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US 9,428,452 B2Granted
Compounds
AssigneeGlaxo Group Limited
InventorsVeronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
Life of this patent
Estimating the term…
Abstract
The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ.
Claims39
A compound of formula (Ia), or a pharmaceutically acceptable salt thereof:
- wherein R1 is selected from the group consisting of H, C1-3alkyl, C1-3alkoxy, CF3, and halo;
- R2, R3 and R4 are H;
- R5 is C1-3alkyl;
- R6 is C3-5alkyl or —CH2C3-4cycloalkyl;
- R7 is selected from the group consisting of:
- each R8 is independently selected from the group consisting of halo, C1-6alkyl, C1-6alkoxy, C3-6cycloalkyl, CN, OH, C(O)OH, C(O)OC1-3alkyl and CH2OH;
- R9 is the group —(CHR10)s—(X)t—(CHR10)u—R11;
- each R10 is independently selected from H, CH3, OH and CH2OH;
- X is CH2, NH or O;
- R11 is a heterocycloalkyl or C3-6 cycloalkyl group which may be unsubstituted or substituted with one or more substituents independently selected from the group consisting of CH3, OCH3, OH, CH2OH and halo;
- r is 0, 1 or 2;
- s is 0, 1 or 2;
- t is 0 or 1;
- u is 0, 1 or 2;
- with the proviso that no more than two R10 groups represent CH3, OH or CH2OH.
12 more elements
A compound which is
A compound, or a pharmaceutically acceptable salt thereof, which is selected from the group consisting of:
- N-(2,4-dimethylphenyl)-2-(hydroxymethyl)-N-(2-methylpropyl)-4-(oxan-4-ylmethoxy)benzene-1-sulfonamide;
- N-(2,4-dimethylphenyl)-N-(2-methylpropyl)-4-(piperidin-4-ylmethoxy)benzene-1-sulfonamide;
- N-(2,4-dimethylphenyl)-3-methyl-N-(2-methylpropyl)-4-(oxan-4-ylmethoxy)benzene-1-sulfonamide;
- N-(2,4-dimethylphenyl)-2-methyl-N-(2-methylpropyl)-4-(oxan-4-ylmethoxy)benzene-1-sulfonamide;
- N-(2,4-dimethylphenyl)-3-fluoro-N-(2-methylpropyl)-4-(oxan-4-ylmethoxy)benzene-1-sulfonamide;
- N-(2,4-dimethylphenyl)-N-(2-methylpropyl)-4-(oxolan-3-ylmethoxy)benzene-1-sulfonamide;
- N-(2,4-dimethylphenyl)-N-(2-methylpropyl)-4-(morpholin-4-yl)benzene-1-sulfonamide;
- N-(4-ethylphenyl)-4-{1-hydroxy-2-[(3-methyloxetan-3-yl)amino]ethyl}-N-(2-methylpropyl)benzene-1-sulfonamide;
- and
- N-(4-ethylphenyl)-4-(1-hydroxy-2-morpholinoethyl)-3-(hydroxymethyl)-N-isobutylbenzenesulfonamide.
7 more elements
Dependencies are inferred from the claim text.