Fenretinide derivatives and uses thereof as therapeutic, diagnostic and imaging agents
View Patent ↗Synthetic peptidomimetic derivatives and phenyl group derivatives of Fenretinide (4-HPR) are disclosed, as are their uses as therapeutic, diagnostic and imaging agents for cancer and other diseases.
1. A compound having the structure:
wherein R is OH;
wherein R 1 , R 2 and R 3 are independently H, Br, Cl, I, F, alkyl, aryl, OH, NO 2 , NHR 4 , OR 4 or heterocyclic, where R 4 is alkyl, aryl or heterocyclic;
or a pharmaceutically acceptable salt thereof.
2. The compound of claim 1 , wherein at least one of R 1 , R 2 and R 3 is OH, Br, Cl, I or F, and wherein at least one of R 1 , R 2 and R 3 is H.
3. The compound of claim 1 , wherein at least one of R 1 and R 3 is Br, Cl, I or F.
4. The compound of claim 1 , wherein R 2 is H or OH.
5. The compound of claim 1 , wherein R 3 is I.
6. The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt thereof.
7. The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt thereof.
8. The compound of claim 1 having the structure:
or a pharmaceutically acceptable salt thereof.
9. The compound of claim 1 , wherein the compound is radiolabeled.
10. The compound of claim 1 , wherein the compound further comprises a nanoparticle conjugated to position R, R 1 , R 2 or R 3 .
11. A pharmaceutical composition comprising the compound of claim 1 , and a pharmaceutically acceptable carrier or diluent.
12. A method of treating a subject having cancer comprising administering the compound of claim 1 to the subject in an amount and manner effective to treat cancer in the subject.
13. The method of claim 12 , wherein the cancer is breast cancer, a rhabdoid tumor, a neuroblastoma, ovarian cancer, renal cancer, a malignant glioma or prostrate cancer.
14. A method of treating a subject having a disease comprising administering the compound of claim 1 to the subject in an amount and manner effective to treat the disease, wherein the disease is diabetes, AIDS, Alzheimer's Disease, cystic fibrosis, allergic encephalomyelitis or ichthyosis.