Discovery of a novel series of selective macrocyclic PKCTheta inhibitors.

Autor: Crosignani S; Galderma SA, Av. d'Ouchy 4, 1006 Lausanne, Switzerland. Electronic address: stefano.crosignani@gmail.com., Campos S; Pharmaron Discovery & Early Development, West Hill Innovation Park, Hertford Road, Hoddesdon, Hertfordshire EN11 9FH, UK., Bouix-Peter C; Galderma SA, Av. d'Ouchy 4, 1006 Lausanne, Switzerland., Harris C; Galderma SA, Av. d'Ouchy 4, 1006 Lausanne, Switzerland., Talbot E; Pharmaron Discovery & Early Development, West Hill Innovation Park, Hertford Road, Hoddesdon, Hertfordshire EN11 9FH, UK., Hu H; Pharmaron Discovery & Early Development, West Hill Innovation Park, Hertford Road, Hoddesdon, Hertfordshire EN11 9FH, UK., Wang S; Pharmaron Discovery & Early Development, West Hill Innovation Park, Hertford Road, Hoddesdon, Hertfordshire EN11 9FH, UK., Maclean J; Pharmaron Discovery & Early Development, West Hill Innovation Park, Hertford Road, Hoddesdon, Hertfordshire EN11 9FH, UK., Zanelli U; Galderma SA, Av. d'Ouchy 4, 1006 Lausanne, Switzerland., Taylor S; Pharmaron Discovery & Early Development, West Hill Innovation Park, Hertford Road, Hoddesdon, Hertfordshire EN11 9FH, UK., Foote K; Pharmaron Discovery & Early Development, West Hill Innovation Park, Hertford Road, Hoddesdon, Hertfordshire EN11 9FH, UK., Hacini-Rachinel F; Galderma SA, Av. d'Ouchy 4, 1006 Lausanne, Switzerland., Nicodeme E; Galderma SA, Av. d'Ouchy 4, 1006 Lausanne, Switzerland., Julia V; Galderma SA, Av. d'Ouchy 4, 1006 Lausanne, Switzerland.

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2024 Mar 01; Vol. 100, pp. 129630. Date of Electronic Publication: 2024 Feb 01.

Rational design of a JAK1-selective siRNA inhibitor for the modulation of autoimmunity in the skin.

Autor: Tang Q; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA.; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Fakih HH; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Zain Ui Abideen M; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Hildebrand SR; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Afshari K; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Gross KY; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Sousa J; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Maebius AS; Program in Molecular Medicine, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Bartholdy C; LEO Pharma A/S, Industriparken 55, 2750, Ballerup, Denmark., Søgaard PP; LEO Pharma A/S, Industriparken 55, 2750, Ballerup, Denmark., Jackerott M; LEO Pharma A/S, Industriparken 55, 2750, Ballerup, Denmark., Hariharan V; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Summers A; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Fan X; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Okamura K; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Monopoli KR; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA.; Bioinformatics and Computational Biology Program, Worcester Polytechnic Institute, Worcester, MA, 01609, USA., Cooper DA; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA.; Program in Molecular Medicine, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Echeverria D; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Bramato B; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., McHugh N; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Furgal RC; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Dresser K; Department of Pathology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Winter SJ; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Biscans A; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Chuprin J; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Haddadi NS; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Sherman S; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Yıldız-Altay Ü; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Rashighi M; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Richmond JM; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA., Bouix-Peter C; Aldena Therapeutics, London, E1 6RA, UK., Blanchard C; Aldena Therapeutics, London, E1 6RA, UK., Clauss A; LEO Pharma A/S, Industriparken 55, 2750, Ballerup, Denmark., Alterman JF; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA. Julia.Alterman@umassmed.edu., Khvorova A; RNA Therapeutics Institute, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA. Anastasia.Khvorova@umassmed.edu.; Program in Molecular Medicine, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA. Anastasia.Khvorova@umassmed.edu., Harris JE; Department of Dermatology, University of Massachusetts Chan Medical School, Worcester, MA, 01605, USA. John.Harris@umassmed.edu.

Publikováno v: Nature communications [Nat Commun] 2023 Nov 04; Vol. 14 (1), pp. 7099. Date of Electronic Publication: 2023 Nov 04.

1092 Topical delivery of siRNA therapeutics into the skin using STAR particles

Autor: Ul Abideen, M. Zain, Tang, Q., Fakih, H., Gross, K., Furgal, R., Blanchard, C., Bouix-peter, C., Portal, T., Khvorova, A., Harris, J.E., Alterman, J.

Publikováno v: In Journal of Investigative Dermatology May 2023 143(5) Supplement:S187-S187

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

Autor: Pierre R; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland., Brethon A; Edelris, 60, Avenue Rockefeller, Bioparc, Bioserra 1 Building, 69008 Lyon, France., Jacques SA; Edelris, 60, Avenue Rockefeller, Bioparc, Bioserra 1 Building, 69008 Lyon, France., Blond A; Edelris, 60, Avenue Rockefeller, Bioparc, Bioserra 1 Building, 69008 Lyon, France., Chambon S; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland., Talano S; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland., Raffin C; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland., Musicki B; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland., Bouix-Peter C; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland., Tomas L; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland., Ouvry G; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland., Morgentin R; Edelris, 60, Avenue Rockefeller, Bioparc, Bioserra 1 Building, 69008 Lyon, France., Hennequin LF; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland., Harris CS; Galderma SA, Rue d'Entre-deux-Villes 10, 1814 Vevey, Switzerland.

Publikováno v: Beilstein journal of organic chemistry [Beilstein J Org Chem] 2021 Jan 18; Vol. 17, pp. 156-165. Date of Electronic Publication: 2021 Jan 18 (Print Publication: 2021).