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A novel orally active inhibitor of HLE
Márton Varga1, Zoltán Kapui, Sándor Bátori
1Chinoin Co. Ltd - Member of Sanofi-Synthelabo Group, Discovery Research, H-1045, Tó utca 1-5, Budapest, Hungary, marton.varga@sanofi-synthelabo.com
European Journal of Medicinal Chemistry
|May 17, 2003
Abstract:
Human leukocyte elastase (HLE) is a serine proteinase, capable of degrading a variety of structural matrix proteins. SSR69071 2-[(4-isopropyl-6-methoxy-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methoxy]-9-(2-piperidin-1-ylethoxy)-4H-pyrido[1,2-a]pyrimidin-4-one was selected as a novel orally active HLE inhibitor for treatment of chronic obstructive pulmonary diseases, asthma, emphysema, cystic fibrosis and several inflammatory diseases (WO 01/44245 A1) (J. Pharm. Exp. Ther., submitted for publication).