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).
MeSH terms
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Administration, Oral
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Animals
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Asthma / chemically induced
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Asthma / drug therapy
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Asthma / pathology
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Cyclic S-Oxides / chemistry
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Cyclic S-Oxides / metabolism
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Cyclic S-Oxides / pharmacology*
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Cystic Fibrosis / chemically induced
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Cystic Fibrosis / drug therapy
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Cystic Fibrosis / pathology
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / metabolism
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Enzyme Inhibitors / pharmacology*
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Hemorrhage / chemically induced
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Hemorrhage / drug therapy
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Hemorrhage / pathology
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Humans
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Inflammation / chemically induced
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Inflammation / drug therapy
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Inflammation / pathology
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Leukocyte Elastase / administration & dosage
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Leukocyte Elastase / antagonists & inhibitors*
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Leukocyte Elastase / metabolism
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Lung Diseases, Obstructive / chemically induced
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Lung Diseases, Obstructive / drug therapy
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Lung Diseases, Obstructive / pathology
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Mice
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Models, Chemical
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Pulmonary Emphysema / chemically induced
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Pulmonary Emphysema / drug therapy
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Pulmonary Emphysema / pathology
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Thiazoles / chemistry
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Thiazoles / metabolism
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Thiazoles / pharmacology*
Substances
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Cyclic S-Oxides
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Enzyme Inhibitors
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SSR 69071
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Thiazoles
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Leukocyte Elastase