Université De Sherbrooke

Societe De Commercialisation Des Produits De La Recheche Appliquee-socpra-science Sante Et Humaines S.e.c.

Domenico Regoli

Witold A Neugebauer

Fernand Gobeil

Pierre Sirois

David Fortin

Bichov Gabra

The present invention provides for novel kinin B1 receptors peptide agonists of formula (I) having very good to excellent affinities and selectivity for the Breceptor, in vitro and in vivo increased resistance to enzymatic degradation, superior pharmacokinetic properties to those of naturally occurring agents, capacity to significantly enhance delivery of chemotherapeutic substances across the blood brain barrier and within peripheral tissues for the treatment of tumors, capacity to protect and restore kidney, heart, brain and other organ functions, when given alone or in combination with other therapies in the treatment of hypertension, diabetes and other cardiovascular diseases particularly, but not limited to, atherosclerosis and arteriosclerosis. Formula (I): aa-aa-aa-aa-aa-aa-aa-aa-Ser-Pro-D-Phe-X.

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The present invention provides for a novel peptidic antagonist for the bradykinin B1 (BKB) receptor having very good to excellent affinities and selectivity for the BKBreceptor, in vitro and in vivo increase resistance to enzymatic degradation, superior pharmacokinetic properties, capability to significantly reduce microvascular leakage observed alongside diabetic-induced increase in vascular permeability, capability to significantly reduced the state of hyperalgesia alongside diabetes, capability to significantly reduce the infiltration of pro-inflammatory cells and general state of inflammation alongside allergic asthma.

Selective bradykinin (BK) B1 peptidic receptor antagonists and uses thereof

Growing community of inventors

Sherbrooke, Canada

Domenico Regoli