# US 6,720,331 B2 · 1-substituted 1,2,3,4-tetrahydro-β-carboline and 3,4-dihydro-β-carboline and analogs as antitumor agents

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- Number: US 6,720,331 B2
- Document ID: US6720331B2
- Status: Granted
- Kind: B2
- Application number: 10/115,312
- Filed: 2002-04-03
- Published: 2003-02-27
- Granted: 2004-04-13
- Earliest claimed: 2001-04-03
- Assignees: National Sun Yat-Sen University; National Yang-Ming University
- Inventors: Sheau Farn Yeh; Ya-Ching Shen
- Web page: https://patentgrep.com/patent/US6720331B2

## CPC

- C07D 471/04: Ortho-condensed systems
- A61P 35/00: Antineoplastic agents
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A composition includes a substituted dihydro- or tetrahydro-β-carboline of formula (II) or (III), wherein the aromatic ring of the carboline may include one or more substituents selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and the C-1 position of the carboline may include a substitutent selected from the group consisting of a carbocyclic group and a heterocyclic group. The composition may include a salt or a prodrug of the substituted dihydro- or tetrahydro-β-carboline. The composition may further includes a pharmaceutically acceptable carrier, diluent, or excipient.

## Claims

### Claim 1

A method for inhibiting cancer cell proliferation, comprising administering an effective amount of a compound according to formula (II) or (III) to a subject in need thereof,
wherein Y is a substituent selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and n is 0, 1, 2, 3, or 4, and R is
and wherein the cancer cell is one selected from breast cancer cell, colon cancer cell, leukaemia cancer cell, liver cancer cell, lung cancer cell, lymphoma, and prostate cancer cell.

### Claim 2 (depends on 1)

The method of claim 1, wherein the compound is in a composition comprising at least one selected from the group consisting of a pharmaceutically acceptable carrier, a pharmaceutically acceptable diluent, and a pharmaceutically acceptable excipient.

### Claim 3

A composition comprising a compound according to formula (II) or(III), or a salt or a prodrug thereof,
wherein Y is a substituent selected from the group consisting of hydroxy, C1-6 alkoxy, benzyloxy, C1-6 acyloxy, amino, C1-6 alkyl, C1-6 dialkylamino, halogen, and carboxy, and n is 0, and R is

### Claim 4 (depends on 3)

The composition of claim 3, further comprising at least one selected from the group consisting of a pharmaceutically acceptable carrier, a pharmaceutically acceptable diluent, and a pharmaceutically acceptable excipient.

### Claim 5 (depends on 3)

The composition of claim 3, wherein the compound is in a form of the salt or the prodrug.

### Claim 6 (depends on 5)

The composition of claim 5, further comprising at least one selected from the group consisting of a pharmaceutically acceptable carrier, a pharmaceutically acceptable diluent, and a pharmaceutically acceptable excipient.