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1. WO2020064597 - USE OF EPAC1 ACTIVATORS FOR THE TREATMENT OF CHRONIC KIDNEY DISEASES

Publication Number WO/2020/064597
Publication Date 02.04.2020
International Application No. PCT/EP2019/075468
International Filing Date 23.09.2019
IPC
A61K 31/7076 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7076containing purines, e.g. adenosine, adenylic acid
A61K 38/17 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
A61P 13/12 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
CPC
A61K 31/7076
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7076containing purines, e.g. adenosine, adenylic acid
A61K 31/7088
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
A61K 38/1709
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
1703from vertebrates
1709from mammals
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
Applicants
  • INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) [FR]/[FR]
  • UNIVERSITÉ PAUL SABATIER TOULOUSE III [FR]/[FR]
  • SORBONNE UNIVERSITÉ, [FR]/[FR]
Inventors
  • LEZOUALC'H, Frank
  • CHATZIANTONIOU, Christos
  • KAVVADAS, Panagiotis
Agents
  • INSERM TRANSFERT
Priority Data
18306233.024.09.2018EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) USE OF EPAC1 ACTIVATORS FOR THE TREATMENT OF CHRONIC KIDNEY DISEASES
(FR) UTILISATION D'ACTIVATEURS EPAC1 POUR LE TRAITEMENT DE MALADIES RÉNALES CHRONIQUES
Abstract
(EN)
Chronic Kidney Disease (CKD) is a major burden of public health affecting millions of people around the world. It is rising in prevalence with high public health costs and is associated with a high degree of morbidity and mortality. Here, the inventors determined whether the exchange protein directly activated by cAMP 1 (Epac1) contributed to severe glomurelonephritis (GN) induced by injecting nephrotoxic serum (NTS) in mice. Treatment of GN mice with a pharmacological activator of Epacl, 8-(4-Chlorophenylthio)-2'-O-methyladenosine-3', 5'- cyclic monophosphate (8-pCPT) improved functional and structural renal parameters, and reduced renal inflammation after NTS injection. Taken together, these findings suggest that Epacl activation is an attractive and promising pharmacological intervention for the therapeutic treatment of CKD. Thus the present invention relates to use of Epac1 activators for the treatment of chronic kidney diseases..
(FR)
La maladie rénale chronique (CKD) est une charge majeure de la santé publique affectant des millions de personnes dans le monde. Celle-ci s'élève en prévalence avec des coûts de santé publique élevés et est associée à un degré élevé de morbidité et de mortalité. Ici, les inventeurs ont déterminé si la protéine d'échange directement activée par cAMP 1 (Epac1) a contribué à une glomurélonéphrite (GN) grave induite par l'injection de sérum néphrotoxique (NTS) chez des souris. Le traitement de souris GN avec un activateur pharmacologique de Epac1, 8-(4-Chlorophénylthio)-2'-O-méthyladénosine-3', monophosphate cyclique-5' (8-pCPT) a amélioré des paramètres rénaux fonctionnels et structuraux, et a réduit l'inflammation rénale après injection de NTS. Considérés ensemble, ces résultats suggèrent que l'activation de l'Epac1 est une intervention pharmacologique intéressante et prometteuse pour le traitement thérapeutique de CKD. Par conséquent, la présente invention porte sur l'utilisation d'activateurs d'Epac1 pour le traitement de maladies rénales chroniques.
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