Ucb Pharma Gmbh

Schwarz Pharma Ag

Schwartz Pharma Ag

Schwarz Pharma Limited

Claus Meese

Bengt Sparf

Hans-Michael Wolff

Roland Drews

Armin Breitenbach

Christoph Arth

Dietrich Wilhelm Schacht

Norma Selve

Klaus Sandrock

Seth C Ennis

Martin Feelisch

Dirk Schmidt

Hilmar Bokens

Jochen Lehmann

Seth Ennis

The compound of formula (I): is provided. It may be produced by subjecting a compound of formula (IV) to a reduction reaction wherein R represents hydrogen, straight or branched C1-C6 alkyl. This compound is a valuable intermediate which may be used in the synthesis of fesoterodine, tolterodine, its active metabolite, and related compounds.

Chiral intermediate, process for producing the same and its use in the manufacture of tolterodine, fesoterodine, or the active metabolite thereof

The compound of formula (I): is provided. It may be produced by subjecting a compound of formula (IV) to a reduction reaction wherein R represents hydrogen, straight or branched C-Calkyl. This compound is a valuable intermediate which may be used in the synthesis of fesoterodine, tolterodine, its active metabolite, and related compounds. 

The invention concerns novel derivatives of 3,3-diphenyl-propylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

Derivatives of 3,3-diphenylpropylamines

The invention relates to a compound of general formula (I) wherein A represents deuterium or hydrogen, R represents a group selected from Calkyl, Ccycloalkyl or phenyl, which can be substituted by C1-3 alkoxy, fluorine, chlorine, bromine, iodine, nitro, amino, hydroxyl, oxo, mercapto or deuterium. The C atom marked with a * (star) can be present in an (R) configuration, in an (S)-configuration or a mixture thereof. The invention is characterized in that the above-mentioned compounds are free bases with a degree of purity of more than 97 wt %. The invention also relates to a method for the production of highly pure compounds of general formula (I) and to the use thereof in the production of medicaments. 

High purity bases of 3,3-diphenylpropylamino monoesters

The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

The present invention provides a process for the production of a compound of formula (I) or a salt thereof, wherein R is hydrogen, a straight, branched or cyclic C-Calkyl group or an aryl group which may optionally be substituted. This process comprises: (a) reacting a compound of formula (II), with a compound of formula (III), wherein R is as defined above and X is a leaving group, in the presence of N,N-di-isopropylethylamine. 

Synthesis of phenolic esters of hydroxymethyl phenols

The invention relates to a device for transdermally administering a compound of formula (I), wherein A represents hydrogen or deuterium, R represents a group selected among Calkyl, Ccycloalkyl, or phenyl, each of which can be substituted by Calkoxy, fluoride, chlorine, bromine, iodine, nitro, amino, hydroxy, oxo, mercapto, or deuterium, the C atom marked by * (asterisk) being provided in the R configuration. The invention is characterized in that the compound of general formula (I) is provided in a polymer matrix and is released at a dose of 0.5 to 20 mg per day through human skin. The invention further relates to the use of said compounds of formula (I) for producing transdermal medicaments. 

Transdermal delivery of (R)-3,3-diphenylpropylamin-monoestern

Transdermal administration of (R)-3,3-diphenylpropylamin-monoesters

This invention relates to azaspiro compounds and their use as medications especially for the treatment of chronic, chronic-phlogistic and/or neuropathic pain. Compounds that lend themselves particularly well to the production of analgesics include 1,3-diazaspiro[4.5]decane-2,4-dion and 1,3-diazaspiro[4.5]decane-2,4-dithion.

Derivatives of azaspiro compounds for the treatment of pain

The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products. The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(&#x2212;)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.

Stable salts of novel derivatives of 3,3-diphenylpropylamines

The invention relates to a method for producing derivatives of 3,3-diarylpropylamines of general formula (I) and sterically highly pure, stable intermediate products, and to their use for producing pharmaceutical compositions.

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Monheim, Germany

Claus Meese