# US 8,785,501 B2 · Anti-cancer tamoxifen-melatonin hybrid ligand

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- Number: US 8,785,501 B2
- Document ID: US8785501B2
- Status: Granted
- Kind: B2
- Application number: 13/497,954
- Filed: 2010-10-12
- Published: 2013-03-21
- Granted: 2014-07-22
- Earliest claimed: 2009-10-13
- Assignees: Duquesne University of the Holy Spirit
- Applicants: Paula A. Witt-Enderby; Vicki L. Davis; David Lapinsky
- Inventors: Paula A. Witt-Enderby; Vicki L. Davis; David Lapinsky
- Web page: https://patentgrep.com/patent/US8785501B2

## CPC

- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 31/4045: Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
- A61P 35/00: Antineoplastic agents
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A particularly constructed tamoxifen-melatonin hybrid ligand gives new and unexpectedly improved results in the prevention and treatment of cancer, particularly breast cancer. The hybrid ligand comprises either tamoxifen or 4-hydroxytamoxifen and also melatonin, with the tamoxifen or 4-hydroxytamoxifen and melatonin's being linked by an unsubstituted C2-C6 alkyl linker between the tamoxifen amine and the carbonyl of melatonin.

## Claims

### Claim 1

A pharmaceutically active agent consisting essentially of a hybrid ligand of tamoxifen and melatonin linked by a 2-6 carbon alkyl linker conjoining said tamoxifen and said melatonin via a covalent linkage between an amino moiety of said tamoxifen and a hydroxylamino moiety of said melatonin.

### Claim 2 (depends on 1)

The hybrid ligand according to claim 1 wherein said tamoxifen is a 4-hydroxytamoxifen moiety.

### Claim 3 (depends on 1)

The hybrid ligand according to claim 1 wherein said alkyl linker is substituted or unsubstituted and contains 5 carbon atoms.

### Claim 4

A pharmaceutical formulation consisting essentially of a hybrid ligand of tamoxifen and melatonin linked by a 2-6 carbon unsubstituted alkyl linker conjoining said tamoxifen and said melatonin via a covalent linkage of an amino moiety of said tamoxifen and a hydroxylamino moiety of said melatonin, and at least one pharmaceutically acceptable excipient.

### Claim 5 (depends on 4)

The pharmaceutical formulation according to claim 4 wherein said tamoxifen is 4-hydroxytamoxifen.