Search results for "PIP"

Multinuclear magnetic resonance, electrospray ionization time-of-flight mass spectral and molecular modelling characterization of lithocholic acid am…

2003

1H, 13C and 15N NMR and electrospray ionization time-of-flight mass spectrometric characterizations of five lithocholate esters of piperazine diamides are described. Two of them are cholaphane-type cyclic structures esterified with 2,2′-bipyridine-4,4 ′ - and pyridine-2,6-dicarboxylic acid and the other three esters are open structures comprising two or four lithocholyl residues. The conformational preferences of the dimeric congeners were examined by using molecular modelling and variable-temperature 1H NMR techniques. Copyright © 2003 John Wiley & Sons, Ltd.

1H-, 13C-, and 15N-NMR and ESI-TOF+ MS studies of a supramolecular complex of silver(I) and a cholaphane

2003

A novel application of the mixed anhydride procedure for synthesising lithocholic acid piperazine diamide, an important intermediate in designing bile acid-based supramolecular host molecules, is reported. The synthesis of a thiophene-containing cholaphane with transition metal complexation ability and 1H-, 13C-, and 15N-NMR as well as ESI-TOF+ MS spectral characterisation of the ligand and its Ag(I) complex are included. The coordination of the Ag(I) ion as well as an ability of the cholaphane to recognise Ag(I) ion over alkali metal ions, especially potassium ion, is discussed. The possible medical applications are also presented.

Real-world effectiveness of long acting aripiprazole: Treatment persistence and its correlates in the Italian clinical practice

2019

Abstract Objectives To identify the variables that are associated with persistence to Aripiprazole-Long Acting (A-LAI), in adult patients with schizophrenia. Methods Observational, retrospective, non-interventional study involving 261 patients with schizophrenia. Results Eighty-six percent of study subjects were persistent for at least 6 months. All subjects with baseline CGI-S of 1 or 2, 95% of subjects with CGI-S of 3, 86% with CGI-S of 4, 82% of subjects with CGI-S of 5, 73% of subjects with CGI of 6 and 90% of subjects with CGI of 7 were persistent. A-LAI treatment continuation rate was higher in patients with: 1) baseline CGI score ≤ 4; 2) schizophrenia dimension (LDPS) mania score ≤ 5…

Comparing 1-year effectiveness and acceptability of once-monthly paliperidone palmitate and aripiprazole monohydrate for schizophrenia spectrum disor…

2022

In this prospective study, we assessed the effectiveness and acceptability of paliperidone palmitate 1-month (PP1M) and aripiprazole monohydrate (AM) over 1-year follow-up. We included 195 subjects (117 treated with PP1M and 78 with AM) with schizophrenia spectrum disorders from real-world settings. We estimated no differences in hospitalization (Odds Ratio=1.59; p = 0.12), symptoms improvement (p = 0.90 adjusted for baseline severity), and discontinuation (Hazard Ratio=0.72; p = 0.20) at study endpoint. Although current evidence suggests the possible superiority of AM over PP1M, our findings showed comparable effectiveness between these drugs. Additional studies in real-world settings with…

Elimination of quiescent/slow-proliferating cancer stem cells by Bcl-XL inhibition in non-small cell lung cancer

2014

Lung cancer is the most common cause of cancer-related mortality worldwide, urging the discovery of novel molecular targets and therapeutic strategies. Stem cells have been recently isolated from non-small cell lung cancer (NSCLC), thus allowing the investigation of molecular pathways specifically active in the tumorigenic population. We have found that Bcl-XL is constantly expressed by lung cancer stem cells (LCSCs) and has a prominent role in regulating LCSC survival. Whereas chemotherapeutic agents were scarcely effective against LCSC, the small molecule Bcl-2/Bcl-XL inhibitor ABT-737, but not the selective Bcl-2 inhibitor ABT-199, induced LCSC death at nanomolar concentrations. Differen…

Control of Flow Rate in Pipeline Using PID Controller

2019

In this paper a PID controller is utilized in order to control the flow rate of the heavy-oil in pipelines by controlling the vibration in motor-pump. A torsional actuator is placed on the motor-pump in order to control the vibration on motor and consequently controlling the flow rates in pipelines. The necessary conditions for asymptotic stability of the proposed controller is validated by implementing the Lyapunov stability theorem. The theoretical concepts are validated utilizing numerical simulations and analysis, which proves the effectiveness of the PID controller in the control of flow rates in pipelines.

Evaluation and clinical analyses of downstream targets of the Akt inhibitor GDC-0068.

2013

Abstract Purpose: The oncogenic PI3K/Akt/mTOR pathway is an attractive therapeutic target in cancer. However, it is unknown whether the pathway blockade required for tumor growth inhibition is clinically achievable. Therefore, we conducted pharmacodynamic studies with GDC-0068, an ATP competitive, selective Akt1/2/3 inhibitor, in preclinical models and in patients treated with this compound. Experimental Design: We used a reverse phase protein array (RPPA) platform to identify a biomarker set indicative of Akt inhibition in cell lines and human-tumor xenografts, and correlated the degree of pathway inhibition with antitumor activity. Akt pathway activity was measured using this biomarker se…

MR IMAGING IN A CASE OF PRIMARY EPIPLOIC APPENDAGITIS IN A 12 YEARS GIRL

2013

Data Augmentation for Pipeline-Based Speech Translation

2020

International audience; Pipeline-based speech translation methods may suffer from errors found in speech recognition system output. Therefore, it is crucial that machine translation systems are trained to be robust against such noise. In this paper, we propose two methods for parallel data augmentation for pipeline-based speech translation system development. The first method utilises a speech processing workflow to introduce errors and the second method generates commonly found suffix errors using a rule-based method. We show that the methods in combination allow significantly improving speech translation quality by 1.87 BLEU points over a baseline system.

Synthesis of a polymer-bound galactosylamine and its application as an immobilized chiral auxiliary in stereoselective syntheses of piperidine and am…

2004

A 2,3,4-tri-O-pivaloylated beta-D-galactopyranosyl azide bearing a hydroxy-functionalized spacer unit at the C-6 position of the galactose was synthesized and immobilized on the solid phase by using a polymer-bound chlorosilane. The azide was reduced to the corresponding galactopyranosylamine, which served as a versatile chiral auxiliary in highly diastereoselective Ugi four-component condensation reactions at ambient temperature. Fluoride-induced cleavage from the polymeric support furnished N-glycosylated N-acylated alpha-amino acid amides. The reaction of the immobilized galactosylamine with aldehydes gave rise to the corresponding aldimines, which underwent a domino Mannich-Michael cond…