Patent
Novel p2x7r antagonists and their use
Michael Boes
- 20 Jan 2012
11
TL;DR: In this article, the authors present an application for P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol 3-ylacetamide compounds.
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Abstract: The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.
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Citations
P2X purinergic receptor ligands: recently patented compounds
TL;DR: The patent literature covering novel drug-like antagonists for each P2X receptor subtype up to December 2009 is described in this review article together with their recent highlights in pharmacology.
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Heterocyclic amide derivatives as p2x7 receptor antagonists
Kurt Hilpert,Francis Hubler,Dorte Renneberg,Simon Stamm +3 more
- 21 Jan 2014
TL;DR: In this article, the authors defined a class of heterocyclic amide derivatives of formula (I), where R1, R2, R3, R4, R5, n, m, p and X are defined in the description, their preparation and their use as pharmaceutically active compounds.
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Indole carboxamide derivatives as p2x7 receptor antagonists
Kurt Hilpert,Francis Hubler,Dorte Renneberg,Simon Stamm +3 more
- 17 Dec 2013
TL;DR: In this article, the indole carboxamide derivatives of formula (I), (I) wherein R1, R 2, R 3, R 4, R5 and R6 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
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Method for treatment of macular degeneration by modulating P2Y12 or P2X7 receptors
Claire H. Mitchell,Alan M. Laties +1 more
- 27 Apr 2012
TL;DR: In this paper, a method for treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the patient.
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Novel quinoline derivatives and their use in neurodegenerative diseases
Srinivasa R. Karra,Yufang Xiao,Jeyaprakashnarayanan Seenisamy,Jayashankaran Jayadevan +3 more
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TL;DR: The present paper relates to quinoline compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P 2X7-related disorders.
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References
Patent
Heteroaryl amide analogues as p2x7 antagonists
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TL;DR: Heteroaryl amide analogues are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals.
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Patent
New p2x7 receptor antagonists and their use
Evans Richard,Eyssade Christine,Ford Rhonan,Barrie Martin,Thompson Toby,Willis Paul +5 more
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TL;DR: In this paper, the authors provide compounds of formula (IA), processes for their preparation, pharmaceutical compositions containing them, and their use in therapy, as well as their application in medical applications.
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Recent progress in the discovery of antagonists acting at P2X7 receptor
TL;DR: The extensive use of high-throughput screening approaches, utilising diverse compound library sources, has lead to the identification of two important lead series (adamantane and benzenamide derivatives) acting on P2X7.
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Novel Biaromatic Compounds, Inhibitors of the P2X7-Receptor
Toby Thompson,Paul AstraZeneca R D Charnwood Willis +1 more
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TL;DR: In this article, the authors defined compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein A represents a group (II), (III), (IV) or (V), and A, Ar2, n, R1, R2, R3, R4 and R5 are as defined in the specification; a process for their preparation; pharmaceutical compositions containing them; and their use in therapy.
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Patent
Substituted phenyl compounds with immunosuppressing activity and pharmaceutical compositions
Mark Furber,Luker Timothy Jon,Mortimore Michael Paul,Philip Thorne,Meghani Premji +4 more
- 22 May 2000
TL;DR: In this article substituted phenyl compounds of general formula (I) are defined in the specification, a process for their preparation, pharmaceutical compositions containing them, and their use in therapy.
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