# US 2014/0194468 A1 · Compounds that Suppress Cancer Cells and Exhibit Antitumor Activity

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- Number: US 2014/0194468 A1
- Document ID: US20140194468A1
- Status: Published application
- Kind: A1
- Application number: 14/076,247
- Filed: 2013-11-10
- Published: 2014-07-10
- Earliest claimed: 2009-04-06
- Assignees: The Governing Council of the University of Toronto; University of Central Florida Research Foundation, Inc.
- Applicants: The Governing Council of the University of Toronto; University of Central Florida Research Foundation, Inc.
- Inventors: James Turkson; Patrick Gunning
- Web page: https://patentgrep.com/patent/US20140194468A1

## CPC

- A61K 31/451: having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
- A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
- A61P 35/00: Antineoplastic agents
- C07C 311/19: to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
- C07D 211/26: with hydrocarbon radicals, substituted by nitrogen atoms
- C07C 2601/14: The ring being saturated
- 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
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.

## Claims

### Claim at position 1

-22. (canceled)

### Claim 23

A method effective to inhibit a cancer cell, comprising the step of contacting the cell with a compound and salts thereof according to Formula 1 or Formula 2:
thereby inhibiting the cancer cell.

### Claim 24 (depends on 23)

The method of claim 23, wherein the compound and salts thereof is according to Formula 1.

### Claim 25 (depends on 23)

The method of claim 23, wherein the compound and salts thereof is according to Formula 2.

### Claim 26 (depends on 23)

The method of claim 23, wherein the cancer cell is a human pancreatic cancer cell.

### Claim 27 (depends on 23)

The method of claim 23, wherein the cancer cell is a human breast cancer cell.

### Claim 28 (depends on 23)

The method of claim 23, wherein the cancer cell is characterized by an aberrant level of Stat3.

### Claim 29

A method effective to inhibit Stat3 activity in a cell, comprising the step of contacting the cell with a compound and salts thereof according to Formula 1 or Formula 2:
thereby inhibiting Stat3 in the cell.

### Claim 30 (depends on 29)

The method of claim 29, wherein the compound and salts thereof is according to Formula 1.

### Claim 31 (depends on 29)

The method of claim 29, wherein the compound and salts thereof is according to Formula 2.

### Claim 32 (depends on 29)

The method of claim 29, wherein the cell is a cancer cell.

### Claim 33 (depends on 32)

The method of claim 32, wherein the cancer cell is a human pancreatic cancer cell.

### Claim 34 (depends on 32)

The method of claim 32, wherein the cancer cell is a human breast cancer cell.

### Claim 35 (depends on 29)

The method of claim 29, wherein the Stat3 is constitutively active.

### Claim 36

A method effective to down-regulate the expression of Stat3-regulated genes in a cell, comprising the step of contacting the cell with a compound and salts thereof according to Formula 1 or Formula 2:
thereby down-regulating Stat3-regulated genes in the cell.

### Claim 37 (depends on 36)

The method of claim 36, wherein the compound and salts thereof is according to Formula 1.

### Claim 38 (depends on 36)

The method of claim 36, wherein the compound and salts thereof is according to Formula 2.

### Claim 39 (depends on 36)

The method of claim 36, wherein the cell is a cancer cell.

### Claim 40 (depends on 39)

The method of claim 39, wherein the cancer cell is a human pancreatic cancer cell.

### Claim 41 (depends on 39)

The method of claim 39, wherein the cancer cell is a human breast cancer cell.

### Claim 42 (depends on 36)

The method of claim 36, wherein the Stat3-regulated genes comprise c-Myc, Bcl.xL, matrix metalloproteinase 9, VEGF, or combinations thereof.