Výsledky vyhledávání - "Craig S. Harris"

Akademický článek

Novel library synthesis of 3,4-disubstituted pyridin-2(1H)-ones via cleavage of pyridine-2-oxy-7-azabenzotriazole ethers under ionic hydrogenation conditions at room temperature

Autor: Romain Pierre, Anne Brethon, Sylvain A. Jacques, Aurélie Blond, Sandrine Chambon, Sandrine Talano, Catherine Raffin, Branislav Musicki, Claire Bouix-Peter, Loic Tomas, Gilles Ouvry, Rémy Morgentin, Laurent F. Hennequin, Craig S. Harris

Publikováno v: Beilstein Journal of Organic Chemistry, Vol 17, Iss 1, Pp 156-165 (2021)

In our hands, efficient access to the 4-amino-3-carboxamide disubstituted pyridine-2(1H)-one kinase hinge-binder motif proved to be more challenging than anticipated requiring a significant investment in route scouting and optimization. This full pap

Externí odkaz: https://doaj.org/article/2acdd653d9364f4c95c1ad7741ba07ae

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Completion of the impurity profile of lymecycline: Formal identification of impurities E and F

Autor: Stéphan, Billié, Kevin, Reversé, Sandrine, Chambon, Tony, Cachot, Romain, Pierre, Thibaud, Gerfaud, Davide, Longoni, Massimiliano, Gennari, Héloïse, Raynard, Eric, Talbot, Karine, Charras, Didier, Bertin, Marine, Joly-Battaglini, Gerald, Pedrassi, Jean-Guy, Boiteau, Cécile, Cren, Craig S, Harris

Publikováno v: Journal of Pharmaceutical and Biomedical Analysis. 220:114993

Lymecycline is the drug substance (DS) used in the Galderma drug product Tetralysal® capsules with 7 impurities currently described in the pharmacopeia labelled as A-G. In the current monograph, the structural identity of all impurities except E and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be983787b90067548f4a46da18cf48d0
https://doi.org/10.1016/j.jpba.2022.114993

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Self-crosslinking smart hydrogels through direct complexation between benzoxaborole derivatives and diols from hyaluronic acid

Autor: Jean-Guy Boiteau, Jing Jing, Vanina Cosenza, Tamiris Vilas Boas Figueiredo, Isabelle Jeacomine, Thibaud Gerfaud, Rachel Auzély-Velty, Johan Olsson, Craig S. Harris, Yu Ogawa

Publikováno v: Polymer Chemistry
Polymer Chemistry, Royal Society of Chemistry-RSC, 2020, 11, pp.3800-3811. ⟨10.1039/D0PY00308E⟩

International audience; Boronate ester cross-linked hydrogels have emerged as promising injectable scaffolds for biomedical applications given their rapid self-healing ability. For a rational design of such networks, all variables influencing their d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e5a65431f5ee1280e17526ec2e3415a
https://hal.archives-ouvertes.fr/hal-03005698/document

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Boronic acid and diol-containing polymers: how to choose the correct couple to form 'strong' hydrogels at physiological pH

Autor: Jean-Guy Boiteau, Yu Ogawa, Johan Olsson, Raphael Michel, Craig S. Harris, Jing Jing, Thibaud Gerfaud, Rachel Auzély-Velty, Sonia Ortega, Tamiris Vilas Boas Figueiredo, Vanina Cosenza, Alicia Vallet, Isabelle Jeacomine

Publikováno v: Soft Matter
Soft Matter, 2020, 16 (15), pp.3628-3641. ⟨10.1039/D0SM00178C⟩
Soft Matter, Royal Society of Chemistry, 2020, 16 (15), pp.3628-3641. ⟨10.1039/D0SM00178C⟩

International audience; Dynamic covalent hydrogels crosslinked by boronate ester bonds are promising materials for biomedical applications. However, little is known about the impact of the crosslink structure on the mechanical behaviour of the result

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::36022ef36df5405698f25b0d6f8d932a
https://pubmed.ncbi.nlm.nih.gov/32222755

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Route scouting and optimization of a potent sulfoximine-based inverse agonist of RORγt

Autor: Craig S. Harris, Romain Pierre, Rodolphe Vatinel, Jean-Marie Arlabosse, Veronique Parnet, Catherine Raffin, Claire Bouix-Peter, Thibaud Gerfaud, Sebastien Daver, Jean-Guy Boiteau, Branislav Musicki, Guillaume Lafitte, Loïc Tomas, Gilles Ouvry

Publikováno v: Tetrahedron. 74:5974-5986

During our research looking for novel inverse agonists of RORγt, we identified a potent sulfoximine-based modulator as one of our pre-clinical candidates for the topical treatment for psoriasis. Herein, we describe the various routes we evaluated du

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::15c9d3c4ef6fb9803ceb24f387ac4293
https://doi.org/10.1016/j.tet.2018.08.043

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Synthesis and stability evaluation of novel peptidomimetic Caspase-1 inhibitors for topical application

Publikováno v: Tetrahedron
Tetrahedron, Elsevier, 2018, 74 (37), pp.4805-4822. ⟨10.1016/j.tet.2018.07.029⟩
Tetrahedron, 2018, 74 (37), pp.4805-4822. ⟨10.1016/j.tet.2018.07.029⟩

International audience; During our search for topically-active Caspase-1 inhibitors, we identified a novel class of potent in-hibitors based on a 1,3,5-trisubstituted uracil motif equipped with an L-aspartate semi-aldehyde derived warhead. In the lit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fec40dca9ff1ebf6ef20f7e1e77cb56
https://doi.org/10.1016/j.tet.2018.07.029

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Identification of 1,5,7-Triazabicyclododecene and Polystyrene-Supported Superbases as Efficient Hydroxylaminolysis Agents of Sterically Hindered and Epimerizable Esters

Autor: Ghizlane El-Bazbouz, Loïc Tomas, Romain Pierre, Grégoire Mouis, Gilles Ouvry, Frédéric Gaigne, Craig S. Harris

Publikováno v: Synlett. 29:1102-1106

In modern pharmaceutical research, the need for reliable protocols for the preparation of chemical libraries in a controlled manner is quintessential to driving the Design-Make-Test cycle in drug discovery programs. In this letter, we communicate the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6a79430b830f133f02d853374d2688f3
https://doi.org/10.1055/s-0036-1591551

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