Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
Saved in:
| Title: | Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist. |
|---|---|
| Authors: | Fauber BP, René O, Deng Y, DeVoss J, Eidenschenk C, Everett C, Ganguli A; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Gobbi A, Hawkins J; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Johnson AR, La H, Lesch J, Lockey P; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Norman M; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Ouyang W, Summerhill S; ⊥Discovery Biology, Argenta, Units 7-9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, U.K., Wong H |
| Source: | Journal of medicinal chemistry [J Med Chem] 2015 Jul 09; Vol. 58 (13), pp. 5308-22. Date of Electronic Publication: 2015 Jun 23. |
| Publication Type: | Journal Article; Research Support, N.I.H., Extramural |
| Journal Info: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE |
| Database: | MEDLINE Ultimate |
| ISSN: | 1520-4804 |
|---|---|
| DOI: | 10.1021/acs.jmedchem.5b00597 |
