Use of Chk2 kinase inhibitors for cancer treatment
AssigneeThe United States of America, as represented by the Secretary, Department of Health and Human Services
InventorsYves Pommier, Robert H. Shoemaker, Dominic Scudiero, Michael Currens, John Cardellina, Andrew Jobson
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Abstract
Described herein are Chk2-inhibitor compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof.
Claims20
A method of down regulating Chk2 phosphorylation in a subject, comprising:
- (a) identifying the subject as suffering from lung cancer, breast cancer, bladder cancer, or melanoma;
- and
- (b) administering to the subject an amount of one or more compounds of the following Formulae (I) or (II) sufficient to down regulate Chk2 phosphorylation:
- wherein each R1 and R2 is independently:
- each R3 is independently alkyl;
- and
- each R is independently H or alkyl;
- or
- a compound of Formula (II):
- wherein each R1 and R2 is independently:
- each R3 is independently alkyl;
- and
- each R is independently H or alkyl.
A method of protecting non-cancerous tissue in a subject suffering from lung cancer, breast cancer, bladder cancer, or melanoma, comprising:
- (a) identifying the subject as having lung cancer, breast cancer, bladder cancer, or melanoma;
- and
- (b) administering to the subject one or more compounds of the following Formulae (I) or
- wherein each R1 and R2 is independently:
- each R3 is independently alkyl;
- and
- each R is independently H or alkyl;
- or
- a compound of Formula (II):
- wherein each R1 and R2 is independently:
- each R3 is independently alkyl;
- and
- each R is independently H or alkyl;
- and,
- (c) administering ionizing radiation to the subject.
A method of inhibiting a substrate selected from p53, E2F1, and PML in a normal cell in a subject, comprising:
- (a) identifying the subject of such treatment as suffering from lung cancer, breast cancer, bladder cancer, or melanoma;
- and
- (b) administering to the subject an amount one or more compounds of the following Formulae (I) or (II) sufficient to inhibit p53, E2F1, or PML in the cell:
- wherein each R1 and R2 is independently:
- each R3 is independently alkyl;
- and
- each R is independently H or alkyl;
- or
- a compound of Formula (II) sufficient to down regulate Chk2 phosphorylation:
- wherein each R1 and R2 is independently:
- each R3 is independently alkyl;
- and
- each R is independently H or alkyl.
Dependencies are inferred from the claim text.