26638-66-4Relevant articles and documents
A process for preparing 3,11-Dichloro-6-methyl -6,11-dihydrodibenzo[c,f][1,2]thiazepine 5,5-dioxide
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Paragraph 0036-0041; 0052-0054, (2020/10/05)
The present invention relates to a method for preparing 3,11-dichloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepine 5,5-dioxide. More particularly, the present invention relates to a method for preparing high-purity 3,11-dichloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepine 5,5-dioxide at a high yield under safe atmosphere through a quantitative reaction without introduction of an excessive amount of hydrogen chloride gas from the outside by substituting the hydroxyl group of 3-chloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepine-11-ol 5,5-dioxide as a starting material with a chloride group by means of hydrogen chloride gas generated in situ under the environment of acetyl chloride and the same equivalent of alcohol.
NOVEL PROCESS FOR THE PREPARATION OF 7-((3-CHLORO-6-METHYL-5,5-DIOXO-6,11-DIHYDRODIBENZO(C,F)(1,2) THIAZEPIN-11-YL)AMINO)HEPTANOATE
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Page/Page column 5, (2010/08/05)
The present invention relates to a novel process for the preparation of sodium 7-((3-Chloro-6-methyl-5,5-dioxo-6,11-dihydrodibenzo(c,f)(1,2)thiazepin-11-yl)amino)heptanoate and intermediates. The invention also encompasses isolation of an essentially non-hygroscopic compound which is substantially pure.
New Triazine Derivatives as Potent Modulators of Multidrug Resistance
Dhainaut, Alain,Regnier, Gilbert,Atassi, Ghanem,Pierre, Alain,Leonce, Stephane,et al.
, p. 2481 - 2496 (2007/10/02)
A series of 70 triazine derivatives have been synthesized and tested for their capacity to modulate multidrug resistance (MDR) in DC-3F/AD and KB-A1 tumor cells in vitro, in comparison with verapamil (VRP), a calcium channel antagonist currently used in therapy as an antihypertensive drug, which also shows MDR modulating activity.Among the 12 selected compounds, 16 (S9788) showed high MDR reversing properties in vitro (300- and 6-fold VRP at 5μM in DC-3F/AD and KB-A1 cells, respectively) and induced a strong accumulation of adriamycin.The relationship between the increase of ADR accumulation and the fold reversal induced by these compounds and their lack of effects on the sensitive DC-3F cells suggest that they act mainly by inhibiting the P-glycoprotein (Pgp) catalyzed efflux of cytotoxic agents, as already described for a majority of MDR modulators.In vivo, in association with the antitumor drug vincristine (0.25 mg/kg), 16 (100 mg/kg) increased the T/C by 39percent in mice bearing the resistant tumor cell line P388/VCR.According to these interesting properties, 16 was selected for a clinical development because it is more bioavailable than 34, even though it was less active.