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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...
A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.
More than 25% of all ischemic strokes per year are cryptogenic; that is their cause is not determined after an appropriate evaluation. In 1988 it was reported that the incidence of a patent foramen ov...
In this work, 27 novel hybrid derivatives containing diverse substituents with chalcogen atoms (selenium or sulfur) and several active heterocyclic scaffolds have been synthesized. Compounds were test...
The patent landscape, like a garden, can tell you much about its designers and users; their motivations, biases, and general interests. While both patent landscapes and gardens may appear to the casua...
The primary objective is to evaluate if patent foramen ovale (PFO) closure and antiplatelet medical management can reduce the risk of recurrent stroke or transient ischemic attack (TIA) wh...
Closure of Patent Foramen Ovale with the AMPLATZER® PFO OCCLUDER in patients with at least two cryptogenic strokes due to presumed paradoxical embolism through a patent foramen ovale and ...
The purpose of this multi-center, interventional, prospective, post-market study is to collect real world data on patient outcomes and evaluate the procedural success and performance of th...
Ereth et al. showed in 1992, using transesophageal echocardiography, that the implantation of a hip prosthesis may be complicated by intracardiac embolization of various origin. A patent ...
The purpose of the study is to determine the safety and efficacy of ibuprofen, compared with indomethacin, in the treatment for the closure of the patent ductus arteriosus in premature bab...
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).
Ring compounds having atoms other than carbon in their nuclei. (Grant & Hackh's Chemical Dictionary, 5th ed)
Compounds with a five-membered heterocyclic ring with two nitrogens and a keto OXYGEN. Some are inhibitors of TNF-ALPHA production.
A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms.
Compounds based on an 8-membered heterocyclic ring including an oxygen. They can be considered medium ring ethers.
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...