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Tytuł:
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A patent review of adenosine A 2B receptor antagonists (2016-present).
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Autorzy:
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Francucci B; School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy.
Dal Ben D; School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy.
Lambertucci C; School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy.
Spinaci A; School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy.
Volpini R; School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy.
Marucci G; School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy.
Buccioni M; School of Pharmacy, Medicinal Chemistry Unit, University of Camerino, Camerino, Italy.
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Źródło:
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Expert opinion on therapeutic patents [Expert Opin Ther Pat] 2022 Jun; Vol. 32 (6), pp. 689-712. Date of Electronic Publication: 2022 Apr 07.
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Typ publikacji:
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Journal Article
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Język:
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English
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Imprint Name(s):
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Publication: London : Informa Healthcare
Original Publication: London : Ashley Pub. Ltd., c1994-
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MeSH Terms:
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Diabetes Mellitus, Type 2*/drug therapy
Receptor, Adenosine A2B*/chemistry
Receptor, Adenosine A2B*/physiology
Adenosine/pharmacology ; Adenosine A2 Receptor Antagonists/pharmacology ; Adenosine A2 Receptor Antagonists/therapeutic use ; Humans ; Patents as Topic ; Signal Transduction
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Contributed Indexing:
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Keywords: A2A/A2BAR antagonists; A2BAR antagonists; cancer; inflammatory pathologies
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Substance Nomenclature:
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0 (Adenosine A2 Receptor Antagonists)
0 (Receptor, Adenosine A2B)
K72T3FS567 (Adenosine)
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Entry Date(s):
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Date Created: 20220407 Date Completed: 20220525 Latest Revision: 20220525
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Update Code:
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20240105
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DOI:
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10.1080/13543776.2022.2057222
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PMID:
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35387537
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Introduction: A 2B adenosine receptor (A 2B AR) plays a crucial role in pathophysiologic conditions associated with high adenosine release, typical of airway inflammatory pathologies, gastrointestinal disorders, cancer, asthma, type 2 diabetes, and atherosclerosis. In some pathologies, simultaneous inactivation of A 2A and A 2B ARs is desirable to have a synergism of action that leads to a greater efficacy of the pharmacological treatment and less side effects due to the dose of drug administered. In this context, it is strongly required to identify molecules capable of selectively antagonizing A 2B AR or A 2A /A 2B ARs.
Areas Covered: The review provides a summary of patents, published from 2016 to present, on chemicals and their clinical use. In this paper, information on the biological activity of representative structures of recently developed A 2B or A 2A /A 2B receptor ligands is reported.
Expert Opinion: Among the four P1 receptors, A 2B AR is the most inscrutable and the least studied until a few years ago, but its involvement in various inflammatory pathologies has recently made it a pharmacological target of high interest. Many efforts by the academy and pharmaceutical companies have been made to discover potential A 2B AR and A 2A /A 2B ARs drugs. Although several compounds have been synthesized only a few molecules have entered clinical trials.