- NOVEL IMIDAZO-PYRAZINE DERIVATIVES
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The invention provides novel imidazo-pyrazine derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, m, n, and R1to R3 are as described herein: formula (I). Further provided are pharmace
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Page/Page column 45; 81-82
(2021/12/31)
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- NOVEL IMIDAZOPYRAZINE DERIVATIVES
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The invention provides novel imidazopyrazine derivatives having the general formula (I), wherein Rx and R3 to R5 are as described herein (formula (I)) or pharmaceutically acceptable salts thereof. Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
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Page/Page column 51-53
(2021/12/31)
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- Novel and selective TLR7 antagonists among the imidazo[1,2- a]pyrazines, Imidazo[1,5- a]quinoxalines, and Pyrazolo[1,5- a]quinoxalines Series
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The Toll-like receptors (TLRs) 7 and 8 play an important role in the immune system activation, and their agonists may therefore serve as promising candidate vaccine adjuvants. However, the chronic immune activation by excessive TLR stimulation is a hallmark of several clinically important infectious and autoimmune diseases, which warrants the search for TLR antagonists. In this study, we have synthesized and characterized a variety of compounds belonging to three heterocyclic chemical series: imidazo[1,2-a]pyrazine, imidazo[1,5-a]quinoxaline, and pyrazolo[1,5-a]quinoxaline. These compounds have been tested for their TLR7 or TLR8 agonistic and antagonistic activities. Several of them are shown to be selective TLR7 antagonists without any TLR7 or TLR8 agonistic activity. The selectivity was confirmed by a comparative ligand-docking study in TLR7 antagonist pocket. Two compounds of the pyrazolo[1,5-a]quinoxaline series (10a and 10b) are potent selective TLR7 antagonists and may be considered as promising starting points for the development of new therapeutic agents.
- Bou Karroum, Nour,Moarbess, Georges,Guichou, Jean-Fran?ois,Bonnet, Pierre-Antoine,Patinote, Cindy,Bouharoun-Tayoun, Hasnaa,Chamat, Soulaima,Cuq, Pierre,Diab-Assaf, Mona,Kassab, Issam,Deleuze-Masquefa, Carine
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p. 7015 - 7031
(2019/08/20)
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- FUSED HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
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Fused heteroaryl derivative compounds which are antagonists of orexin receptors are provided. The compounds can be used in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. Also provided is a composition which comprises the compound can be use to prevent or treat such diseases in which orexin receptors are involved.
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Page/Page column 79
(2016/07/27)
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- IMIDAZOPYRAZINES FOR USE AS MPS-1 AND TKK INHIBITORS IN THE TREATMENT HYPERPROLIFERATIVE DISORDERS
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The present invention relates to substituted imidazopyrazine compounds of general formula (I) : in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
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Page/Page column 40
(2012/06/30)
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