# US 8,541,467 B2 · Use of 2,5-dihydroxybenzene compounds and derivatives for the treatment of hematological dyscrasias and cancer of an organ

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- Number: US 8,541,467 B2
- Document ID: US8541467B2
- Status: Granted
- Kind: B2
- Application number: 11/839,525
- Filed: 2007-08-15
- Published: 2008-05-29
- Granted: 2013-09-24
- Earliest claimed: 2006-08-16
- Assignees: Action Medicines, S.L.
- Applicants: Pedro Cuevas Sánchez; Guillermo Gimenez Gallego; Inigo Saenz de Tejada Morgan; Javier Angulo Frutos; Rosa Maria Lozano Puerto; Antonio Romero Garrido; Serafin Valverde Lopez
- Inventors: Pedro Cuevas Sánchez; Guillermo Gimenez Gallego; Inigo Saenz de Tejada Morgan; Javier Angulo Frutos; Rosa Maria Lozano Puerto; Antonio Romero Garrido; Serafin Valverde Lopez
- Web page: https://patentgrep.com/patent/US8541467B2

## CPC

- A61K 31/255: of sulfoxy acids or sulfur analogues thereof
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 31/095: Sulfur, selenium, or tellurium compounds, e.g. thiols
- A61K 31/10: Sulfides; Sulfoxides; Sulfones
- A61K 31/185: Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids (hydroxamic acids A61K31/16; peroxy acids A61K31/327)
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/216: of acids having aromatic rings, e.g. benactizyne, clofibrate
- A61K 31/222: with compounds having aromatic groups, e.g. dipivefrine, ibopamine
- A61K 31/225: Polycarboxylic acids
- A61K 31/235: having an aromatic ring attached to a carboxyl group
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 17/12: Keratolytics, e.g. wart or anti-corn preparations
- A61P 23/00: Anaesthetics
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/10: Antimycotics
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 57/44: Cinnamic acid
- C07C 59/68: the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring
- C07C 65/03: monocyclic and having all hydroxy or O-metal groups bound to the ring
- C07C 65/19: having unsaturation outside the aromatic ring
- C07C 69/017: Esters of hydroxy compounds having the esterified hydroxy group bound to a carbon atom of a six-membered aromatic ring
- C07C 69/84: of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
- C07C 309/24: of a carbon skeleton containing six-membered aromatic rings
- C07C 309/42: having the sulfo groups bound to carbon atoms of non-condensed six-membered aromatic rings
- C07C 309/68: of a carbon skeleton substituted by singly-bound oxygen atoms
- C07C 309/75: containing singly-bound oxygen atoms bound to the carbon skeleton
- 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

## Abstract

The present invention refers to the use of the compound of Formula (I′) or pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of hematological dyscrasias, including myelodisplastic syndromes (MDSs) and for improving the efficacy of chemotherapy, radiation therapy and/or cancer immunotherapy. In addition, it relates to the use of a compound of formula (I″) for the treatment and/or prophylaxis of cancer of an organ.

## Claims

### Claim 1

A method for therapeutic treatment of existing glioma comprising administering to a subject in need of treatment of glioma a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof, wherein the compound is 2,5-bis(acetyloxy)benzenesulfonic acid.

### Claim 2 (depends on 1)

The method of claim 1, wherein the compound is administered topically, transdermally, orally, buccally, parenterally, by inhalation, rectally, intravaginally, intraocularly or otically.

### Claim 3 (depends on 1)

The method of claim 1, further comprising administration of at least one additional therapeutic agent.

### Claim 4 (depends on 1)

The method of claim 1, wherein the compound is administered at least once per week.

### Claim 5 (depends on 4)

The method of claim 4, wherein the compound is administered at least once per day.

### Claim 6 (depends on 5)

The method of claim 5, wherein the compound is administered at least twice per day.

### Claim 7 (depends on 1)

The method of claim 1, wherein the compound is present in a pharmaceutical composition in an amount of about 0.001% to about 30% w/w.

### Claim 8 (depends on 7)

The method of claim 7, wherein the compound is present in a pharmaceutical composition in an amount of at least about 2.5% w/w.

### Claim 9 (depends on 7)

The method of claim 7, wherein the compound is present in a pharmaceutical composition in an amount of at least about 5% w/w.

### Claim 10 (depends on 7)

The method of claim 7, wherein the compound is present in a pharmaceutical composition in an amount of at least about 10% w/w.

### Claim 11 (depends on 7)

The method of claim 7, wherein the compound is present in a pharmaceutical composition in an amount of at least about 15% w/w.

### Claim 12 (depends on 1)

The method of claim 1, wherein the compound is administered over a period of at least about one week.

### Claim 13 (depends on 12)

The method of claim 12, wherein the compound is administered over a period of at least about four weeks.

### Claim 14 (depends on 7)

The method of claim 7, wherein the compound is present in a pharmaceutical composition in an amount of about 1% w/w.