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US 2004/0171654 A1Published application
Aryl sulfonamides
AssigneeChemoCentryx, Inc.
InventorsSolomon Ugashe, Zheng Wei, J. J. Wright, Andrew Pennell
Life of this patent
Estimating the term…
Abstract
Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
Claims85
A compound of the formula (I), or a salt thereof:
- 251
- where
- X represents from 1 to 4 substituents independently selected from the group consisting of halogen, —CN, —NO2, —OH, —OR1, —C(O)R1, —CO2R′, —O(CO)R1, —C(O)NR1R2, —OC(O)NR1R2, —SR1, —SOR1, —SO2R1, —SO2NR1R2, —NR1R2, —NR1C(O)R2, —NR1C(O)2R2, —NR1SO2R2, —NR1(CO)NR2R3, unsubstituted or substituted C1-8 alkyl, unsubstituted or substituted C2-8 alkenyl, unsubstituted or substituted C2-8 alkynyl, unsubstituted or substituted C3-8 cycloalkyl, unsubstituted or substituted C6-10 aryl, unsubstituted or substituted 5- to 10-membered heteroaryl, and unsubstituted or substituted 3- to 10-membered heterocyclyl;
- R1, R2 and R3 are each independently selected from the group consisting of hydrogen, unsubstituted or substituted C1-6 haloalkyl, unsubstituted or substituted C1-6 alkyl, unsubstituted or substituted C3-6 cycloalkyl, unsubstituted or substituted C2-6 alkenyl, unsubstituted or substituted C2-6 alkynyl, unsubstituted or substituted C6-10 aryl, unsubstituted or substituted 5- to 10-membered heteroaryl, unsubstituted or substituted aryl-C1-4 alkyl, unsubstituted or substituted aryl-C1-4 alkyl, and unsubstituted or substituted aryloxy-C1-4 alkyl;
- or two of R1, R2 and R3 together with the atom(s) to which they are attached, may form an unsubstituted or substituted 5-, 6- or 7-membered ring;
- Y represents from 1 to 3 substituents, each independently selected from the group consisting of halogen, —CN, —NO2, —OH, —OR4, —C(O)R4, —CO2R4, —SR4, —SOR4, —SO2R4, and unsubstituted or substituted C1-4 alkyl;
- R4 is selected from the group consisting of hydrogen, unsubstituted or substituted C1-6 haloalkyl, unsubstituted or substituted C1-6 alkyl, unsubstituted or substituted C3-6 cycloalkyl, unsubstituted or substituted C2-6 alkenyl, and unsubstituted or substituted C2-6 alkynyl;
- L is —C(O)—, —S—, —SO— or —S(O)2—;
- and
- Z represents either unsubstituted or substituted monocyclic or bicyclic C5-10 heteroaryl or unsubstituted or substituted monocyclic or bicyclic C3-10 heterocyclyl,
- with the proviso that when X is methyl, then Z is not 2-thiophene, 2-(3-hydroxy-1H-indole) or 3-(1-methylpyridinium).
8 more elements
Dependencies are inferred from the claim text.