An optimization effort was undertaken within a series of piperidinylaminopyrrolo[1,2,-b]pyridazine-3-carboxamide JAK1/3 inhibitors with the aim of improving their selectivity against ROCK1 to avoid off target cardiovascular effects. The synthesis and structure activity relationship (SAR) is described. This effort led to the identification of a series of potent compounds with greatly improved ROCK1 selectivity.

Janus kinase 1/3 (JAK1/3) inhibitors: Improving selectivity against Rho kinase 1 (ROCK1) in a series of piperidinylaminopyrrolo[1,2-b]pyridazine-3-carboxamides

255th National Meeting (2018)

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