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Heterocyclic compounds and their uses: a patent evaluation of WO2010151735A2.

06:00 EDT 26th March 2011 | BioPortfolio

Summary of "Heterocyclic compounds and their uses: a patent evaluation of WO2010151735A2."

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.

Affiliation

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.

Journal Details

This article was published in the following journal.

Name: Expert opinion on therapeutic patents
ISSN: 1744-7674
Pages:

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Medical and Biotech [MESH] Definitions

Heterocyclic compounds that contain two rings that share two non-adjacent atoms in common.

Multiple ring heterocyclic compounds containing two or more rings that share two atoms and one bond in common.

A class of heterocyclic compounds that include four or more fused rings. Both aromatic or non-aromatic ring structures are included in this category.

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