Abstract: The present invention concerns compositions containing ranitidine or one of its pharmaceutically acceptable salts having low iron species content. The present invention also concerns compositions having low content of iron species that are not under complexed form with a chelating agent and/or having low content of iron species that are partially or completely under complexed form with a chelating agent and/or having low content of iron species that are under complexed form with a chelating agent other than ranitidine and/or having low content of complexes formed between ranitidine and iron species. The present invention also concerns a process for the preparation of said compositions. The present invention also concerns the second medical use of said compositions.

Abstract: Provided is a new photochemical process for preparing artemisinin. Also provided are certain dihydroartemisinic acid derivatives useful for preparing artemisinin.

Abstract: Provided is a new photochemical process for preparing artemisinin. Also provided are certain dihydroartemisinic acid derivatives useful for preparing artemisinin.

Abstract: The disclosure relates to derivatives of morphine-6-glucuronide of formula (I) wherein R1 is as defined in the disclosure, or an acid addition salt thereof, as well as in hydrate or solvate form. The disclosure also relates to the preparation method thereof and to the use of same in therapeutics.

Abstract: The present invention relates to a method for the preparation of morphine compounds comprising a low content of ?,?-unsaturated compounds, which comprises the steps of: (i) bringing the crude morphine compound into contact with a base, at a pH of greater than 13, under conditions which make possible the Michael addition reaction on the ?,?-unsaturated compound(s) present; (ii) separating the morphine compound from the reaction mixture; and (iii) if appropriate, separating the addition product formed from the morphine compound. It also relates to a composition comprising at least 99% by dry weight of morphine compound or of a pharmaceutically acceptable salt thereof, and an ?,?-unsaturated compound in a content of less than 100 ppm.

Abstract: The disclosure relates to compounds of formula (I): wherein R1, R2, and n are as defined in the disclosure, and addition salts solvates and hydrates thereof. The disclosure also relates to the preparation method of said compounds and to the use of the same in therapeutics.

Abstract: The invention discloses and claims N-Methylnaltrexone zwitterion, of formula (I), substantially in the anhydrous form or a hydrate thereof:

Abstract: The disclosure relates to a method for preparing morphine-6-glucuronide or one of the deritives thereof comprising reacting a compound of formula (I): wherein R1 is as defined in the disclosure, with a glucuronic acid derivative of formula (II): wherein PG, X, and R4 are as defined in the disclosure, in the presence of an aromatic solvent and trimethylsilyl trifluoromethanesulfonate; (ii) reacting the product obtained in step (i) with a strong basic agent; and then (iii) recovering the product obtained in step (ii).

Abstract: The disclosure relates to derivatives of morphine-6-glucuronide of formula (I) wherein R1 is as defined in the disclosure, or an acid addition salt thereof, as well as in hydrate or solvate form. The disclosure also relates to the preparation method thereof and to the use of same in therapeutics.

Abstract: The disclosure relates to a method for preparing morphine-6-glucuronide or one of the deritives thereof comprising reacting a compound of formula (I): wherein R1 is as defined in the disclosure, with a glucuronic acid derivative of formula (II): wherein PG, X, and R4 are as defined in the disclosure, in the presence of an aromatic solvent and trimethylsilyl trifluoromethanesulfonate; (ii) reacting the product obtained in step (i) with a strong basic agent; and then (iii) recovering the product obtained in step (ii).

Abstract: The disclosure relates to compounds of formula (I): wherein R1, R2, and n are as defined in the disclosure, and addition salts solvates and hydrates thereof. The disclosure also relates to the preparation method of said compounds and to the use of the same in therapeutics.

Abstract: Provided is a new photochemical process for preparing artemisinin. Also provided are certain dihydroartemisinic acid derivatives useful for preparing artemisinin.

Abstract: The present invention relates to a method for the preparation of morphine compounds comprising a low content of ?,?-unsaturated compounds, which comprises the steps of: (i) bringing the crude morphine compound into contact with a base, at a pH of greater than 13, under conditions which make possible the Michael addition reaction on the ?,?-unsaturated compound(s) present; (ii) separating the morphine compound from the reaction mixture; and (iii) if appropriate, separating the addition product formed from the morphine compound. It also relates to a composition comprising at least 99% by dry weight of morphine compound or of a pharmaceutically acceptable salt thereof, and an ?,?-unsaturated compound in a content of less than 100 ppm.

Abstract: The invention discloses and claims N-Methylnaltrexone zwitterion, of formula (I), substantially in the anhydrous form or a hydrate thereof:

Abstract: The invention relates to a novel process for preparing N-methylnaltrexone bromide, comprising at least the steps consisting in: (i) reacting N-methylnaltrexone methyl sulfate in aqueous solution with an alkaline agent chosen from the group constituted by sodium carbonate, potassium carbonate, calcium carbonate, magnesium carbonate, cesium carbonate, strontium carbonate and mixtures thereof, for a pH of the aqueous reaction medium of between 7 and 10, and then in (ii) reacting the product thus obtained with hydrobromic acid, which is added for a pH of the aqueous reaction medium of between 0.5 and 5, in order thus to obtain the N-methylnaltrexone bromide.

Abstract: A process for the preparation of for the preparation of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide and of its salts, wherein 1,5-dibromopentane is reacted with a compound of formula (IIIa) in the presence of Na2CO3 in acetonitrile heated at reflux.

Abstract: The invention relates to a novel process for preparing N-methylnaltrexone bromide, comprising at least the steps consisting in: (i) reacting N-methylnaltrexone methyl sulfate in aqueous solution with an alkaline agent chosen from the group constituted by sodium carbonate, potassium carbonate, calcium carbonate, magnesium carbonate, cesium carbonate, strontium carbonate and mixtures thereof, for a pH of the aqueous reaction medium of between 7 and 10, and then in (ii) reacting the product thus obtained with hydrobromic acid, which is added for a pH of the aqueous reaction medium of between 0.5 and 5, in order thus to obtain the N-methylnaltrexone bromide.

Abstract: A process for the preparation of for the preparation of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide and of its salts, wherein 1,5-dibromopentane is reacted with a compound of formula (IIIa) in the presence of Na2CO3 in acetonitrile heated at reflux.

Abstract: The present invention provides a method of making alkali metal and alkaline earth metal salts of L-ascorbic acid 2-monophosphate comprising reacting a L-ascorbic acid 2-polyphosphate under alkaline conditions with an alkali metal or alkaline earth metal salt of L-ascorbic-acid in concentrated aqueous solution. The amount of the L-ascorbic acid salt is in molar excess of the polyphosphate and the pH value of the reaction medium is maintained in the range of from about 8 to about 11 wherein the reaction is carried out until substantially all of the polyphosphate has been consumed and only L-ascorbic acid 2-monophosphate salt is present. A further aspect of the present invention comprises spray drying the mixture obtained after completion of the reaction, cooling and dilution to a suitable viscosity.