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US 12,390,461 B2Granted
Modulators of RAR-related orphan receptors (RORs)
Assignee11949098 Canada Inc.
InventorsAhmed Fouda, Jean Tchervenkov, Steven Paraskevas, Sarita Negi
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Abstract
The invention encompasses the novel class of compounds represented by the Formula (I), (II), (III) and (IV) below, which are modulators of RORγt: The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing autoimmune diseases and antibody mediated rejection in a patient in need thereof.
Claims14
A pharmaceutical compound selected from the group consisting of:
- N-(3-(4-benzylpiperazine-1-carbonyl)-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl)-2-fluorobenzamide;
- N-(3-(benzylcarbamoyl)-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)-5-chloro-2-(methylthio)pyrimidine-4-carboxamide;
- N-(6-ethyl-3-{[(2-methylphenyl)amino]carbonyl-4,5,6,7-tetrahydro-1-benzothien-2-yl)-1-methyl-1H-pyrazole-5-carboxamide;
- N-{6-tert-butyl-3-[(4-methyl-1-piperazinyl)carbonyl]-4,5,6,7-tetrahydro-1-benzothien-2-yl}-2-fluorobenzamide;
- 2-fluoro-N-{6-methyl-3-[(4-methyl-1-piperazinyl)carbonyl]-4,5,6,7-tetrahydro-1-benzothien-2-yl}benzamide;
- N-benzyl-2-[(trifluoroacetyl) amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide;
- N-benzyl-2-({[(4-methyl-2-pyrimidinyl)thio]acetyl}amino)-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide;
- N-benzyl-2-[(1-piperidinylacetyl) amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide;
- N-benzyl-2-{[(4-methyl-1-piperazinyl) acetyl]amino}-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide;
- N-benzyl-2-{[(4-methyl-1-piperidinyl) acetyl]amino}-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide;
- N-(3-(2-methylpyrrolidine-1-carbonyl)-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl)nicotinamide;
- N-(3-((2R,4R)-2,4-dimethylpiperidine-1-carbonyl)-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)nicotinamide;
- N-(3-(((1r,4r)-4-hydroxycyclohexyl)carbamoyl)-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)nicotinamide;
- N-(3-(3-ethylpyrrolidine-1-carbonyl)-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl)nicotinamide;
- N-benzyl-2-(2-((1-methyl-1H-imidazol-2-yl)thio)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide;
- N-(3-(3-(hydroxymethyl) pyrrolidine-1-carbonyl)-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)nicotinamide;
- N-(6,6-dimethyl-3-(morpholine-4-carbonyl)-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl) pyrazine-2-carboxamide;
- N-(3-(((1-methyl-1H-1,2,4-triazol-3-yl)methyl) carbamoyl)-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)nicotinamide;
- (S)-N-(3-((1-cyanoethyl) carbamoyl)-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl)nicotinamide;
- and
- N-(3-((piperidin-4-ylmethyl) carbamoyl)-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl)nicotinamide.
18 more elements
Dependencies are inferred from the claim text.