Journal of Medicinal Chemistry
Article
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The following patent applications describing TYK2 inhibitors were
also published: (a) Buchmann, B.; Eis, K., Bothe, U.; Bonin, A.;
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(42) Our compounds were found to be consistently much less active
against the JAK3 enzyme than TYK2 (>50-fold difference between the
JAK3 Ki and TYK2 Ki). JAK3 inhibitory activities were not reported
for the majority of compounds described in this work except for
compound 3 (Figure 1) and compounds 35−37 (Table 3). Recent
reports also suggested that JAK3 inhibition is not sufficient in blocking
effects of type I cytokines and that JAK1 is the dominant kinase:
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G.; Behrmann, I.; Zerwes, H.-G. JAK1 has a dominant role over JAK3
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J. Immunol., submitted.
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