The Scripps Research Institute

Jonathan W Lockner

Kim D Janda

Nicholas T Jacob

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.

Pharmacophore for trail induction

The invention provides chiral haptens (&#x2212;)-3'-AmNic and (&#x2212;)-N4N for use in generating antibodies in a patient specific for (&#x2212;)-nicotine. The haptens can be conjugated to suitable carrier proteins and administered as an antigenic mixture, optionally comprising adjuvant(s), to a patient suffering from nicotine or tobacco addiction or habituation.

Enantiopure haptens for nicotine vaccine development

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.

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San Diego, CA, United States of America

Jonathan W Lockner