Pharmaceutical compositions based on anticholinergics and endothelin antagonists

• US 6,608,054 B2
• Filed: 03/18/2002
• Issued: 08/19/2003
• Est. Priority Date: 03/20/2001
• Status: Expired due to Term

• Current Assignee: Boehringer Ingelheim Pharma GmbH & Company Kg (C.H. Boehringer Sohn AG & Co. KG)
• Original Assignee: Boehringer Ingelheim Pharmaceuticals Incorporated (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Pairet, Michel, Pieper, Michael P., Meade, Christopher J. M.
• Primary Examiner(s): Weddington, Kevin E.
• Application Number:
  US10/100,659
• Publication Number:
  US 20020183347A1
• Time in Patent Office: 519 Days
• Field of Search: 514/229.5, 514/374, 514/378, 514/518, 514/826
• US Class Current: 514/229.5
• 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 31/335 having oxygen as the only ring hetero atom, e.g. fungichromin
• CPC Class Codes: A61K 31/42 Oxazoles
• 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 31/495 having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazinesA61K31/48 takes precedence ; with three nitrogen atoms A61K31/53
• CPC Class Codes: A61K 31/505 Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• CPC Class Codes: A61K 31/54 having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
• CPC Class Codes: A61K 9/0075 for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
• CPC Class Codes: A61K 9/0078 for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]

Abstract

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

Claims

1. An inhalable powder which comprises at least two active drug substances which drug substances are a salt of tiotropium and one or more endothelin antagonists, together with a pharmaceutically acceptable excipient selected from glucose, arabinose, lactose, saccharose or maltose.

2. The inhalable powder as recited in claim 1 wherein the salt of tiotropium is the chloride, bromide, iodide, methane sulphonate or paratoluene sulphonate salt.

3. The inhalable powder as recited in claim 2 wherein the salt of tiotropium is the bromide salt.

4. The inhalable powder as recited in claim 1 wherein the endothelin antagonist is selected from tezosentan, bosentan, enrasentan, sixtasentan, T-0201, BMS-193884, K-8794, PD-156123, PD-156707, PD-160874, PD-180988, S-0139 and ZD-1611.

5. The inhalable powder as recited in claim 4 wherein the endothelin antagonist is selected from tezosentan, bosentan, enrasentan, sixtasentan, T-0201 and BMS-193884.

6. The inhalable powder as recited in claim 1 wherein the weight ratio of tiotropium salt to endothelin antagonist is about 1:

300 to about 50;

1.

7. The inhalable powder as recited in claim 6 wherein the weight ratio of anticholinergic substance to endothelin antagonist is about 1:

250 to about 40;

1.

8. A method for the treatment of asthma which method comprises administering the inhalable powder as recited in claim 1.

9. A method for the treatment of chronic obstructive pulmonary disease which method comprises administering the inhalable powder as recited in claim 1.