Poly(ADP-Ribose) Polymerase 1 Inhibitors Structurally Unrelated to NAD
AssigneeInstitute for Cancer Research d/b/a The Research Institute of Fox Chase Cancer Center
InventorAlexei Tulin
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Abstract
Compounds that are not related to NAD, and which target PARP1-histone H4 interaction are provided, as well as compositions of these compounds, and methods for specific inhibition of poly(ADP-ribose) polymerase 1 (PARP-1) using these compounds are provided. These PARP-1 inhibitors may be used to treat cancer in which PARP-1 activation or biologic activity plays a role, including prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma, among others.
Claims32
A compound of Formula
- wherein:
- R1 is an alkyl or ether group;
- R2 is either CH3 or not present, wherein when R2 is CH3, the nitrogen atom is positively charged, and
- R3 is either
- wherein R4 includes one or more ring structures;
- provided that the compound is not
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A compound comprising
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A method for inhibiting the biologic activity of poly(ADP-ribose) polymerase 1 (PARP1), comprising contacting PARP1 with an amount of a compound effective to inhibit the biologic activity of PARP1, the compound comprising:
- wherein:
- R1 is an alkyl or ether group;
- R2 is either CH3 or not present, wherein when R2 is CH3, the nitrogen atom is positively charged, and
- R3 is either
- wherein R4 includes one or more ring structures.
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A method for inhibiting the biologic activity of poly(ADP-ribose) polymerase 1 (PARP1), comprising contacting PARP1 with an amount of a compound effective to inhibit the biologic activity of PARP1, the compound comprising:
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A method for treating a cancer patient, comprising administering to the patient in need thereof an effective amount of the compound of Formula
- wherein:
- R1 is an alkyl or ether group;
- R2 is either CH3 or not present, wherein when R2 is CH3, the nitrogen atom is positively charged, and
- R3 is either
- wherein R4 includes one or more ring structures, thereby treating the cancer in the patient.
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Dependencies are inferred from the claim text.