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Details for Patent: 5,686,464

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Details for Patent: 5,686,464

Title: 3,3-diphenylpropylamines, their use and preparation
Abstract: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.
Inventor(s): Johansson; Rolf Arne (Huddinge, SE), Moses; Pinchas (Satsjo-Boo, SE), Nilvebrant; Lisbeth (Bromma, SE), Sparf; Bengt .ANG.ke (Tr.ang.ngsund, SE)
Assignee: Pharmacia AB (Stockholm, SE)
Filing Date:Jul 22, 1996
Application Number:08/684,638
Claims:1. A 3 3-diphenylpropylamine of the formula I: ##STR13## 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 ##STR14## 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; or a physiologically acceptable acid salt thereof.

2. The 3,3-diphenylpropylamine according to claim 1 wherein R.sup.4 and R.sup.5 are each independently saturated hydroxy substituted or unsubstituted hydrocarbyl groups.

3. The 3,3 -diphenylpropylamine according to claim 1, wherein the HOCH.sub.2 -group is in the 5-position on the phenyl ring, R.sup.2 is hydrogen and R.sup.3 is hydrogen or hydroxy.

4. A pharmaceutical composition comprising an effective amount of a 3,3-diphenylpropylamine according to claim 1 and a compatible pharmaceutical carrier.

5. The 3,3-diphenylpropylamine according to claim 1, wherein said compound is an individual enantiomer.

6. The 3 3-diphenylpropylamine according to claim 2, wherein R.sup.4 and R.sup.5 independently represent a hydroxy substituted or unsubstituted C.sub.1-8 -alkyl group or adamantyl and the total number of carbon atoms contained in R.sup.4 and R.sup.5 is at least four carbon atoms.

7. The 3,3-diphenylpropylamine according to claim 6, wherein R.sup.4 and R.sup.5 independently represent a hydroxy substituted or unsubstituted C.sub.1-6 -alkyl group.

8. The 3,3-diphenylpropylamine according to claim 3, wherein R.sup.3 is in the 2-position on the phenyl ring.

9. A method for treating acetylcholine-mediated disorders which comprises administering to a patient in need thereof an effective amount of a 3,3-diphenylpropylamine as claimed in claim 1.

10. The method according to claim 9, wherein said disorder is urinary incontinence.
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