5-Lipoxygenase inhibitors: a patent evaluation (WO2011161615).
1,5-Diarylpyrazoles are privileged scaffolds used for the development of COX-2 (cyclooxygenase 2) selective inhibitors (coxibs). Derivatives of 1,5-diarylpyrazoles are currently being used as 5-lipoxygenase (5-LO) inhibitors for the treatment of respiratory diseases, inflammatory and autoimmune disorders. The following article, which evaluates this patent application, describes 1,5-arylpyrazoles and their pharmacological ability to inhibit 5-LO. Furthermore, the authors describe how these compounds relate to pyrazole derivatives in terms of their synthesis and how they are used for treating several respiratory diseases including: chronic obstructive pulmonary disease (COPD), bronchial asthma and other disorders. The authors have come to the conclusion that this current patent evaluation is insufficient for the complete evaluation of these compounds. However, this does not diminish the importance of the versatile synthesis of 1,5-pyrazole derivatives and their use in the treatment of inflammatory-related pathologies.
Goethe-University Frankfurt, Institute of Pharmaceutical Chemistry, ZAFES/OSF, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany.
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D000818:Animals; D001094:Arachidonate 5-Lipoxygenase / Q000187:drug effects* / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000201:enzymology; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010330:Patents as Topic; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012140:Respiratory Tract Diseases / Q000188:drug therapy / Q000503:physiopathology
D016859:Lipoxygenase Inhibitors; D011720:Pyrazoles; D001094:Arachidonate 5-Lipoxygenase