424 research outputs found
Multifunctional Drugs: New challenging chimeras in medicinal chemistry and drug discovery
No full textNovel adenosine 5'-triphosphate-sensitive potassium channel ligands: a patent overview (2005 - 2010)
No full textIntroduction: ATP-sensitive potassium channels are important metabolic regulators that link cellular metabolism to excitability. Their wide distribution in various tissues and organs makes them significant and topical targets in a large number of diseases.
Areas covered: This review summarizes the current understanding of the molecular biology and pharmacology of KATP channels, and the pathological states that result from aberrant expression or function of these proteins. In particular, relevant research, patents and patent applications of the past 5 years are discussed.
Expert opinion: The tissue-specific KATP channel modulation reflects an early discovery stage in drug design. The wide distribution of KATP channels lets us consider them as valid targets for several pathologies, but on other hand the ubiquitous nature is a relevant drawback in developing an effective therapy because of the onset of side effects related to the lack of selectivity. On this basis, further investigations on both the structures and the localization of each receptor subtype should be carried out either exploring the structure-activity relationship of the already existing KATP ligands or developing new selective fluorescent probes. To date, this research area still strives to design new tissue-targeted ligands that could pave the way to the development of innovative and effective drugs for clinical use
Spiro-heterocyclic benzopyrane derivatives: new activators of mito- KATP channels as potential cardioprotective agents
No full text
New Synthetic Methodology for Drug-like Molecules
No full textThe field of synthetic methodology plays a pivotal role in the quest for safe and effective drugs [...]
2-OXO-1,2-DIHYDROPYRIDINE-3-CARBOXAMIDE COMPOUNDS AND THEIR USE AS INHIBITORS OF PDK1 (US Patent App. 15/735,468, 2018)
No full textThe present invention concern a 2-oxo-1,2-dihydropyridine-3-carboxamide compound of Formula (I) and new 2-oxo-1,2-dihydropyridine-3-carboxamide compounds of Formula (II) in the treatment of pathologies which require an inhibitor of PDK1 enzyme such as diabetes, neurodegenerative diseases such as Alzheimer's and Prion Diseases, and tumours such as breast, and pancreatic cancers and glioblastoma, particularly glioblastoma
2-OXO-1,2-DIHYDROPYRIDINE-3-CARBOXAMIDE COMPOUNDS AND THEIR USE AS INHIBITORS OF PDK1 (US Patent App. 15/735,468, 2018)
No full textThe present invention concern a 2-oxo-1,2-dihydropyridine-3-carboxamide compound of Formula (I) and new 2-oxo-1,2-dihydropyridine-3-carboxamide compounds of Formula (II) in the treatment of pathologies which require an inhibitor of PDK1 enzyme such as diabetes, neurodegenerative diseases such as Alzheimer's and Prion Diseases, and tumours such as breast, and pancreatic cancers and glioblastoma, particularly glioblastoma
COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DI PDK1.
No full textThe invention concerns 2-oxo-1,2-dihydropyridine-3-carboxamide compounds
10 and their use as inhibitors and/or modulators of PDK1
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