Thematische Bibliographien / EPC2206

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Auswahl der wissenschaftlichen Literatur zum Thema „EPC2206“

Autor: Grafiati

Veröffentlicht am 28. Juni 2021

Zuletzt aktualisiert am 1. Februar 2022

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Zeitschriftenartikel zum Thema "EPC2206"

Read, W. L., P. Rosen, P. Lee, S. Anthony, R. Korn, N. Raghunand, B. Tseng, J. Whisnant, D. Von Hoff und R. Tibes. „Pharmacokinetic and pharmacodynamic results of a 4-hr IV administration phase I study with EPC2407, a novel vascular disrupting agent“. Journal of Clinical Oncology 27, Nr. 15_suppl (20.05.2009): 3569. http://dx.doi.org/10.1200/jco.2009.27.15_suppl.3569.

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3569 Background: EPC2407 is a 4-aryl-chromene single isomer microtubulin inhibitor with vascular disrupting and apoptotic activity at nanomolar concentrations. In an earlier phase I study dosing by 1 hr infusions daily x3 on a 21 day cycle, DLT at 21 mg/m2 was pain at tumor sites and vasoconstriction with increases of BP and QTc. MTD was 13 mg/m2 over 1 hr (ASCO 2008, Abst 2531). All drug-related toxicities resolved within an hour of stopping the infusion. Prolonged infusion of EPC2407 to extend exposure of tumor vasculature was designed with administration of EPC2407 over 4 hrs for 3 consecutive days of a 21 day cycle. Eleven patients have received this schedule and their cancers included leiomyosarcoma, colo-rectal, ovary, hepatocellular (2), NSCLC, pancreas, carcinoid, hemangiopericytoma, larynx and small bowel. Results: Doses escalated from 13 to 30 mg/m2 over 4 hours, with MTD determined to be 24 mg/m2. DLTs at 30 mg/m2 were similar to those seen in the 1 hr infusion, with pain at tumor sites in 1 participant and asymptomatic ST depression in a second. Other toxicities were also similar and included transient hypertension. QTc increases were not significant and no new toxicities were encountered. T1/2 with 4 hr infusion was ∼2hr, also seen with 1 hr infusion. AUC and Cmax values were similar to that predicted from the 1 hr data except AUC at 13 mg/m2 was lower than expected. DCE-MRI was done at baseline and after infusion on day 3, cycle 1. Analysis to date of DCE-MRI data of 4 patients showed a median decrease of 40% in both tumor permeability (Ktrans) and tumor perfusion volume (Vp). The two patients with hepatocellular carcinoma had notable stable disease and clear clinical benefit. Both patients received 18 mg/m2 dose, with one receiving 7 cycles over 5 months, and the other still on study (cycle 6) with stable disease for at least 4 cycles. Conclusions: EPC2407 shows clinical promise, with infusion-associated toxicities characteristic of the VDA drug class but without sustained or cumulative toxicity. Studies combining EPC2407 with conventional cytotoxic/cytostatic regimens are being designed. [Table: see text]

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Anthony, S. P., D. Von Hoff, J. K. Whisnant und B. Y. Tseng. „EPC2407, a new beta-tubulin vascular disrupting agent with potent apoptosis and cell growth inhibition“. Journal of Clinical Oncology 25, Nr. 18_suppl (20.06.2007): 14043. http://dx.doi.org/10.1200/jco.2007.25.18_suppl.14043.

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14043 Background: Compounds which bind to colchicine-like sites of microtubules have contributed greatly to the armamentarium of cancer therapies. But new modes of administration of taxanes and potent new vascular disruption agent molecules such as combretastatin continue to challenge drug development for ways to improve the therapeutic index in this important class. EPC2407 is a novel 4-aryl chromene of nM anti-tumor potency; it is crossing the translational bridge based on an array of preclinical anti-tumor pharmacology and supported by multiple toxicology trials which included drug exposure data. Methods: Vascular disrupting agents demand careful preclinical workup. What we have done is summarized in the table below. This data is from cellular metabolic, cell proliferation, vascular endothelial, in vivo tumor, and animal toxicokinetic and safety studies. Results: Please see table below of the preclinical experiments. Conclusions: A Phase I clinical trial has been designed and initiated to replicate the safety margin shown by the analysis of preclinical drug exposure data. The critical safety issue for human dosing was the dose exposure which might produce the well known ECG abnormality of delayed repolarization or prolonged QTc. A dose related QTc effect was demonstrated in cynomolgus monkeys after a 2 min infusion which achieved acute plasma exposures higher than 3836 nM. These effects were dose related and persisted only through 4 short half-lives of the parent compound. Initial human analysis fails to show any prolongation of the QTc. [JW1] [JW1]THE END HERE, all else was draft. [Table: see text] No significant financial relationships to disclose.

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Gambini, Emanuela. „No Patents on Seeds Files an Opposition against Monsanto's Patent EP 2 134 870 B1 Covering the Selection of Soybean Plants and Seeds“. European Journal of Risk Regulation 6, Nr. 1 (März 2015): 134–40. http://dx.doi.org/10.1017/s1867299x00004360.

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On 25th November, 2014, the coalition “No Patents on Seeds” filed an opposition against the European patent EP 2 134 870 B1, held by the U.S. Company Monsanto Technology. The patent, granted on 26th February, 2014, by the European Patent Office, covers “utility of SNP [single nucleotide polimorfism] markers associated with major soybean plant maturity and growth habit genomic regions” and includes “methods for screening plants and seeds from the genus Glycine withmarkers associated with genomic regions that are related to the plant maturity and growth habit of Glycine plants”.“No Patents on Seeds” claims that the patent should be completely revoked, as it falls within the exclusion of essentially biological processes for the production of plants from patentability under art. 53(b) of the European Patent Convention (EPC2000) and is not a patentable invention according to art. 52(2)(a) EPC. This case note gives an overview of the opposition and discusses its implications.

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Mahesh S und Balaji G L. „PEG-SO3H promoted one pot grinding method for the synthesis of 2-amino-4H-chromene-3-carboxylates“. International Journal of Research in Pharmaceutical Sciences 11, Nr. 4 (25.09.2020): 5321–27. http://dx.doi.org/10.26452/ijrps.v11i4.3152.

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There is a crucial medical need for the synthesis of 4H-chromene compounds via simple efficient methods. 4H-chromene compounds are stated to have a wide range of medicinal applications such as anti-bacterial, anti-cancer (EPC2407 and MX58151), antimalarial, antifungal, anti-rheumatic and anti-viral properties depending up on the substituents which is present on the heterocyclic compounds. Nowadays multi component protocols shows a better advantages such as better yield, less reaction time and no usage of different solvents for synthesis of biological important heterocyclic compounds over other synthetic approaches. The operational simplicity and applicability of this protocol to various analogues make it an alternative to previous reported methods.Therefore, this work was to prepare a series of 4H-chromene analogues via simple method with short time. Here, we reported the synthesis of 2-amino-4H-chromene-3-carboxylates using green solvent(water) under grinding method by one pot three component reaction of substituted aldehydes, dimedone and cyano acetates. This reaction was catalysed by catalytic amount of PEG-SO3H at room temperature. This catalyst proved the efficient for synthesis of many heterocyclic compounds. This reaction proceeds with very short time i.e. 5 mins. The 2-amino-4H-chromene derivatives (4a-i) was obtained with excellent yields(85-94%).

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Anthony, S. P., W. Read, P. J. Rosen, R. Tibes, D. Park, D. Everton, B. Tseng, J. Whisnant und D. D. Von Hoff. „Initial results of a first-in-man phase I study of EPC2407, a novel small molecule microtubule inhibitor anticancer agent with tumor vascular endothelial disrupting activity“. Journal of Clinical Oncology 26, Nr. 15_suppl (20.05.2008): 2531. http://dx.doi.org/10.1200/jco.2008.26.15_suppl.2531.

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Naida, S. A., Y. O. Onykienko, O. I. Drozdenko, O. I. Smolenska, V. S. Baran und N. O. Iakunina. „Analysis of the influence of load inductance on nonlinear distortions of a class D amplifier caused by «dead time»“. Electrical Engineering & Electromechanics, Nr. 3 (23.06.2021): 32–37. http://dx.doi.org/10.20998/2074-272x.2021.3.05.

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Goal. Analysis of the effect of load inductance at the output of the class D amplifier for different values of the duration of «dead time» and assessment of the adequacy of existing mathematical models for calculating the THD at the output of the amplifier depending on the duration of «dead time». Methodology. The study of the effect of «dead time» on the THD was performed using a computer model of the half-bridge converter board EPC9035 from Efficient Power Conversion. This board contains GaN transistors EPC2022 eGaN®, the corresponding control driver and other necessary elements for operation. The use of GaN transistors has made it possible to investigate the operation in a wide range of frequent switching, both to control the motor and to amplify the audio signal. Results. It is established that the value of load inductance affects the level of nonlinear distortions caused by «dead time». At inductance values that provide a constant sign of the output current, a difference arises between the duration of the input and output pulses, which increases the THD. At inductance values, when the choke current changes sign during a pulse, there is no error between the duration of the input and output pulses. Changing the inductance changes the relationship between the error signal and the non-error signal. THD changes accordingly. At high conversion frequencies, the voltage spikes caused by the choke current through the built-in diodes during the dead time are partially compensated by overcharging the output capacitance of the transistors, which also reduces harmonic distortion. Originality. For the first time, the value of the THD at the outlets in the fallowness of the different indices of the inductance of the choke and the theoretical calculation of the value in the results of the computer model was obtained. Practical significance. The dependence of the THD values on the inductance of the choke for converters with a switching frequency range from 1 kHz to 400 kHz, which allows them to be used both to control the motor and to amplify the audio signal.

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„EIPC. EIPC to manage EPC2000“. Circuit World 26, Nr. 3 (September 2000). http://dx.doi.org/10.1108/cw.2000.21726cab.021.

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„EPC2002 exhibitors meeting well attended“. Circuit World 28, Nr. 2 (Juni 2002). http://dx.doi.org/10.1108/cw.2002.21728bab.002.

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Dissertationen zum Thema "EPC2206"

Galia, Jan. „Měnič s tranzistory GaN pro elektrický kompresor“. Master's thesis, Vysoké učení technické v Brně. Fakulta elektrotechniky a komunikačních technologií, 2021. http://www.nusl.cz/ntk/nusl-442787.

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This master’s thesis deals with the design and realization of a functional sample power inverter for an electric compressor, which is used in hybrid cars. The electric compressor powered by the inverter is E-compressor by Garrett Advancing Motion. An inverter will be using modern High Electron Mobility Transistors which are based on gallium nitride (GaN). The purpose of this thesis is to find if GaN transistors can be used in E-boosting application.

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