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COMPOUNDS FOR USE IN THE TREATMENT OF HEART FAILURE WITH PRESERVED EJECTION FRACTION (HFPEF), THROUGH TARGETING OF S100A9 AND CORRESPONDING DIMER PARTNER AND RECEPTORSCM Patents

The present invention refers to inhibitors of the S100 calcium- binding protein A9 (S100A9)/S100A8 – Toll Like Receptor 4(TLR4) dimer-receptor axis for use in the treatment of Heart Failure with preserved Ejection Fraction (HFpEF). The present invention further refers to pharmaceutical formulations comprising the said inhibitors. The present invention's use of compounds and pharmaceutical formulations may be advantageously employed in HFpEF by attenuating the deleterious effect on endothelial function and prevention of inflammation, production of reactive oxygen species, apoptosis, senescence and pro-fibrotic phenotype.

Datos clave

CategoríaInvención

Índice de la ficha

Updated at
05/11/2026
Numero publicacion
WO.2025122021.A1
Fecha publicacion
12/06/2025
Anio publicacion
2025
Numero solicitud
WO2024PT50047

En detalle

Reivindicaciones

CLAIMS 1. Inhibitors of the S100 calcium-binding protein A9 (S100A9) /S100A8 - Toll Like Receptor 4 (TLR4) dimer-receptor axis for use in the treatment of heart failure with preserved ejection fraction (HFpEF) , through attenuating the deleterious effect of EVs on endothelial function and prevention of a pro-fibrotic phenotype. 2. Use according to claim 1 wherein the said inhibitors comprise Resatorvid (TAK-242, CLI095) ; Eritoran; Dutasteride (DB01126) ; Buclizine (DB00354) ; Conivaptan (DB00872) ; Lomitapide (DB08827) ; Adapalene (DB00210) ; Lumacaftor (DB09280) ; Dihydroergotamine (DB00320) ; Bromocriptine (DB01200) ; Tolvaptan (DB06212) Nandrolone phenpropionate (DB00984) ; Flunarizine (DB04841) ; Irinotecan (DB00762) ; Dihydrotachysterol (DB01070) ; Antrafenine (DB01419) ; Nilotinib (DB04868) ; Medrogestone (DB09124) ; Itraconazole (DB01167) ; Doxercalci f erol (DB06410) ; Ponatinib (DB08901) ; Netupitant (DB09048) ; Difenoxin (DB01501) ; Paricalcitol (DB00910) ; Pimozide (DB01100) ; Tasosartan (DB01349) ; Alfacalcidol (DB01436) ; Fluspirilene (DB04842) ; Azilsartan medoxomil (DB08822) ; Cabozantinib (DB08875) ; Lorpiprazole (DB09195) Ergocalciferol (DB00153) ; Loperamide (DB00836) ; Drospirenone (DB01395) Pranlukast (DB01411) ; Ziprasidone (DB00246) ; Meclizine (DB00737) ; Sertindole (DB06144) ; Lurasidone (DB08815) ; Vorapaxar (DB09030) ; Umeclidinium (DB09076) , as well as S100A9 Inhibitors, such as ABR-238901; Tasquinimod (ABR-215050 ) ; Paquinimod (ABR 25757) ; laquinimod (ABR-215062 ) ; Roquinimex (ABR212626) ; Azeliragon; FPS-ZM1; RAGE 229; AC-73; antagonist peptide-9 (AP9) and combinations thereof . 3. Pharmaceutical formulation for use for use in the treatment of HFpEF characterized by comprising inhibitors of the S100A9/S100A8-TLR4 dimer-receptor axis. 4. Pharmaceutical formulation according to claim 3 wherein the said inhibitors comprise Resatorvid (TAK-242, CLI095) ; Eritoran; Dutasteride (DB01126) ; Buclizine (DB00354) ; Conivaptan (DB00872) ; Lomitapide (DB08827) ; Adapalene (DB00210) ; Lumacaftor (DB09280) ; Dihydroergotamine (DB00320) ; Bromocriptine (DB01200) ; Tolvaptan (DB06212) Nandrolone phenpropionate (DB00984) ; Flunarizine (DB04841) ; Irinotecan (DB00762) ; Dihydrotachysterol (DB01070) ; Antrafenine (DB01419) ; Nilotinib (DB04868) ; Medrogestone (DB09124) ; Itraconazole (DB01167) ; Doxercalcif erol (DB06410) ; Ponatinib (DB08901) ; Netupitant (DB09048) ; Difenoxin (DB01501) ; Paricalcitol (DB00910) ; Pimozide (DB01100) ; Tasosartan (DB01349) ; Alfacalcidol (DB01436) ; Fluspirilene (DB04842) ; Azilsartan medoxomil (DB08822) ; Cabozantinib (DB08875) ; Lorpiprazole (DB09195) Ergocalciferol (DB00153) ; Loperamide (DB00836) ; Drospirenone (DB01395) Pranlukast (DB01411) ; Ziprasidone (DB00246) ; Meclizine (DB00737) ; Sertindole (DB06144) ; Lurasidone (DB08815) ; Vorapaxar (DB09030) ; Umeclidinium (DB09076) ; ABR- 238901; Tasquinimod (ABR-215050) ; Paquinimod (ABR 25757) ; laquinimod (ABR-215062 ) ; Roquinimex (ABR212626) , Azeliragon; FPS-ZM1; RAGE 229; AC-73; antagonist peptide-9 (AP9) and combinations thereof. Lisbon, 6<th>December 2024

Etiquetas

Inventores
Esperança dos Santos Nascimento DianaESPERANÇA dos SANTOS NASCIMENTO, DianaDA COSTA SILVA, Elsa DanielaDa Costa Silva Elsa DanielaDA CONCEIÇÃO PINTO-DO-Ó, PerpétuaDa Conceição Pinto-Do-Ó PerpétuaPérez Vizcaíno FranciscoPÉREZ VIZCAÍNO, FranciscoCorreia Ferreira Leite-Moreira Joaquim AdelinoCORREIA FERREIRA LEITE-MOREIRA, Joaquim Adelino
Solicitantes
I3S - Instituto de Investigação e Inovação em Saúde, AssociaçãoUniversidad Complutense de MadridUniversidade do Porto
Clasificacion ipc
A61K 31/ 18 A IA61K 31/ 4704 A IA61P 9/ 04 A I
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