# US 12,005,056 B2 · Centrally-active ghrelin agonist and medical uses thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,005,056 B2 - Document ID: US12005056B2 - Status: Granted - Kind: B2 - Application number: 16/982,107 - Filed: 2019-03-14 - Published: 2023-05-25 - Granted: 2024-06-11 - Earliest claimed: 2018-03-22 - Assignees: Helsinn Healthcare SA - Applicants: Helsinn Healthcare SA - Inventors: Claudio Giuliano; Claudio Pietra; Silvina Garcia Rubio; Angelo Guainazzi; Marielle Martinez-Loi - Web page: https://patentgrep.com/patent/US12005056B2 ## CPC - A61K 31/4468: having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl - A61P 9/00: Drugs for disorders of the cardiovascular 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 25/16: Anti-Parkinson drugs - A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia - 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 new compound 3-(1-(2,3-dichloro-4-methoxyphenyl) ethyl)-1-methyl-1-(1,3, 3-trimethylpiperidin-4-yl)urea monohydrochloride salt has a high capability to permeate through the blood-brain barrier and to display, at central nervous system level, a consistent ghrelin agonist activity; the compound is effective in the treatment and/or prevention of a medical condition mediated by the ghrelin receptor in the central nervous system. In particular, in experimental tests, the compound has shown high efficacy in the treatment of neurotoxic damage, with a useful combined pattern of neuroprotective effects both at central and peripheral level. The compound is further useful in the treatment of conditions which require a reduction of the heart rate. The compound is pharmacologically active at low to moderate doses, thus showing a favourable therapeutic index. ## Claims ### Claim 1 A method of treating a medical condition mediated by the ghrelin receptor in the central nervous system of a subject in need thereof, the method comprising administering compound 3-(1-(2,3-dichloro-4-methoxyphenyl)ethyl)-1-methyl-1-(1,3,3-trimethylpiperidin-4-yl)urea monohydrochloride salt to the subject. ### Claim 2 (depends on 1) The method of claim 1, wherein said medical condition is neurodegeneration, neuropathy, neuropathic pain, encephalomyelitis, Parkinson's Disease, Alzheimer's Disease, cognitive disorders, vagal hyperstimulation, or tachycardia. ### Claim 3 (depends on 2) The method of claim 2, wherein said neuropathy is a chemotherapy-induced neuropathy. ### Claim 4 (depends on 3) The method of claim 3, wherein said chemotherapy-induced neuropathy is induced by a proteasome inhibitor or an alkylating agent. ### Claim 5 (depends on 4) The method of claim 4, wherein said proteasome inhibitor is bortezomib, carfilzomib, ixazomib, oprozomib, delanzomib, marizomib, MG-132, ONX-0914, VR-23, celastrol, or epoxomicin. ### Claim 6 (depends on 4) The method of claim 4, wherein said alkylating agent is cisplatin or carboplatin. ### Claim 7 (depends on 2) The method of claim 2, wherein said tachycardia is a chemotherapy-induced tachycardia. ### Claim 8 (depends on 1) The method of claim 1, wherein said compound is administered in a dose amount ranging from about 0.03 and to about 10 mg, expressed as free base. ### Claim 9 (depends on 1) The method of claim 1, wherein said compound is administered externally to the central nervous system. ### Claim 10 (depends on 9) The method of claim 9, wherein said compound is administered by an oral, peroral, buccal, sublingual, ocular, percutaneous, transcutaneous, intravenous, intramuscular, inhalatory or rectal route. ### Claim 11 (depends on 3) The method of claim 3, wherein said compound is administered in a dose amount ranging from about 0.03 to about 10 mg, expressed as free base. ### Claim 12 (depends on 4) The method of claim 4, wherein said compound is administered in a dose amount ranging from about 0.03 to about 10 mg, expressed as free base. ### Claim 13 (depends on 7) The method of claim 7, wherein said compound is administered in a dose amount ranging from about 0.03 to about 10 mg, expressed as free base. ### Claim 14 (depends on 3) The method of claim 3, wherein said compound is administered externally to the central nervous system. ### Claim 15 (depends on 4) The method of claim 4, wherein said compound is administered externally to the central nervous system. ### Claim 16 (depends on 7) The method of claim 7, wherein said compound is administered externally to the central nervous system. ### Claim 17 A method of preventing a medical condition mediated by the ghrelin receptor in the central nervous system of a subject in need thereof, the method comprising administering compound 3-(1-(2,3-dichloro-4-methoxyphenyl)ethyl)-1-methyl-1-(1,3,3-trimethylpiperidin-4-yl)urea monohydrochloride salt to the subject, wherein the medical condition is chemotherapy-induced neuropathy. ### Claim 18 (depends on 17) The method of claim 17, wherein said chemotherapy-induced neuropathy is induced by a proteasome inhibitor or an alkylating agent. ### Claim 19 (depends on 18) The method of claim 18, wherein said proteasome inhibitor is bortezomib, carfilzomib, ixazomib, oprozomib, delanzomib, marizomib, MG-132, ONX-0914, VR-23, celastrol, or epoxomicin. ### Claim 20 (depends on 18) The method of claim 18, wherein said alkylating agent is cisplatin or carboplatin. ### Claim 21 (depends on 17) The method of claim 17, wherein said compound is administered in a dose amount ranging from about 0.03 to about 10 mg, expressed as free base. ### Claim 22 (depends on 17) The method of claim 17, wherein said compound is administered externally to the central nervous system.