65 results about "Tapentadol" patented technology

A once daily controlled release pharmaceutical compositions comprising tapentadol, wherein preferably the mean T_max of tapentadol is reached after 10 hours of administration of the composition. The composition comprises tapentadol, such that it maintains serum concentration of tapentadol of at least about 20 ng/ml for at least about 17 hours after oral administration of the composition. According to one embodiment the controlled release pharmaceutical composition comprises tapentadol, which is gastroretentive.

The use of tapentadol for the manufacture of a medicament comprising at least one administration unit A containing dose a of tapentadol and at least one administration unit B containing dose b of tapentadol, where dose a<dose b, for the treatment of pain.

An aqueous pharmaceutical composition adapted for parenteral administration of tapentadol or a physiologically acceptable salt thereof having a pH value of at least 5.4.

An aqueous pharmaceutical composition containing tapentadol or a physiologically acceptable salt thereof and being adapted for oral administration. The composition has excellent storage stability without relying on the presence of high amounts of preservatives.

The invention relates to the field of drug synthesis, in particular to a method for preparing an analgesic tapentadol intermediate (2R,3R)-3-(3-methoxyl phenyl)-N,N,2-trimethyl amylamine hydrochloride. The method is characterized by comprising the following steps of: chlorinating optically active (2S,3R)-1-dimethylamino-3-(3-methoxyl phenyl)-2-methyl amyl-3-ol and phosphorus pentachloride and salifying with hydrogen chloride to obtain hydrochloride, and then carrying out stereoselective hydrogenolysis in the presence of a catalyst, and salifying with the hydrogen chloride to obtain the analgesic tapentadol intermediate. The method provided by the invention has the advantages of cleanness, safety, convenience for after treatment and lower production cost. Compared with a method in a literature, the method has reaction time shortened by nearly 80 hours.

The invention provides methods for preparing substituted phenylalkanes. In particular, the processes comprise reacting a phenyl boronic compound with an α-β unsaturated carbonyl-containing compound via an asymmetric 1,4-addition reaction. The processes may be useful in the synthesis of tapentadol.

A process for the synthesis of a salt of tapentadol.

The present invention discloses processes for the preparation of 3-[(1R,2R)-3-(dimethyl-amino)-1-ethyl-2-methyl-propyl]phenol (Tapentadol), salts thereof and related compounds of formula (A), including stereoisomers and pharmaceutically acceptable salts thereof, and to certain intermediates used in such process.

The use of tapentadol in the treatment of pain and/or pain chronification in a subject suffering from pain chronification and/or in the treatment of pain and inhibition of pain chronification in a subject suffering from pain and at risk of pain chronification, as well as the use of tapentadol for the treatment or inhibition of migraine.

The present invention relates to methods of treating and managing Parkinson's disease and related disorders. The methods especially find use in managing motor symptoms, including gait problems, particularly during advanced stages when effectiveness of standard medications wear off or side effects become problematic, as seen in Parkinson's disease, other disorders treated with dopaminergic agents, and other conditions associated with motor problems, such as aging or stroke. The treatment also may include disease-modifying effects, neuroprotection of, or neurorescue effects on neuronal cells in patients with Parkinson's disease and other neurodegenerative disorders. In particular, the invention relates to method of administering pharmaceutical compositions comprising effective amounts of tapentadol or a pharmaceutically acceptable salt or derivative thereof or, in other embodiments, stavudine or nabumetone, or a derivative thereof, for treating symptoms associated with Parkinson's disease, either as individual active agents, in combination with each other, or in combination with agents known to treat Parkinson's disease, such as the dopaminergic agent levodopa. The invention also relates to methods of preparing pharmaceutical compositions comprising effective amounts of tapentadol, stavudine, or nabumetone, or a derivative thereof, or further in combination with a dopaminergic agent, or derivative thereof, as well as to methods of using the pharmaceutical compositions in treating Parkinson's disease, related disorders, other conditions treated with dopaminergic agents, and other conditions with gait problems, for example by oral administration of the compositions.

A semisolid aqueous pharmaceutical composition containing tapentadol or a physiologically acceptable salt thereof.

The invention discloses a synthetic method of tapentadol. The method comprises the following steps: reacting meta-substitution cinnamic acid serving as a starting material with a chiral adjuvant to obtain amide; reacting the amide with a nucleophilic reagent and an electrophilic reagent, and introducing two chiral centers to obtain a chiral product; performing reduction and deprotection on the chiral product to obtain chiral alcohol; performing an amination reaction and a substitution reaction on the chiral alcohol to obtain the tapentadol. The tapentadol is synthesized by taking cheap and readily-available (1R,2R)-psedo-ephedrine as the chiral adjuvant, forming two chiral centers by using a one-pot method and performing simper deprotection and subsequent transformation. By adopting the synthetic method, the reaction route can be simplified, post-treatment steps can be reduced, and the production cost is reduced. The synthetic method is more suitable for industrial application.

The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below

using the (2R,3R)—O,O′-dibenzoyltartaric chiral acid wherein said resolution is quantitative.

The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.