AU2023366352A1 — New inhibitors of phosphatidylinositol 3-kinase

USPTO Abstract

The present invention relates to the prevention and/or treatment of protein tyrosine kinase mediated diseases, in particular phosphatidylinositol 3-kinases (PI3Ks) mediated diseases. PI3Ks are well-known as oncology targets and several inhibitors of PI3Ks have been developed that inhibit multiple class 1A PI3K isoforms. The development of selective inhibitors of PI3K-α may enable sufficient target inhibition while avoiding some toxicity drawbacks known for pan PI3K inhibitors. The inventors found that new specific carbamothioyl-pyrrolidine-carboxamide compounds of formula (I) exhibit an advantageous PI3K inhibitory activity, especially with a high selectivity for the isoform PI3K alpha. In particular, the present invention relates to compounds of formula (I), or a deuterated or tritiated form of the compound of formula (I), and pharmaceutically acceptable salts thereof. It also relates to pharmaceutical composition containing said compound of formula (I) and the compounds of formula (I) for use in the treatment and/or prevention of Protein tyrosine kinase mediated diseases.