- Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists
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A high-throughput screen against Inventiva's compound library using a Gal4/RORγ-LBD luciferase reporter gene assay led to the discovery of a new series of quinoline sulphonamides as RORγ inhibitors, eventually giving rise to a lead compound having an inte
- Amaudrut, Jér?me,Argiriadi, Maria A.,Barth, Martine,Breinlinger, Eric C.,Bressac, Didier,Broqua, Pierre,Calderwood, David J.,Chatar, Mohamed,Cusack, Kevin P.,Gauld, Stephen B.,Jacquet, Sébastien,Kamath, Rajesh V.,Kort, Michael E.,Lepais, Valérie,Luccarini, Jean-Michel,Masson, Philippe,Montalbetti, Christian,Mounier, Laurent,Potin, Dominique,Poupardin, Olivia,Rouaud, Sylvie,Spitzer, Luc,Wallace, Craig D.
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- Benzenesulfonamide derivatives as bradykinin antagonists
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PCT No. PCT/FR96/01262 Sec. 371 Date Apr. 7, 1997 Sec. 102(e) Date Apr. 7, 1997 PCT Filed Aug. 7, 1996 PCT Pub. No. WO97/07115 PCT Pub. Date Feb. 27, 1997The present invention relates to compounds selected from the group consisting of the compounds of formula (I): X is a halogen atom, A is -CH2-, -CH(OH)-, -CH(NH-COCH3)- or S, R is H, CO2H, CO2-B-R1 or CO-N(R2)-B-R1, B is linear, branched or cyclic C1-C10-alkylene, R1 is H, CH2OH, CH2-O-CH3, CH2-NR3R4 or phenyl, R2 is H or C1-C4-alkyl, R3 is H or linear, branched or cyclic C1-C10-alkyl, R4 is H or linear or branched C1-C10-alkyl, it being possible for NR3R4 to be a saturated heterocyclic radical having from 5 to 8 ring members and containing at least one nitrogen atom, and the carbon carrying the substituent R, when Q is saturated, can be of indeterminate (R,S) configuration or of determinate (R) or (S) configuration; and their addition salts. It further relates to their use in therapeutics, especially for pathological conditions involving bradykinin.
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