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US 6,555,577 B1Granted
Compounds, their preparation and use
AssigneeNovo Nordisk A/S
InventorsJohn Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
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).
Claims50
A compound of formula (I)
- wherein
- A is aryl, wherein A is optionally substituted with one or more substituents selected from hydroxy, halogen, perhalomethyl, perhalomethoxy, acyl, cyano, amino, C1-6-alkylamino, C1-6-dialkylamino, methylenedioxy, aralkenyl, aralkynyl, heteroaryloxy, heteroaralkoxy, aralkyl, heteroaralkyl, arylamino, or
- A is optionally substituted with C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl each of which is optionally substituted with one or more substituents selected from C1-6-alkoxycarbonyl or carboxy, or
- A is optionally substituted with C1-6-alkoxy, C1-6-alkylthio or C2-6-alkenyloxy each of which is optionally substituted with one or more halogens, or
- A is optionally substituted with aryloxy, arylthio or aralkoxy each of which is optionally substituted with one or more substituents selected from C1-6-alkoxy, nitro, carboxy or C1-6-alkoxycarbonyl;
- and
- X1 and X2 independently are hydrogen, aryl or heteroaryl each of which is optionally substituted with one or more substituents selected from hydroxy, aryloxy, arylthio, aralkoxy, heteroaryloxy, aralkoxy, C1-6-alkoxy, C1-6-alkylthio, halogen, perhalomethyl, perhalomethoxy, acyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cyano, amino, C1-6-alkylamino, C1-6-dialkylamino, arylamino or methylenedioxy, or aryl or heteroaryl each of which is optionally substituted with one or more substituents selected from C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl each of which is optionally substituted with hydroxy;
- or
- Y is hydrogen, or Y is C1-12-alkyl, C2-12-alkenyl, C2-12-alkynyl, C4-12-alkenynyl, aralkyl or heteroaralkyl, each of which is optionally substituted with one or more substituents selected from halogen, C1-6-alkyl, perhalomethyl, hydroxy, aryl, heteroaryl, carboxy or amino;
- and
- Z is hydrogen, halogen, hydroxy, or Z is C1-6-alkyl or C1-6-alkoxy, each of which is optionally substituted with one or more substituents selected from halogen, hydroxy, carboxy, amino, cyano or C1-6-alkoxy;
- and
- Q is O, S or NR6, wherein R6 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C4-6-alkenynyl, aralkyl, heteroaralkyl and wherein R6 is optionally substituted with one or more substituents selected from halogen, hydroxy, C1-6-alkoxy, amino or carboxy;
- and
- Ar is arylene, which can be optionally substituted with one or more substituents selected from C1-6-alkyl, aryl or C1-6-alkoxy each of which can be optionally substituted with halogen, hydroxy, carboxy, cyano or-heterocyclyl;
- and
- R1 is hydrogen, hydroxy or halogen;
- or R1 forms a bond together with R2;
- and
- R2 is hydrogen or C1-6-alkyl;
- or R2 forms a bond together with R1;
- and
- R3 is hydrogen, or R3 is C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C4-6-alkenynyl, aryl, aralkyl, C1-6-alkoxyC1-6alkyl, acyl, heterocyclyl, heteroaryl or heteroaralkyl each of which is optionally substituted with one or more substituents selected from halogen, perhalomethyl, hydroxy or cyano;
- and
- R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C4-6-alkenynyl or aryl;
- and
- n is an integer ranging from 0 to 3;
- and
- m is an integer ranging from 0 to 1;
- or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or any tautomeric forms, stereoisomers, mixture of stereoisomers including a racemic mixture, or polymorphs,
- provided that when m and n are both 0, X1, X2, Y, Z, R1, R2, R3 and R4 do not all represent H.
28 more elements
Dependencies are inferred from the claim text.