5-Lipoxygenase inhibitors: a patent evaluation (WO2011161615).
Summary of "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.
Affiliation
Goethe-University Frankfurt, Institute of Pharmaceutical Chemistry, ZAFES/OSF , Max-von-Laue-Str. 9, D-60438 Frankfurt am Main , Germany; proschak@pharmchem.uni-frankfurt.de.
Journal Details
This article was published in the following journal.
Name: Expert opinion on therapeutic patents
ISSN: 1744-7674
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/22697185
- DOI: http://dx.doi.org/10.1517/13543776.2012.694868
Medical and Biotech [MESH] Definitions
5-lipoxygenase-activating Protein Inhibitors
Compounds that bind to and inhibit the action of 5-LIPOXYGENASE-ACTIVATING PROTEINS.
Lipoxygenase Inhibitors
Compounds or agents that combine with lipoxygenase and thereby prevent its substrate-enzyme combination with arachidonic acid and the formation of the eicosanoid products hydroxyeicosatetraenoic acid and various leukotrienes.
Lipoxygenase
An enzyme of the oxidoreductase class that catalyzes reactions between linoleate and other fatty acids and oxygen to form hydroperoxy-fatty acid derivatives. Related enzymes in this class include the ARACHIDONATE LIPOXYGENASES; ARACHIDONATE 5-LIPOXYGENASE; ARACHIDONATE 12-LIPOXYGENASE; and ARACHIDONATE 15-LIPOXYGENASE. EC 1.13.11.12.
Persistent Fetal Circulation Syndrome
A syndrome of persistent PULMONARY HYPERTENSION in the newborn infant (INFANT, NEWBORN) without demonstrable HEART DISEASES. This neonatal condition can be caused by severe pulmonary vasoconstriction (reactive type), hypertrophy of pulmonary arterial muscle (hypertrophic type), or abnormally developed pulmonary arterioles (hypoplastic type). The newborn patient exhibits CYANOSIS and ACIDOSIS due to the persistence of fetal circulatory pattern of right-to-left shunting of blood through a patent ductus arteriosus (DUCTUS ARTERIOSUS, PATENT) and at times a patent foramen ovale (FORAMEN OVALE, PATENT).
Foramen Ovale, Patent
A condition in which the FORAMEN OVALE in the ATRIAL SEPTUM fails to close shortly after birth. This results in abnormal communications between the two upper chambers of the heart. An isolated patent ovale foramen without other structural heart defects is usually of no hemodynamic significance.
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