Development of the telescoped flow Pd-catalyzed aerobic alcohol oxidation/reductive amination sequence in the synthesis of new phosphatidylinositide 3-kinase inhibitor (CPL302415).

Herein, we describe a two-step sequential flow synthesis: Pd-catalyzed aerobic oxidation to an aldehyde 2, which is then converted by reductive amination in H-Cube® PRO into CPL302415 (3). CPL302415 is our new PI3Kδ inhibitor, which is now under evaluation for the treatment of systemic lupus erythematosus. The process was optimized using the DoE approach and generalized to other biologically active derivatives of CPL302415.

Generation of red light with intense photoluminescence assisted by Forster resonance energy transfer from Znq and DCM thin films.

In this work, a novel experimental investigation of photoluminescence properties of Znq thin films co-doped with different concentrations of DCM were performed. The thin films were successfully deposited on glass substrates with different compositions, under high vacuum, by using the vacuum evaporation technique. For all compositions, the photoluminescence was measured at room temperature and also at low temperature in a wide range from 77 to 300 K with a step of 25 K in a high vacuum.

Discovery and development of CPL207280 as new GPR40/FFA1 agonist.

Due to a unique mechanism that limits the possibility of hypoglycemia, the free fatty acid receptor (FFA1) is an attractive target for the treatment of type 2 diabetes. So far, however, none of the promising agonists have been able to enter the market. The most advanced clinical candidate, TAK-875, was withdrawn from phase III clinical trials due to liver safety issues.

Novel pegylated liposomal formulation of docetaxel with 3-n-pentadecylphenol derivative for cancer therapy.

The taxanes are commonly used in the treatment of many types of cancer. The disadvantages of using taxanes in therapy are their low solubility in water, the toxicity or relatively poor pharmacokinetics of existing formulations. Using liposomes as carriers would help in overcoming these problems, however, their use is limited by the low incorporation efficiency of taxane molecules within bilayer and by subsequent drug crystallization.

Investigation of damping effects on low-frequency steady-state acoustical behaviour of coupled spaces.

In the low-frequency range, the acoustical behaviour of enclosed spaces is strongly influenced by excited acoustic modes resulting in a spatial irregularity of a steady-state sound field. In the paper, this problem has been examined theoretically and numerically for a system of coupled spaces with complex-valued conditions on boundary surfaces. Using a modal expansion method, an analytic formula for Green's function was derived allowing to predict the interior sound field for a pure-tone excitation.

Diversity of extended-spectrum beta-lactamase-producing Escherichia coli rods.

Introduction: The aim of the study was to evaluate genetic relatedness and antimicrobial susceptibility of extended-spectrum beta-lactamase-producing E. coli strains isolated from patients hospitalized in the University Hospital in Bydgoszcz (Poland).

Material And Methods: The study included 33 extended-spectrum beta-lactamase-producing E.

[Relationship of serum alanine aminotransferase (ALT) to body weight, age and sex in blood donors population].

The activity of alanine aminotransferase (ALT) is the most popular parameter in hepatology. Increase of ALT usually suggests the damage of hepatocytes. The aim of the study was to assess the range of value of serum alanine aminotransferase in healthy population and to assess the relationship between ALT level and body mass index (BMI), age and gender.