Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Bradykinin; kallidin; related peptides
Reexamination Certificate
2006-05-09
2006-05-09
Weber, Jon (Department: 1653)
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Bradykinin; kallidin; related peptides
C514S002600, C514S015800, C530S327000, C530S328000, C424S009100
Reexamination Certificate
active
07041785
ABSTRACT:
The present invention relates to novel antagonists to a B1-bradykinin (B1-BK) receptor which have a good affinity and selectivity therefor, some of which being at least partially resistant to enzymatic degradation. The synthesis of the B1receptors is induced during inflammation. Symptoms associated with inflammation (elevated hydrostatic pressure and plasma leakage or extravasation) have been observed in diabetic animal models (streptozotocin-induced diabetes (STZ)) as well as in spontaneously hypertensive rats (SHR). The present inventors confirm the presence of B1-BK receptors in these two models. B1-BK antagonists abolished the vasocontraction induced by B1-BK in SHR and STZ, and reduced the glycemia of diabetic animals to normal levels. The present B1-antagonists are useful for treating any condition wherein B1-receptor is expressed, particularly during inflammation, and more particularly wherein B1-receptor expression results in diabetic vasculopathy, other diabetic symptoms associated with an insulitis and a post-capillary resistance building as a consequence of the presence of a B1-receptor.
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Catanzaro Orlando L.
Gobeil Fernand
Neugebauer Witold A.
Plante Gerard E.
Recoli Domenico
Innovar L.L.C.
Kam Chih-Min
Matos Rick
Universite de Sherbrooke
Weber Jon
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