- Identification of the decomposition products in an industrial nitration process under thermal runaway conditions
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Directive 96/82/EC on the control of major-accident hazards involving dangerous substances, so-called Seveso II Directive, requires inventorying of dangerous substances which are believed might be generated during loss of control of an industrial chemical process. In the present work a nitration process that has underlined a potential risk of thermal runaway has been studied. A kinetic model has been developed and validated using the calorimetric data from a Mettler RC1 and a differential scanning calorimeter, along with the commercial software BatchCAD. The model has been later used to simulate the behavionr of an industrial reactor under abnormal conditions and to evaluate their consequences. Finally, the conditions that lead to thermal runaway scenarios have been reproduced to identify the decomposition products, as Seveso II Directive requires, using thermogravimetry and adiabatic calorimetry coupled with FTIR gas analyser.
- Lunghi, Angelo,Alos, Miquel A.,Gigante, Lucia,Feixas, Joan,Sironi, Eugenio,Feliu, Josep A.,Cardillo, Paolo
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- Isomeric methoxy analogs of nimesulide for development of brain cyclooxygense-2 (COX-2)-targeted imaging agents: Synthesis, in vitro COX-2-inhibitory potency, and cellular transport properties
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Nimesulide analogs bearing a methoxy substituent either at the ortho-, meta- or para-position on the phenyl ring, were designed, synthesized, and evaluated for potential as radioligands for brain cyclooxygenase-2 (COX-2) imaging. The synthesis of nimesulide and regioisomeric methoxy analogs was based on the copper-mediated arylation of phenolic derivatives for the construction of diaryl ethers. These isomeric methoxy analogs displayed lipophilicity similar to that of nimesulide itself, as evidenced by their HPLC log P7.4 values. In vitro inhibition studies using a colorimetric COX (ovine) inhibitor-screening assay demonstrated that the para-methoxy substituted analog retains the inhibition ability and selectivity observed for parent nimesulide toward COX-2 enzyme, whereas the meta- and ortho-methoxy substituents detrimentally affected COX-2-inhibition activity, which was further supported by molecular docking studies. Bidirectional transport cellular studies using Caco-2 cell culture model in the presence of the P-glycoprotein (P-gp) inhibitor, verapamil, showed that P-gp did not have a significant effect on the efflux of the para-methoxy substituted analog. Further investigations using the radiolabeled form of the para-methoxy substituted analog is warranted for in vivo characterization.
- Yamamoto, Yumi,Hisa, Takuya,Arai, Jun,Saito, Yohei,Yamamoto, Fumihiko,Mukai, Takahiro,Ohshima, Takashi,Maeda, Minoru,Ohkubo, Yasuhito
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p. 6807 - 6814
(2015/11/11)
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- Nimesulide derivative method for its preparation and a pharmaceutical composition containing the same
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A product of Formula (I): wherein X has the meanings stated in the description.Moreover, a method of preparing the product of Formula (I) and a pharmaceutical composition that contains said product of Formula (I) are also described.
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Page/Page column 4
(2008/06/13)
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- Method for the treatment and prevention of cachexia
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Cachexia, including anorexia and other forms of weight loss, is a frequent complication of acute and chronic infections, and result from induction of cytokines, prostaglandins, and other inflammatory mediators that are critical for pathogen elimination. The present invention includes methods for the treatment or prevention of cachexic conditions while maintaining the production of factors essential for infection control through the administration of an effective amount of a cyclooxygenase-2 selective inhibiting compound.
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- Controlled release anti-inflammatory oral formulation and a process for the preparation thereof
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A controlled release anti-inflammatory nimesulide oral formulation. The formulation comprises 45-65% by weight of nimesulide and 10-30% by weight of hydrophilic polymer as retardant with pharmaceutically acceptable auxiliary agents and/or excipients. The nimesulide is partially or fully dispersed in the hydrophilic polymer. The process for the preparation of the formulation comprises mixing the nimesulide with the hydrophilic polymer and pharmaceutically acceptable auxiliary agents and/or excipients.
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- Antiangiogenic combination therapy for the treatment of cancer
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The present invention provides combinations of a DNA topoisomerase I inhibiting agent and a selective COX-2 inhibiting agent for preventing, treating, and/or reducing the risk of developing a neoplasia disorder in a mammal.
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- Controlled release formulations of nimesulide and a process for the manufacture thereof
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A controlled release formulation in the form of oral dosage for treating inflamatory and pain disorders by administering Nimesulide in combination with hyprohilic matrix forming polymer to produce granules together with pharmaceutically acceptable excipients including binders and lubricants, tableted as per the commonly used pharmaceutical technology, said oral formulation provides a drug release of nimesulide for extended period of 24 hours.
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