Pharmacia Ab

Pfizer Health Ab

Lisbeth Nilvebrant

Rolf A Johansson

Pinchas Moses

Birgitta Olsson

Anders Ringberg

Martin Wikberg

Bengt A Sparf

Gary Johansson

Ulla Hoeck

Helle Kristensen

Lene Orup Jacobsen

Bengt Ang Sparf

Torkel Gren

Bengt ANGke Sparf

Uli Hacksell

Bengt Hall&eacute;n

Gunilla Glas

Bj Orn Nilsson

Jan Str&ouml;mbom

Gunnar Nordvall

Torkek Gren

Jan Strombom

Bo Kreilg&aring;rd

Bengt Hallen

Bo Kreilgård

Bengt Hallén

Jan Strömbom

The invention relates to 3,3-diphenylpropylamines of formula (I), wherein Rsignifies hydrogen or methyl, Rand Rindependently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula (II), wherein Rand Rsignify non-aromatic hydrocarbyl groups, which may be the same or different and which together contain at least three carbon atoms, and wherein Rand Rmay form a ring together with the amine nitrogen, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The invention also relates to methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs

3,3-diphenylpropylamines, their use and preparation

3,3-Diphenylpropylamines, their use and preparation

The present invention is drawn to a method of treating an unstable or overactive urinary bladder by treating the patient with tolterodine or a tolterodine-related compound, or pharmaceutically acceptable salt thereof, with a controlled release formulation that maintains a substantially constant serum level of the active moiety or moieties for at least 24 hours. The present invention is further drawn to a formulation for the method.

Therapeutic formulation for administering tolterodine with controlled release

The invention relates to a pharmaceutical formulation containing tolterodine or a tolterodine-related compound, or a pharmacologically acceptable salt thereof, as active ingredient, in which the formulation exhibits a controlled in vitro release of the active ingredient in phosphate buffer at pH 6.8 of not less than about 80% after 18 hours, and after oral administration to a patient is capable of maintaining a substantially constant serum level of the active moiety or moieties for 24 hours. The invention also relates to the use of the pharmaceutical formulation for treating overactive bladder and gastrointestinal disorders.

Pharmaceutical formulation and its use

A 3,3-diphenylpropylamine of the formula I, or its physiologically acceptable acid salt thereof: ##STR1## wherein R.sup.1 represents hydrogen or methyl, R.sup.2 and R.sup.3 independently represent hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula II ##STR2## wherein R.sup.4 and R.sup.5 independently represent a hydroxy substituted or unsubstituted non-aromatic hydrocarbyl group which can join together to form a ring and which together contain at least three carbon atoms, wherein at least one of R.sup.4 and R.sup.5 is hydroxy substituted, is useful in treating acetylcholine-mediated disorders such as urinary incontinence.

Heteroaromatic quinuclidinenes, their use and preparation

The invention relates to 3,3-diphenylpropylamines of formula (I), wherein R.sup.1 signifies hydrogen or methyl, R.sup.2 and R.sup.3 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of formula (II), wherein R.sup.4 and R.sup.5 signify non-aromatic hydrocarbyl groups, which may be the same or different and which together contain at least three carbon atoms, and wherein R.sup.4 and R.sup.5 may form a ring together with the amine nitrogen, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The invention also relates to methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs ##STR1##

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Bromma, Sweden

Lisbeth Nilvebrant