57 results about "Dronedarone" patented technology

The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.

The invention provides a solid drug combination, consisting of micronized hydrochlorid Dronedarone, surfactant and hydrophilic polymer which is used as cosolvent. The invention is mainly used to cure arrhythmia.

The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof, which comprises reacting of compound of formula (IV) with compound of formula (VI) in a Grignard reaction, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and processes for the preparation thereof.

The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof, characterized in that a compound of formula (II)—where L is leaving group—is reacted with compound of formula (III) and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.

The invention relates to a process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that from the compound of formula (II). The hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.

The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof the hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.

The present disclosure relates to a solid composition comprising ranolazine and a spray-dried phosphoric acid salt of dronedarone in a bilayer tablet.

The present invention relates to a method for the treatment or prevention of atrial fibrillation and / or atrial flutter comprising coadministration of a synergistically therapeutic amount of dronedarone or a pharmaceutically acceptable salt or salts thereof and a synergistically therapeutic amount of ranolazine or a pharmaceutically acceptable salt or salts thereof. Also provided are methods for modulating ventricular and atrial rhythm and rate. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.

The invention relates to a method for synthesis of dronedarone. The method comprises the following steps that 1), p-nitrophenol, paraformaldehyde and concentrated hydrochloric acid as raw materials undergo a condensation reaction in the presence of concentrated hydrochloric acid or phosphoric acid as a catalyst to produce 2-chloromethyl-4-nitrophenol; 2), 2-chloromethyl-4-nitrophenol and triphenylphosphine undergo a reflux reaction in the presence of chloroform to produce 2-hydroxy-5-nitrobenzyl-triphenyl-phosphonium chloride, and 3), 2-hydroxy-5-nitrobenzyl-triphenyl-phosphonium chloride and n-valeryl chloride undergo a condensation reaction in a toluene solution in the presence of triethylamine and n-pentanoic acid as catalysts to produce 2-(n-butyl)-5-nitrobenzofuran.