Competitive PPAR-gamma antagonists
AssigneeFraunhofer-Gesellschaft zur Föderung der angewandten Forschung e.V.
InventorsTilo Knape, Andreas Von Knethen, Michael John Parnham, Manfred Schubert-Zsilavecz, Mario Wurglics, Daniel Flesch
Life of this patent
Estimating the term…
Abstract
The present invention pertains to a new compound E)-2-(5-((4-methoxy-2-(trifluoromethyl)quinolin-6-yl)methoxy)-2-((4-(trifluoromethyl) benzyl)oxy)-benzylidene) hexanoic acid (MTTB), and its derivatives. The compounds of the invention are useful as selective peroxisome proliferator-activated receptor gamma (PPARγ) antagonists and are indicated for the use in the treatment of immune related diseases such as systemic inflammation, sepsis and septic shock.
Claims15
A compound of the formula (I), or a stereoisomer, or salt thereof:
- wherein
- R1 is selected from a non-substituted, monosubstituted or polysubstituted aryl or heteroaryl residue,
- R2 is a radical of the formula (III),
- wherein
- X and Z are independently selected from C or N,
- R9 to R12 are independently selected from H, hydroxyl, a non-substituted, monosubstituted or polysubstituted C1-C18-alkyl, wherein the alkyl can be straight, branched or cyclic, alkenyl, trifluormethyl, a non-substituted, monosubstituted or polysubstituted aryl or heteroaryl residue, a non-substituted, monosubstituted or polysubstituted benzyl group, an acyl group, or a branched or heteroatom- or aryl-substituted acyl group, an alkoxy substituent, the alkyl group thereof is branched, non-branched or cyclic, an alkyl group bound through a sulfur atom, or a sulfonyl group, or a nitrogen substituent, or fluoro, chloro, bromo, iodo, —CN or a hetero substituent, if X is N then R11 is absent, and if Z is N then R12 is absent;
- and
- R1 and R2 are different, and
- R3 is a non-substituted, monosubstituted or polysubstituted C1-C10-alkyl, wherein the alkyl can be straight, branched or cyclic.
Dependencies are inferred from the claim text.