PKC delta inhibitors for use as therapeutics
AssigneeFaller & Williams Technology, LLC
InventorsDouglas V. Faller, Robert M. Williams
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Abstract
The invention is directed to compounds that are specific inhibitors of PKC delta, and methods and compositions for the treatment and prevention of cancers and other disorders. Compositions comprising compounds of the invention are used to treat cancers such as, for example, carcinoid and neuroendocrine tumors, malignant melanomas, pancreatic, gastrointestinal and lung cancers. Neuroendocrine tumor cell lines of pulmonary and gastrointestinal origin are surprisingly sensitive to PKC delta inhibition by the compounds of the invention. The invention is further directed to methods, compositions and kits containing compounds of the formulas (Ia), (IIa), (IIIa), (IVa), and (V) as disclosed and described in FIGS. 11 and 12.
Claims10
A method comprising:
- assessing cells of a patient for aberrant PKC delta activity;
- determining a therapeutically effective amount that inhibits PKC delta activity of a pharmaceutical composition containing a compound of the formula:
- wherein:
- R1 is selected from the group consisting of H and a lower alkyl;
- R2 and R3 are each independently selected from the group consisting of H, OH and OR;
- A, B, C, D, W, X, Y, and Z are each independently selected from the group consisting of N and CH;
- G is selected from the group consisting of O, NR, S, and CH2,
- R is selected from the group consisting of H, a lower alkyl and aryl;
- and
- n is an integer selected from the group consisting of 1, 2, 3, and 4;
- and administering the therapeutically effective amount of the pharmaceutical composition to the cells of the patient.
Dependencies are inferred from the claim text.