# US 8,541,395 B2 · Use of telocinobufagin as an analgesic in the treatment of acute and chronic pains

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- Number: US 8,541,395 B2
- Document ID: US8541395B2
- Status: Granted
- Kind: B2
- Application number: 13/322,917
- Filed: 2010-05-26
- Published: 2012-03-29
- Granted: 2013-09-24
- Earliest claimed: 2009-05-28
- Assignees: Cristalia Produtos Quimicos Farmaceuticos Ltda.; Genpharma Consultoria Farmaceutica E Genetica Ltda.
- Applicants: Krishnamurti De Morais Carvalho; Dòris Maria Fernandes Carvalho; Maria Denise Fernandes Carvalho; Ogari de Castro Pacheco; Roberto Carlos Debom Moreira
- Inventors: Krishnamurti De Morais Carvalho; Dòris Maria Fernandes Carvalho; Maria Denise Fernandes Carvalho; Ogari de Castro Pacheco; Roberto Carlos Debom Moreira
- Web page: https://patentgrep.com/patent/US8541395B2

## CPC

- A61K 31/585: containing lactone rings, e.g. oxandrolone, bufalin
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/06: Antimigraine agents
- A61P 25/30: for treating abuse or dependence
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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

The present invention is directed to the use of telocinobufagin, or its pharmaceutically acceptable derivatives, in the manufacture of a medicament for the treatment or prevention of acute and chronic pains. The present invention also refers to a pharmaceutical composition comprising an effective amount of telocinobufagin; also provides a method to induce analgesia in response to acute and chronic pains that comprehends administering an effective amount of telocinobufagin to human beings or animals. According to the outcomes of in vivo assays, telocinobufagin is more potent than morphine, though without presenting the known side effects of opioids. In addition, in vivo and in vitro essays showed that TBC does not present cardiotoxicity.

## Claims

### Claim 1

A method for treating acute or chronic pain, comprising administering, to a human being or animal in need of said treatment, an effective amount of telocinobufagin, or an enantiomer or prodrug thereof that is selected from the group consisting of carbonates, carbamates, phosphates, phosphonates, glycosides, sulfates, fulfonates, ethers and esters of telocinobufagin, optionally in combination with a pharmaceutically acceptable excipient, wherein the pain is acute neurogenic pain or chronic neuropathic pain.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the administration to human beings or animals occurs by an oral, sublingual, nasal, rectal, intragingival, endovenous, intramuscular, intraarticular, subcutaneous, inhalatory, transdermal, topical, subarachnoid spinal or peridural spinal route.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the administration occurs by the oral route.

### Claim 4 (depends on 1)

The method of claim 1, wherein the neuropathic pain is hyperalgesia or allodynia.