A novel orally active inhibitor of HLE.

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).

• Authors: Márton Varga, Zoltán Kapui, Sándor Bátori, Lajos T Nagy, Lelle Vasvári-Debreczy, Endre Mikus, Katalin Urbán-Szabó, Péter Arányi
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 38 Issue 4 Pg. 421-5 (Apr 2003) ISSN: 0223-5234 [Print] France
• PMID: 12750030 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Cyclic S-Oxides
• Enzyme Inhibitors
• SSR 69071
• Thiazoles
• Leukocyte Elastase

Topics

• Administration, Oral
• Animals
• Asthma (chemically induced, drug therapy, pathology)
• Cyclic S-Oxides (chemistry, metabolism, pharmacology)
• Cystic Fibrosis (chemically induced, drug therapy, pathology)
• Dose-Response Relationship, Drug
• Enzyme Inhibitors (chemistry, metabolism, pharmacology)
• Hemorrhage (chemically induced, drug therapy, pathology)
• Humans
• Inflammation (chemically induced, drug therapy, pathology)
• Leukocyte Elastase (administration & dosage, antagonists & inhibitors, metabolism)
• Lung Diseases, Obstructive (chemically induced, drug therapy, pathology)
• Mice
• Models, Chemical
• Pulmonary Emphysema (chemically induced, drug therapy, pathology)
• Thiazoles (chemistry, metabolism, pharmacology)