# US 8,569,309 B2 · 4′-demethylepipodophyllotoxin derivative, preparation method and use thereof

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- Number: US 8,569,309 B2
- Document ID: US8569309B2
- Status: Granted
- Kind: B2
- Application number: 13/641,114
- Filed: 2011-04-22
- Published: 2013-02-14
- Granted: 2013-10-29
- Earliest claimed: 2010-04-23
- Assignees: Hubei University of Technology
- Applicants: YaJie Tang
- Inventors: YaJie Tang
- Web page: https://patentgrep.com/patent/US8569309B2

## CPC

- C07D 405/14: containing three or more hetero rings
- A61K 31/365: Lactones
- A61K 31/497: containing further heterocyclic rings
- A61P 35/00: Antineoplastic agents
- C07D 493/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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 4′-demethylepipodophyllotoxin derivative of formula(III) having anti-tumor activity is provided. After the activation of hydroxyl in position C4 of 4′-demethylepipodophyllotoxin, tetramethylpyrazine is introduced by transamination to obtain the 4′-demethylepipodophyllotoxin derivative which is preferably used to inhibit gastric cancer line BGC-823.

## Claims

### Claim 1

A compound with the structure shown in Formula (III) or its salts:

### Claim 2 (depends on 1)

Said compound of claim 1 or its salts, wherein said salts comprise hydrochloride or phosphate.

### Claim 3 (depends on 1)

A composition comprising effective amounts of said compound or its salts of claim 1 and pharmaceutically accepted carriers.

### Claim 4 (depends on 3)

Said composition of claim 3, wherein said salts comprise hydrochloride or phosphates.