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DHP-I INHIBITORS FOR USE AS NEUROPROTECTANTS AND IN THE TREATMENT OF NEUROINFLAMMATORY DAMAGES OF THE VISUAL PATHWAYCM Patents

Índice de la ficha

Updated at
24/07/2026
Numero publicacion
EP.4574146.A1
Fecha publicacion
25/06/2025
Numero solicitud
EP20230383314
Fecha presentacion
18/12/2023

En detalle

Resumen

[0001] The present invention relates to a DHP-I inhibitor for use in a method for the prophylactic and/or therapeutic treatment of a neuroinflammatory disease. In some embodiments, it relates to a DHP-I inhibitor for use in a method for the prophylactic treatment of neurodegeneration. The present invention also relates to a DHP-I inhibitor for use as neuroprotectant. It further pertains to related methods for the prophylactic and/or therapeutic treatment of a neuroinflammatory disease and the use of a DHP-I inhibitor in the manufacturing of a medicament for use in these methods. The present invention also provides pharmaceutical compositions and delivery systems for use in the methods of the invention, as well as to a pharmaceutical composition or drug delivery systems suitable for administration by a route bypassing the blood brain barrier (BBB) and/or the blood retinal barrier (BRB), preferably selected intrathecal, intracranial, intranasal and/or ocular administration; or suitable for trespassing the BBB and/or the BRB.

Reivindicaciones

1. DHP-I inhibitor for use as a neuroprotective medicament. 2. DHP-I inhibitor for use in a method for the prophylactic and/or therapeutic treatment of a neuroinflammatory disease in a mammalian subject, preferably a human subject, wherein a neuroinflammatory disease is a neurological or mental disease of the central nervous system (CNS) and/or the peripheral nervous system (PNS), which pathogenesis involves primary or secondary neuroinflammation and may evolve into neurodegeneration. 3. The DHP-I inhibitor for use according to claim 2, wherein the neuroinflammatory disease is a neurological disease, preferably selected from the group consisting of Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, ocular neurodegenerative diseases, primary tauopathies, frontotemporal dementia (FTD), synucleinopathies (e.g., Lewy body dementia [LBD] and multisystem atrophy [MSA]), Huntington's disease (HD) and related polyglutamine (polyQ) diseases (including spinocerebellar ataxias [SCA]), prion disease (PrD), traumatic brain injury (TBI), chronic traumatic encephalopathy (CTE), stroke, migraine, spinal cord injury (SCI) and autoimmune encephalitides, such as systemic lupus erythematosus, Hashimoto encephalopathy, Sydenham chorea, Behçhet disease, Rasmussen encephalitis and limbic encephalitis epilepsy. 4. The DHP-I inhibitor for use according to claim 3, wherein the neuroinflammatory disease is an ocular neurodegenerative disease, preferably selected from the group consisting of glaucoma, age-related macular degeneration, diabetic retinopathy, retinitis pigmentosa and neuromyelitis optica spectrum disorders (NMOSD). 5. The DHP-I inhibitor for use according to claim 4, wherein the ocular neurodegenerative disease is glaucoma, such as, (i) normotensive glaucoma or (ii) high pressure glaucoma, including high pressure glaucoma resistant to intraocular pression (IOP)-lowering treatment. 6. The DHP-I inhibitor for use according to any one of claims 2 to 5, wherein the DHP-I inhibitor is administered by a systemic route of administration, preferably by the parenteral route, such as by the intramuscular, intraperitoneal, subcutaneous or intravascular route, more preferably by the intravascular route. 7. The DHP-I inhibitor for use according to any one of claims 2 to 6, wherein the DHP-I inhibitor is administered by the intrathecal or intracranial route or locally in the eye by topical, intraocular, comprising intravitreal or intracameral administration, and/or periocular administration, such as by subconjunctival, retrobulbar, peribulbar, subtenon, posterior juxtascleral, transcleral or suprachoroidal administration, preferably by intravitreal administration. 8. The DHP-I inhibitor for use according to any one of claims 2 to 7, wherein the DHP-I inhibitor is administered in combination with another treatment. 9. The DHP-I inhibitor for use according to claim 8, wherein the DHP-I inhibitor and the other treatment are simultaneously administered, preferably forming part of the same pharmaceutical composition or wherein the DHP-I inhibitor and the other treatment are separately administered. 10. The DHP-I inhibitor for use according to any one of claims 2 to 7, wherein the method comprises administering the DHP-I inhibitor as single agent. 11. A pharmaceutical composition comprising a DHP-I inhibitor and a pharmaceutically acceptable excipient; or a drug delivery system comprising a DHP-I inhibitor or the pharmaceutical composition comprising thereof, for use according to anyone of claims 1 to 10. 12. A pharmaceutical composition comprising a DHP-I inhibitor and a pharmaceutically acceptable excipient, or a drug delivery system comprising a DHP-I inhibitor or the pharmaceutical composition comprising thereof, wherein the pharmaceutical composition or drug delivery system is suitable for trespassing the blood brain barrier (BBB) and/or the blood retinal barrier (BRB). 13. A pharmaceutical composition comprising a DHP-I inhibitor and a pharmaceutically acceptable excipient, or a drug delivery system comprising a DHP-I inhibitor or the pharmaceutical composition comprising thereof, wherein the pharmaceutical composition or drug delivery system is suitable for administration by a route bypassing the BBB, preferably selected from intrathecal, intracranial, intranasal and/or ocular administration, including topical, intraocular and/or periocular administration. 14. The drug delivery system according to claim 13, wherein the delivery system is an ocular delivery system, such as contact lenses, ocular implants, or microneedles; or wherein the delivery system is an implantable device, such as an implantable cathether-pump system. 15. The DHP-I inhibitor for use according to any of claims 1 to 10, the pharmaceutical composition or drug delivery system for use of claim 11, or the pharmaceutical composition or drug delivery system of any of claims 12 or 13, wherein the DHP-I inhibitor is cilastatin or a pharmaceutically acceptable salt thereof, preferably cilastatin sodium.

Etiquetas

Inventores
Lázaro Fernández AlbertoLópez Gallardo MeritxellGonzález-Nicolás González María ÁngelesMarco López Eva MaríaMartín Sánchez BeatrizSan Felipe Riba DiegoLlorente de Miguel RicardoMartínez López Miguel ÁngelRubio Casado Sara
Solicitantes
Telara Pharma S LFundacion Para la Investig Biomedica del Hospital Gregorio Maranon FibhgmUniversidad Complutense de Madrid
Clasificacion ipc
A61K 31/ 198 A IA61P 27/ 06 A IA61K 9/ 00 A IA61P 25/ 00 A I
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