A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/70 (2006.01) C07H 21/00 (2006.01)
Patent
CA 2332540
The present invention relates to P1-(cytidine 5'-)-P4-(uridine 5'- )tetraphosphates and its salts, esters and amides, and formulations thereof which are highly stable and selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. The compounds of the invention are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, primary ciliary dyskinesia, cystic fibrosis, as well as prevention of pneumonia due to immobility, and the induction of sputum and its expectoration. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis and otitis media. They are also useful in the treatment of dry eye disease and retinal detachment.
L'invention concerne des P?1¿-(cytidine 5'-)-P?4¿-(uridine 5'-)tétraphosphates, leurs sels, esters et amides, ainsi que des formulations élaborées à base de ces derniers qui sont des agonistes sélectifs extrêmement stables du récepteur purinergique P2Y¿2? et/P2Y¿4?. Ces composés sont utiles pour traiter des maladies pulmonaires obstructives chroniques, telles que la bronchite chronique, la dyskinésie ciliaire primaire, la fibrose kystique, ainsi que pour prévenir la pneumonie due à l'immobilité et pour provoquer les crachats et leur expectoration. De plus, étant donné leur capacité générale à dégager les sécrétions des mucosités retenues et à stimuler la fréquence des battements ciliaires, ces composés sont également utiles pour traiter les milieux favorables aux otites et aux sinusites.
Boucher Richard C.
Pendergast William
Picher Maryse
Rideout Janet L.
Stutts Monroe Jackson
Gowling Lafleur Henderson Llp
Inspire Pharmaceuticals Inc.
The University Of North Carolina At Chapel Hill
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