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US 2008/0293785 A1Published application
Substituted benzothiazole kinase inhibitors
OwnerPeter J. Connolly, Stuart L. Emanuel +2inventors
InventorsPeter J. Connolly, Stuart L. Emanuel, Shenlin Huang, Ignatius J. Turchi
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Abstract
The present invention is directed to substituted benzothiazole compounds of formula (I): and forms thereof, their synthesis and use for treating a chronic or acute protein kinase mediated disease, disorder or condition.
Claims27
A compound of formula (I)
- and forms thereof, wherein
- R1 is hydrogen or is selected from C1-6alkyl, C1-6alkoxy, amino, halogen, cyano, amino-sulfonyl, C1-4alkyl-amino-sulfonyl, halo-C1-4alkyl or halo-C1-4alkoxy;
- R2 is hydrogen or is selected from aryl, heteroaryl, heterocyclyl or C3-12cycloalkyl optionally substituted with one or two substituents selected from C1-6alkyl, C1-6alkoxy or halogen;
- R3 is hydrogen or is C1-4alkyl;
- X is selected from carbonyl, amino-carbonyl, oxy-carbonyl or sulfonyl;
- and
- R4 is selected from a C1-4alkyl, aryl, aryl-C1-4alkyl, heteroaryl, heteroaryl-C1-4alkyl, heterocyclyl, heterocyclyl-C1-4alkyl, C3-12cycloalkyl or C3-12cycloalkyl-C1-4alkyl optionally substituted on aryl, heteroaryl, heterocyclyl or C3-12cycloalkyl with one, two or three substituents selected from C1-6alkyl, C1-6alkenyl, C1-6alkynyl, C1-6alkoxy, C1-6alkyl-carbonyl, C1-6alkoxy-carbonyl, amino, halogen, cyano, nitro, amino-sulfonyl, halo-C1-4alkyl, halo-C1-4alkoxy, aryl, heteroaryl, heterocyclyl or C3-12cycloalkyl.
4 more elements
An intermediate compound of Formula (Ia):
- wherein
- R1 is hydrogen or is selected from C1-6alkyl, C1-6alkoxy, amino, halogen, cyano, amino-sulfonyl, C1-4alkyl-amino-sulfonyl, halo-C1-4alkyl or halo-C1-4alkoxy;
- and,
- R2 is hydrogen or is selected from aryl, heteroaryl, heterocyclyl or C3-12cycloalkyl optionally substituted with one or two substituents selected from C1-6alkyl, C1-6alkoxy or halogen.
1 more element
An intermediate compound selected from the group consisting of:
- N2-phenyl-benzothiazole-2,4-diamine,
- N2-(4-methoxy-phenyl)-benzothiazole-2,4-diamine,
- 4-(4-amino-benzothiazol-2-ylamino)-benzenesulfonamide, and
- N2-p-tolyl-benzothiazole-2,4-diamine.
1 more element
Dependencies are inferred from the claim text.