit avec la fraction de guanidinium positivement chargée (cationique) du résidu 34 de l'arginine spécifique du doigt de zinc 1 de la PARP-I et ne contient pas de substituants benzamide ou lactame. L'invention concerne notamment des benzopyrones substituées et des indoles substituées ainsi que leurs compositions pharmaceutiques contenant lesdits composés qui modulent l'activité de la PARP-I. L'invention concerne également la composition de matière, des nécessaires et des méthodes d'utilisation thérapeutique et/ou prophylactique de ces derniers pour traiter des maladies et des troubles décrits dans l'invention, par administration de quantités efficaces desdits composés. De préférence, les compositions et méthodes de l'invention inhibent l'activité de la PARP.

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