# US 7,744,867 B2 · PTPase inhibitors and method of using same

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- Number: US 7,744,867 B2
- Document ID: US7744867B2
- Status: Granted
- Kind: B2
- Application number: 10/159,473
- Filed: 2002-05-31
- Published: 2003-05-15
- Granted: 2010-06-29
- Earliest claimed: 2001-05-31
- Assignees: The Cleveland Clinic Foundation
- Inventors: Taolin Yi
- Web page: https://patentgrep.com/patent/US7744867B2

## CPC

- A61K 31/29: Antimony or bismuth compounds
- A61K 31/39: having oxygen in the same ring
- A61K 38/193: {Colony stimulating factors [CSF]}
- A61K 38/21: Interferons {[IFN]}
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- G01N 2333/9121: with an alcohol group as acceptor (2.7.1), e.g. general tyrosine, serine or threonine kinases
- G01N 2500/04: Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
- 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
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

The various embodiments of the present invention are directed to pentavalent antimonials, purified pentavalent antimonials, and pentavalent antimonials that are comprised of an antimonial portion and an organic moeity portion. Alternatively the present invention is directed to agents and methods of screening agents which mimic the activity of pentavalent antimonials, particularly sodium stibogluconate and glucatime. An appropriate organic moeity may be selected based upon a desired interaction (e.g. steric action) with active site of a cellular component (e.g. a PTPase). In a preferred embodiment of the present invention the active site includes a cysteine residue which may be impacted by the compositions of the present invention.

## Claims

### Claim 1

A therapeutic composition comprising:
(i) an effective amount of a pentavalent antimonial selected from the group consisting of glucantime and sodium stibogluconate, wherein said effective amount is from about 10 mg/kg to 140 mg/kg of said pentavalent antimonial; and
(ii) further comprising an effective amount of IFN-α.

### Claim 2 (depends on 1)

The therapeutic composition of claim 1, wherein said pentavalent antimonial is glucantime.

### Claim 3 (depends on 1)

The therapeutic composition of claim 1, wherein said pentavalent antimonial is sodium stibogluconate.

### Claim 4 (depends on 1)

The therapeutic composition of claim 1, wherein said effective amount of the pentavalent antimonial is effective in treating cancer.

### Claim 5 (depends on 4)

The therapeutic composition of claim 4, wherein said cancer is selected from the group consisting of lymphoma, multiple myeloma, leukemia, melanoma, prostate cancer, breast cancer, renal cancer, and bladder cancer.

### Claim 6 (depends on 1)

The therapeutic composition of claim 1, wherein said effective amount of the pentavalent antimonial is effective in enhancing cytokine activity.

### Claim 7 (depends on 1)

The therapeutic composition of claim 1, wherein said effective amount of the cytokine is about 500 U/ml.

### Claim 8

A therapeutic composition comprising an effective amount of a purified fraction of a pentavalent antimonial, selected from the group consisting of glucantime and sodium stibogluconate, wherein said effective amount is from about 20 mg/kg to 50 mg/kg of said pentavalent antimonial and further comprising an effective amount of IFN-α.

### Claim 9 (depends on 8)

The therapeutic composition of claim 8, wherein said pentavalent antimonial is glucantime.

### Claim 10 (depends on 8)

The therapeutic composition of claim 8, wherein said pentavalent antimonial is sodium stibogluconate.

### Claim 11 (depends on 8)

The therapeutic composition of claim 8, wherein said effective amount of the pentavalent antimonial is effective in treating cancer.

### Claim 12 (depends on 11)

The therapeutic composition of claim 11, wherein said cancer is selected from the group consisting of lymphoma, multiple myeloma, leukemia, melanoma, prostate cancer, breast cancer, renal cancer, and bladder cancer.

### Claim 13 (depends on 8)

The therapeutic composition of claim 8, wherein said effective amount of pentavalent antimonial is effective in enhancing cytokine activity.

### Claim 14 (depends on 8)

The therapeutic composition of claim 8, wherein said effective amount of the cytokine is about 500 U/ml.

### Claim 15 (depends on 1)

The therapeutic composition of claim 1, further comprising a pharmaceutically acceptable carrier.

### Claim 16 (depends on 8)

The therapeutic composition of claim 8, further comprising a pharmaceutically acceptable carrier.

### Claim 17 (depends on 8)

The therapeutic composition of claim 8, wherein said effective amount of the cytokine is about 500,000 Units.

### Claim 18 (depends on 1)

The therapeutic composition of claim 1, wherein said effective amount of the cytokine is about 500,000 Units.