Therapeutic modulators of peroxisome proliferator-activated receptors (PPAR): a patent review (2008-present).
BACKGROUND
Peroxisome proliferator-activated receptors (PPAR) are ligand-activated transcription factors belonging to the nuclear receptor superfamily. The three known subtypes PPARα, PPARγ and PPARδ have different tissue distribution and play a key role as regulators of glucose and lipid homeostasis as well as in cell proliferation, differentiation and inflammatory responses. They have gained a lot of interest as pharmaceutical targets over the last years and with the antidiabetic thiazolidindiones (TZDs) and the hypolipidemic fibrates, two classes of drugs had entered the market. Early observations of severe adverse events changed the situation in the recent past.


METHODS
Herein the authors summarize recent (2008-present) patent applications concerning PPAR ligands claimed for the use in metabolic disorders as well as patents indicating new applications for modulators of the PPAR subtypes.


CONCLUSIONS
Looking at the recent patent activity regarding novel compounds, there have not been real innovations. As major applications for therapeutic PPAR ligands cancer therapy, skin-related disorders and systemic anti-inflammatory therapies might arise in the mid-term future. The known PPAR targeting drugs might see a repurposing for novel indications.
Goethe University Frankfurt, Institute of Pharmaceutical Chemistry, Max-von-Laue-Str. 9, Frankfurt, Germany.
Christina
C
Lamers
Manfred
M
Schubert-Zsilavecz
Daniel
D
Merk
D000818:Animals; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D008024:Ligands; D008659:Metabolic Diseases / Q000188:drug therapy / Q000503:physiopathology; D047493:PPAR alpha / Q000187:drug effects* / Q000378:metabolism; D047494:PPAR delta / Q000187:drug effects* / Q000378:metabolism; D047495:PPAR gamma / Q000187:drug effects* / Q000378:metabolism; D010330:Patents as Topic
D008024:Ligands; D047493:PPAR alpha; D047494:PPAR delta; D047495:PPAR gamma