Back to results
US 6,468,996 B1Granted
Substituted hetero-polycyclic compounds as PPARα and PPARγ activators
AssigneesNovo Nordisk A/S, Dr. Reddy's Research Foundation
InventorsLone Jeppesen, Paul Stanley Bury, Per Sauerberg
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
Claims9
A compound of formula (Ia)
- wherein R1, R2, R3, and R4 independently of each other represent hydrogen, halogen, perhalomethyl, hydroxy, nitro, cyano, formyl, or C1-12-alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl, C1-12-alkoxy, aryl, aryloxy, aralkyl, aralkoxy, heterocyclyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroaralkoxy, acyl, acyloxy, hydroxyC1-12-alkyl, amino, acylamino, C1-12-alkylamino, arylamino, aralkylamino, aminoC1-12-alkyl, C1-12-alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, C1-12-alkoxyC1-12-alkyl, aryloxyC1-12-alkyl, aralkoxyC1-12-alkyl, C1-12-alkylthio, thioC1-12-alkyl, C1-12-alkoxycarbonylamino, aryloxycarbonylamino, aralkoxycarbonylamino, —COR11, or —SO2R12, wherein R11 and R12 independently of each other are selected from hydroxy, halogen, perhalomethyl, C1-6alkoxy or amiino optionally substituted with one or more C1-6-alkyl, perhalomethyl or aryl;
- optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano;
- ring A fused to the ring containing X and N represents a 5-6 membered cyclic ring, optionally substituted with one or more hydrogen, halogen, perhalomethyl, hydroxy or C1-7-alkyl, C2-7-alkenyl, C2-7-alkynyl, C1-7-alkoxy or aryl;
- X is a valence bond, —(CHR9)—, or —(C═O)—,
- Ar represents arylene or heteroarylene, optionally substituted with one or more C1-6-alkyl or aryl;
- R5 represents hydrogen, hydroxy, halogen, C1-12-alkoxy, C1-12-alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl or aralkyl;
- optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano;
- or R5 forms a bond together with R6,
- R6 represents hydrogen, hydroxy, halogen, C1-12-alkoxy, C1-12-alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl, acyl or aralkyl;
- optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano;
- or R6 forms a bond together with R5,
- R7 represents hydrogen, C1-12-alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl, aryl, aralkyl, C1-12-alkoxyC1-12-alkyl, C1-12-alkoxycarbonyl, aryloxycarbonyl, C1-12-alkylaminocarbonyl, arylaminocarbonyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl groups;
- optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano;
- R8 represents hydrogen, C1-12-alkyl, C4-12-alkenynyl, C2-12-alkenyl, C2-12-alkynyl, aryl, aralkyl, heterocyclyl, heteroaryl or heteroaralkyl groups;
- optionally substituted with one or more halogen, perhalomethyl, hydroxy, nitro or cyano;
- Y represents oxygen, sulphur or NR10, where R10 represents hydrogen, C1-12-alkyl, aryl, hydroxyC1-12-alkyl or aralkyl groups or when Y is NR10, R8 and R10 may form a 5 or 6 membered nitrogen containing ring, optionally substituted with one or more C1-6-alkyl;
- n is an integer ranging from 1 to 4 and m is an integer ranging from 0 to 1;
- or a pharmaceutically acceptable salt thereof.
15 more elements
Dependencies are inferred from the claim text.