# US 2025/0205239 A1 · Compositions and methods for preventing and treating neurodegenerative diseases > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2025/0205239 A1 - Document ID: US20250205239A1 - Status: Published application - Kind: A1 - Application number: 18/991,922 - Filed: 2024-12-23 - Published: 2025-06-26 - Earliest claimed: 2022-06-24 - Assignees: Aribio Co., Ltd. - Applicants: Aribio Co., Ltd. - Inventors: Jai Jun Choung; Bo Seung Seo; Byungwoo Kang - Web page: https://patentgrep.com/patent/US20250205239A1 ## CPC - A61K 31/519: ortho- or peri-condensed with heterocyclic rings - A61K 31/27: of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine - A61K 31/325: Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof (thiurams A61K31/145) - A61K 31/445: Non condensed piperidines, e.g. piperocaine - A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - 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 present invention provides a composition for preventing or treating a neurodegenerative disease containing a phosphodiesterase 5 inhibitor (PDE5 inhibitors) and an acetylcholinesterase inhibitor (AChEI) and a method using thereof, wherein the PDE5 inhibitor is selected from among mirodenafil, sildenafil, vardenafil, tadalafil, udenafil, dasantafil, avanafil, pharmaceutically acceptable salts, solvates, hydrates, and a mixture thereof; and the AchEI is selected from among donepezil, rivastigmine, galantamine, physostigmine, tacrine, metrifonate, phenserine, tolserine, eseroline, huperizine A and B, galangin, cardanol, donepezil-AP2238, donepezil-tacrine, tacrine-ferulic acid hybrid, tacrine-hydroxyquinoline, ladostigil, indenyl derivatives, pharmaceutically acceptable salts, solvates, hydrates and a mixture thereof; and the neurodegenerative disease is dementia, Parkinson's disease (PD), Alzheimer's disease (AD), Huntington's disease (HD) or Multiple sclerosis (MS). ## Claims ### Claim at position 1 1-16. (canceled) ### Claim 17 A pharmaceutical composition comprising: at least one phosphodiesterase 5 inhibitor; and at least one acetylcholinesterase inhibitor as active ingredients, and pharmaceutically acceptable salts, solvates, hydrates of said phosphodiesterase 5 inhibitor and said acetylcholinesterase inhibitor. ### Claim 18 (depends on 17) The composition of claim 17, wherein the phosphodiesterase 5 inhibitor comprises mirodenafil, sildenafil, vardenafil, tadalafil, udenafil, dasantafil, avanafil, and derivatives and mixtures thereof. ### Claim 19 (depends on 18) The composition of claim 18, wherein the phosphodiesterase 5 inhibitor is mirodenafil and derivatives thereof. ### Claim 20 (depends on 17) The composition of claim 17, wherein the acetylcholinesterase inhibitor comprises donepezil, rivastigmine, galantamine, physostigmine, tacrine, metrifonate, phenserine, tolserine, eseroline, huperizine A and B, galangin, cardanol, donepezil-AP2238, donepezil-tacrine, tacrine-ferulic acid hybrid, tacrine-hydroxyquinoline, ladostigil, indenyl derivatives, and mixtures thereof. ### Claim 21 (depends on 17) A method for preventing or treating neuroinflammation comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 22 (depends on 17) A method for preventing and/or inhibiting formation and/or accumulation of beta-amyloid comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 23 (depends on 17) A method for preventing or treating a neurodegenerative disease comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 24 (depends on 23) The method of claim 23, wherein the neurodegenerative disease comprises dementia, Parkinson's disease (PD), Dementia with Lewy body (DLB), Alzheimer's disease (AD), Huntington's disease (HD), Multiple sclerosis (MS), Vascular Dementia (VaD), and a mixed etiologies thereof. ### Claim 25 (depends on 17) A method for preventing or treating Dementia comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 26 (depends on 17) A method for inhibiting Aβ Oligomer/Fibril formation by reducing Aβ aggregation comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 27 (depends on 17) A method for inhibiting β-Amyloidogenic processing by reducing BACE-1 comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 28 (depends on 17) A method for reducing extracellular Aβ monomers, oligomers & Aβ Fibril/Plaque by increasing the cerebral blood flow comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 29 (depends on 17) A method for suppressing neuronal cell death, promoting neurogenesis, synaptogenesis and/or angiogenesis by activating NO/cGMP/PKG/CREB Pathway comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 30 (depends on 17) A method for restoring synaptic plasticity by activating Wint signaling and/or inhibiting DKK-1 comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 31 (depends on 17) A method for inhibiting production of APP and/or reducing Aβ accumulation by suppressing positive feedback loop for Aβ production comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 32 (depends on 17) A method for inhibiting formation of Aβ Fibril/plaque by removing intracellular toxic and soluble Aβ oligomers by activating autophagy comprising: administering an effective amount of the pharmaceutical composition of claim 17. ### Claim 33 A pharmaceutical composition, mirodenafil, or pharmaceutically acceptable salts, solvates, hydrates, derivatives thereof; and at least one of donepezil, galantamine, rivastigmine, or pharmaceutically acceptable salts, solvates, hydrates, derivatives, and/or mixtures thereof. ### Claim 34 (depends on 33) A method for preventing or treating neuroinflammation comprising: administering an effective amount of the pharmaceutical composition of claim 33. ### Claim 35 (depends on 33) A method for preventing or inhibiting formation and/or accumulation of beta-amyloid comprising: administering an effective amount of the pharmaceutical composition of claim 33. ### Claim 36 (depends on 33) A method for preventing or treating a neurodegenerative disease comprising: administering an effective amount of the pharmaceutical composition of claim 33. ### Claim 37 (depends on 36) The method of claim 36, wherein the neurodegenerative disease comprises dementia, Parkinson's disease (PD), Dementia with Lewy body (DLB), Alzheimer's disease (AD), Huntington's disease (HD), Multiple sclerosis (MS), Vascular Dementia (VaD), and a mixed etiologies thereof. ### Claim 38 (depends on 33) A method for preventing or treating Dementia comprising: administering an effective amount of the pharmaceutical composition of claim 33. ### Claim 39 (depends on 33) A method for inhibiting Aβ Oligomer/Fibril formation by reducing Aβ aggregation comprising: administering an effective amount of the pharmaceutical composition of claim 33. ### Claim 40 (depends on 33) A method for inhibiting β-Amyloidogenic processing by reducing BACE-1 comprising: administering an effective amount of the pharmaceutical composition of claim 33. ### Claim 41 (depends on 33) A method for reducing extracellular Aβ monomers, oligomers & Aβ Fibril/Plaque by increasing the cerebral blood flow comprising: administering an effective amount of a pharmaceutical composition of claim 33. ### Claim 42 (depends on 33) A method for suppressing neuronal cell death, promoting neurogenesis, synaptogenesis and/or angiogenesis by activating NO/cGMP/PKG/CREB Pathway comprising: administering an effective amount of the pharmaceutical composition of claim 33. ### Claim 43 (depends on 33) A method for restoring synaptic plasticity by activating Wint signaling and/or inhibiting DKK-1 comprising: administering an effective amount of the pharmaceutical composition of claim 33. ### Claim 44 (depends on 33) A method for inhibiting the production of APP and/or reducing Aβ accumulation by suppressing positive feedback loop for Aβ production comprising: administering an effective amount of the pharmaceutical composition of claim 33. ### Claim 45 (depends on 33) A method for inhibiting formation of Aβ Fibril/plaque by removing intracellular toxic and soluble Aβ oligomers by activating autophagy comprising: administering an effective amount of the pharmaceutical composition of claim 33.