title: Heterocyclic compounds and their uses: a patent evaluation of WO2010151735A2.
abstract: A series of pyrido-pyrimidin-4-ones, incorporating purine/pyrimidine scaffolds, were prepared by a succession of standard reactions and tested for the inhibition of 4 isoforms of the phosphatidylinositol 3-kinase (PI3K) class I, that is, the α, β, δ and γ PI3Ks. Compounds with activity, from the nanomolar to the micromolar, against isoform PI3Kδ were detected, and have been assayed in vivo with the human B cells proliferation assay, stimulated by anti-IgM or IL-4, showing remarkable activity. The patent claims a very promising new class of PI3Kδ inhibitors with selectivity for the δ-class enzymes, involved in a variety of diseases, such as, but not limited to, cancer, autoimmune disease and allergy. The chemotype claimed in the patent is new, and a large chemical diversity was generated by standard chemical processes. The biological activity and selectivity of these enzyme inhibitors seem to be very good.
authors: Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy. andrea.scozzafava@unifi.it
authors: Andrea
authors: A
authors: Scozzafava
authors: Claudiu T
authors: CT
authors: Supuran
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D006571:Heterocyclic Compounds / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D010330:Patents as Topic; D000081082:Phosphoinositide-3 Kinase Inhibitors
chemical_list: D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D000081082:Phosphoinositide-3 Kinase Inhibitors