Pharmaceutical compositions based on anticholinergics and PDE-IV inhibitors

• US 20040024007A1
• Filed: 07/03/2003
• Published: 02/05/2004
• Est. Priority Date: 03/07/2001
• Status: Abandoned Application

• Current Assignee: Boehringer Ingelheim Pharmaceuticals Incorporated (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Boehringer Ingelheim Pharmaceuticals Incorporated (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Pieper, Michael P., Pairet, Michel, Meade, Christopher J. M.
• Application Number:
  US10/613,783
• Publication Number:
  US 20040024007A1
• Time in Patent Office: Days
• US Class Current: 514/291
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• CPC Class Codes: A61K 31/4745 condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir

Abstract

The present invention relates to novel pharmaceutical compositions based on anticholinergics and PDE-IV inhibitors, processes for preparing them and their use in the treatment of respiratory tract diseases.

Claims

1. A pharmaceutical composition of matter comprising one or more anticholinergics and one or more PDE-IV inhibitors as active components of the pharmaceutical composition, wherein one or more of the active components may be an enantiomer, a mixture of enantiomers, a racemate, a solvate or an hydrate.

2. The pharmaceutical composition as recited in claim 1 wherein the pharmaceutical composition further comprises a pharmaceutically acceptable excipient.

3. The pharmaceutical composition as recited in claim 1 wherein the active components are present together in a single formulation.

4. The pharmaceutical composition as recited in claim 1 wherein the active components are in at least two separate formulations.

5. The pharmaceutical composition as recited in claim 1 wherein the anticholinergic is selected from the group consisting of one or more tiotropium salts, one or more oxitropium salts and one or more ipratropium salts.

6. The pharmaceutical composition as recited in claim 5 wherein the anticholinergic is one or more tiotropium salts.

7. The pharmaceutical composition as recited in claim 1 wherein one or more anticholinergic is present in the form of a chloride, bromide, iodide, methanesulphonate, paratoluene sulphonate or a methyl sulphate.

8. The pharmaceutical composition as recited in claim 7 wherein one or more anticholinergics is present in the form of a bromide.

9. The pharmaceutical composition as recited in claim 1 wherein one or more PDE-IV inhibitors is selected from among enprofylline, roflumilast, ariflo, Bay-198004, CP-325,366, BY343, D-4396 (Sch-351591), V-11294A, AWD-12-281 and the tricyclic nitrogen heterocycles of general formula 2a

10. The pharmaceutical composition as recited in claim 9 wherein one or more of the PDE-IV inhibitors is selected from among enprofylline, roflumilast, ariflo, AWD-12-281 and the tricyclic nitrogen heterocycles of general formula 2a.

11. The pharmaceutical composition as recited in claim 1 wherein the weight ratio of the anticholinergic to the PDE-IV inhibitor is about 1:

300 to about 50;

1.

12. The pharmaceutical composition as recited in claim 11 wherein the weight ratio of the anticholinergic to the PDE-IV inhibitor is about 1:

250 to about 40;

1.

13. The pharmaceutical composition as recited in claim 1 in the form of a formulation suitable for inhalation.