Claims for Patent: 8,338,478

Summary for Patent: 8,338,478

Title:	Derivatives of 3,3-diphenylpropylamines
Abstract:	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.
Inventor(s):	Claus Meese, Bengt Sparf
Assignee:	UCB Pharma GmbH
Application Number:	US13/161,049
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,338,478
Patent Claims:	1. 3,3-Diphenylpropylamines of the formula where: R1 is hydrogen and R2 is C1-C6 alkylcarbonyl; or R1 is C1-C6 alkylcarbonyl and R2 is hydrogen; and X is a tertiary amino group of formula where R8 and R9 are each independently C1-C8 alkyl and together comprise at least three carbon atoms; their salts with physiologically acceptable acids, their free bases and, when the 3,3-Diphenylpropylamines are in the form of optical isomers, the racemic mixture and the individual enantiomers. 2. The 3,3-Diphenylpropylamines of claim 1 where R8 and R9 are each independently C1-C6 alkyl. 3. The 3,3-Diphenylpropylamines of claim 1 where X is selected from the group consisting of: 4. The 3,3-Diphenylpropylamines of claim 1 where R1 is hydrogen and R2 is C1-C6 alkylcarbonyl. 5. The 3,3-Diphenylpropylamines of claim 1 where R1 is C1-C6 alkylcarbonyl and R2 is hydrogen. 6. A method of treating urinary incontinence in a patient in need thereof, the method comprising administering to the patient an effective amount of a 3,3-Diphenylpropylamine of the formula where: R1 is hydrogen and R2 is C1-C6 alkylcarbonyl; or R1 is C1-C6 alkylcarbonyl and R2 is hydrogen; and X is a tertiary amino group of formula where R8 and R9 are each independently C1-C8 alkyl and together comprise at least three carbon atoms; or its salt with a physiologically acceptable acid, its free base or, when the 3,3-Diphenylpropylamine is in the form of optical isomers, the racemic mixture and the individual enantiomers. 7. The method of claim 6 where R8 and R9 are each independently C1-C6 alkyl. 8. The method of claim 6 where X is selected from the group consisting of: 9. The method of claim 6 where R1 is hydrogen and R2 is C1-C6 alkylcarbonyl. 10. The method of claim 6 where R1 is C1-C6 alkylcarbonyl and R2 is hydrogen. 11. The method of claim 6, where the 3,3-Diphenylpropylamine is administered to the patient in the form of a pharmaceutical composition comprising a pharmaceutically acceptable carrier. 12. A pharmaceutical composition comprising an effective amount of a 3,3-Diphenylpropylamine according to any one of claims 1-5 and a pharmaceutically acceptable carrier.