2. Academic Validation
  3. A novel orally active inhibitor of HLE

A novel orally active inhibitor of HLE

  • Eur J Med Chem. 2003 Apr;38(4):421-5. doi: 10.1016/s0223-5234(03)00046-1.
Márton Varga 1,  Zoltán Kapui,  Sándor Bátori,  Lajos T Nagy,  Lelle Vasvári-Debreczy,  Endre Mikus,  Katalin Urbán-Szabó,  Péter Arányi
Affiliations

Affiliation

  • 1 Chinoin Co. Ltd - Member of Sanofi-Synthelabo Group, Discovery Research, H-1045, Tó utca 1-5, Budapest, Hungary, marton.varga@sanofi-synthelabo.com
PMID: 12750030 DOI: 10.1016/s0223-5234(03)00046-1
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).

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