Isothiazole and isoxazole compounds as transforming growth...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C544S353000, C544S354000, C544S355000, C544S356000

Reexamination Certificate

active

07030125

ABSTRACT:
Novel isothiazole and isoxazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-β signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer, and fibrotic diseases.

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J. Singh, et al., “Successful Shape-Based Virtual Screening: The Discovery of a Potent Inhibitor of the Type I TGFβ Receptor Kinase (TβRI)”,Bioorganic&Medicinal Chemistry Letters, 13 (2003) 4355-4359.

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