Pharmacophore for trail induction
AssigneeThe Scripps Research Institute
InventorsKim D. Janda, Nicholas T. Jacob, Jonathan W. Lockner
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Abstract
There are disclosed imidazolinopyrimidinone compounds that have activity to induce TRAIL gene expression in macrophages. There is further disclosed a method for treating various cancers comprising administering effective amounts of an imidazolinopyrimidinone having the structure of Formula I herein. The invention is directed, in various embodiments, to a compound and pharmaceutical composition comprising an effective amount of a compound capable of inducing expression of TRAIL gene in cells capable of expressing the TRAIL gene to produce the cytokine TRAIL.
Claims6
A compound of formula (IA)
- wherein
- Ar1 and Ar2 are each independently aryl groups which are substituted with 0, 1, or 2 J groups;
- R is independently H or (C1-C6)alkyl;
- J is independently (C1-C6)alkyl, (C3-C9)cycloalkyl, (C3-C9)cycloalkyl(C1-C6)alkyl, halo, or (C1-C6)haloalkyl;
- or a pharmaceutically acceptable salt thereof.
A method for treating cancer, comprising administering an effective amount of a compound of formula (IA)
- wherein
- Ar1 and Ar2 are each independently aryl groups which are substituted with 0, 1, or 2 J groups;
- R is independently H or (C1-C6)alkyl;
- J is independently (C1-C6)alkyl, (C3-C9)cycloalkyl, (C3-C9)cycloalkyl(C1-C6)alkyl, halo, or (C1-C6)haloalkyl;
- or a pharmaceutically acceptable salt thereof,
- wherein the cancer is selected from the group consisting of monocytic leukemias, B-cell derived leukemias, T-cell derived leukemias, and combinations thereof.
Dependencies are inferred from the claim text.