# US 10,865,176 B2 · Small molecule modulators of microRNA-34a

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- Number: US 10,865,176 B2
- Document ID: US10865176B2
- Status: Granted
- Kind: B2
- Application number: 14/109,301
- Filed: 2013-12-17
- Published: 2014-06-26
- Granted: 2020-12-15
- Earliest claimed: 2012-12-21
- Assignees: The Chinese University of Hong Kong
- Applicants: The Chinese University of Hong Kong
- Inventors: Yangchao Chen
- Web page: https://patentgrep.com/patent/US10865176B2

## CPC

- C07C 49/84: containing ether groups, [IMAGE cpc-sch-C07C-0958.gif] groups,[IMAGE cpc-sch-C07C-0959.gif] groups, or[IMAGE cpc-sch-C07C-0960.gif] groups
- A61K 31/12: Ketones
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- 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)

## Abstract

The present invention provides methods for identifying compounds that act as miR-34a modulators. The present invention also provides miR-34a modulators and compositions containing the modulators. The present invention further provides methods for treating diseases by administration of miR-34a modulators.

## Claims

### Claim 1

A method of inhibiting human cancer cell proliferation comprising contacting a human cancer cell with an effective amount of:
wherein R1-R5 is CH3, and R6 is H, and
wherein the effective amount is an amount effective to increase miRNA-34a expression in the human cancer cell and wherein p53 gene in the human cancer cell is wild-type or mutated but not deleted.

### Claim 2 (depends on 1)

The method of claim 1, wherein the human cancer cell is present in a human patient.

### Claim 3 (depends on 2)

The method of claim 2, wherein the contacting step comprises subcutaneous, intramuscular, intravenous, intraperitoneal, or oral administration.

### Claim 4 (depends on 3)

The method of claim 3, wherein the method further comprises administering an anti-anemia compound, an anti-nausea compound, an anti-inflammatory, an immunomodulator, or a chemotherapeutic.

### Claim 5 (depends on 1)

The method of claim 1, wherein the miRNA-34a expression is increased at least 3-fold in comparison to miRNA-34a expression level in a mammalian cell that has not been contacted.

### Claim 6 (depends on 1)

The method of claim 1, wherein the method further comprises detecting activation of miRNA-34a expression with a polynucleotide encoding a reporter gene.

### Claim 7 (depends on 6)

The method of claim 6, wherein the polynucleotide encoding a reporter gene comprises a sequence encoding for a luciferase or a fluorescent protein.

### Claim 8 (depends on 1)

The method of claim 1, wherein the human cancer cell is a human breast cancer cell.

### Claim 9 (depends on 3)

The method of claim 3, wherein the human cancer cell is a human colorectal cancer cell.

### Claim 10 (depends on 1)

The method of claim 1, wherein the human cancer cell is a human liver cancer cell.

### Claim 11 (depends on 1)

The method of claim 1, wherein the human cancer cell is a human lung cancer cell.

### Claim 12 (depends on 1)

The method of claim 1, wherein the human cancer cell is a human prostate cancer cell.