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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.
Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy firstname.lastname@example.org.
This article was published in the following journal.
Name: Expert opinion on therapeutic patents
N-Heterocyclic olefins (NHOs), the alkylidene derivatives of N-heterocyclic carbenes (NHCs), have recently emerged as a new family of promising organocatalysts with strong nucleophilicity and Brønste...
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This study proposes a different angle to social network analysis that evaluates patent value and explores its influencing factors using the network centrality and network position. This study utilizes...
Patent urachus (PU) is due to an incomplete obliteration of the urachus, whereas patent omphalomesenteric duct (POMD) is due to an incomplete obliteration of the vitelline duct. These anomalies are ve...
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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.
Aniline compounds that contain two amino groups. They are used as a precursor in the synthesis of HETEROCYCLIC COMPOUNDS and POLYMERS. p-Phenylenediamine is used in the manufacture of HAIR DYES and is an ALLERGEN.
A syndrome of persistent PULMONARY HYPERTENSION in the newborn infant (INFANT, NEWBORN) without demonstrable HEART DISEASES. This neonatal condition can be caused by severe pulmonary vasoconstriction (reactive type), hypertrophy of pulmonary arterial muscle (hypertrophic type), or abnormally developed pulmonary arterioles (hypoplastic type). The newborn patient exhibits CYANOSIS and ACIDOSIS due to the persistence of fetal circulatory pattern of right-to-left shunting of blood through a patent ductus arteriosus (DUCTUS ARTERIOSUS, PATENT) and at times a patent foramen ovale (FORAMEN OVALE, PATENT).
An assay is an analytic procedure for qualitatively assessing or quantitatively measuring the presence or amount or the functional activity of a target entity. This can be a drug or biochemical substance or a cell in an organism or organic sample. ...
Cancer is not just one disease but many diseases. There are more than 100 different types of cancer. Most cancers are named for the organ or type of cell in which they start - for example, cancer that begins in the colon is called colon cancer; cancer th...