Azolopyridin-2-one derivatives as lipase and phospholipase...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C514S301000, C546S115000, C546S114000

Reexamination Certificate

active

07846943

ABSTRACT:
The present invention provides compounds which have an inhibitory effect on hormone-sensitive lipase or endothelial lipase. The compounds of the invention are azolopyridin-2-one derivatives of the general formula Iwherein the substituents are as defined herein. The compounds of formula I wherein R2 is hydrogen are distinguished by favorable effects on disorders of lipid metabolism. They beneficially influence the HDL to LDL ratio and increase in particular the HDL level and are suitable for the prevention and treatment of dyslipidemias and metabolic syndrome and their diverse sequelae such as atherosclerosis, coronary heart disease, heart failure, obesity and diabetes. The compounds of formula I wherein R1 and R2 together form a ring system are distinguished by favorable effects on metabolic disorders. They beneficially influence lipid and sugar metabolism; in particular they lower the triglyceride level and are suitable for the prevention and treatment of type II diabetes and arteriosclerosis and the diverse sequelae thereof.

REFERENCES:
patent: 4988719 (1991-01-01), Wagner et al.
patent: 5147883 (1992-09-01), Aichaioui et al.
patent: WO 2004/094393 (2004-11-01), None
patent: WO 2004/094394 (2004-11-01), None
patent: WO 2005/073199 (2005-08-01), None
Claus et al., J Pharm Exper Thera, 315 (3), line 1396-1402, 2005.
Slee et al., J Med Chem, 46:1120-1122, 2003.

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