PHARMACEUTICAL COMPOSITIONS ON ANTICHOLINERGICS, CORTICOSTEROIDS AND BETAMIMETICS

• US 20090088408A1
• Filed: 08/29/2008
• Published: 04/02/2009
• Est. Priority Date: 06/23/2001
• Status: Abandoned Application

• Current Assignee: Christopher J.M. Meade, Michael P. Pieper, Michel Pairet
• Original Assignee: Christopher J.M. Meade, Michael P. Pieper, Michel Pairet
• Inventors: Pieper, Michael P., Meade, Christopher J. M., Pairet, Michel
• Application Number:
  US12/201,149
• Publication Number:
  US 20090088408A1
• Time in Patent Office: Days
• US Class Current: 514/171
• 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 31/537 spiro-condensed or forming part of bridged ring systems
• CPC Class Codes: A61K 31/538 ortho- or peri-condensed with carbocyclic ring systems
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14

Abstract

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

Claims

1. A pharmaceutical composition of matter comprising as active substances at least one anticholinergic, at least one corticosteroid and at least one betamimetic, optionally in the form of the enantiomers, mixtures of the enantiomers or in the form of the racemates thereof, optionally in the form of the solvates or hydrates.

2. The pharmaceutical composition of mailer as recited in claim 1 further comprising a pharmaceutically acceptable excipient or carrier.

3. The pharmaceutical composition of matter as recited in claim 1, wherein the active substances are present either together in a single formulation or in two separate formulations.

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

5. The pharmaceutical composition of mailer as recited in claim 4, wherein the anticholinergic is selected from the group consisting of tiotropium salts.

6. The pharmaceutical composition of matter as recited in claim 1, wherein the corticosteroid is selected from the group consisting of flunisolide, beclomethasone, triamcinolone, budesonide, fluticasone, mometasone, ciclesonide, rofleponide, GW 215864, KSR 592, ST-126 and dexamethasone.

7. The pharmaceutical composition of mailer as recited in claim 1, wherein the betamimetic is selected from bambuterol, bitolterol, carbuterol, clenbuterol, fenoterol, formoterol, hexoprenaline, ibuterol, pirbuterol, procaterol, reproterol, saimeterol, sulphonterol, terbutaline, tolubuterol, 4-hydroxy-7-[2-{[2-{[3-(2-phenylethoxy)propyl]sulphonyl}ethyl]-amino}ethyl]-2(3H)-benzothiazolone, 1-(2-fluoro-4-hydroxyphenyl)-2-[4-(1-benzimidazolyl)-2-methyl-2-butylamino]ethanol, 1-[3-(4-methoxybenzyl-amino)-4-hydroxyphenyl]-2-[4-(1-benzimidazolyl)-2-methyl-2-butylamino]ethanol, 1-[2H-5-hydroxy-3-oxo-4H-1,4-benzoxazin-8-yl]-2-[3-(4-N,N-dimethylaminophenyl)-2-methyl-2-propylamino]ethanol, 1-[2H-5-hydroxy-3-oxo-4H-1,4-benzoxazin-8-yl]-2-[3-(4-methoxyphenyl)-2-methyl-2-propylamino]ethanol, 1-[2H-5-hydroxy-3-oxo-4H-1,4-benzoxazin-8-yl]-2-[3-(4-n-butyloxyphenyl)-2-methyl-2-propylamino]ethanol, 1-[2H-5-hydroxy-3-oxo-4H-1,4-benzoxazin-8-yl]-2-{4-[3-(4-methoxyphenyl)-1,2,4-triazol-3-yl]-2-methyl-2-butylamino}ethanol, 5-hydroxy-8-(1-hydroxy-2-isopropylaminobutyl)-2H-1,4-benzoxazin-3-(4H)-one, 1-(4-amino-3-chloro-5-trifluoromethylphenyl)-2-tert.-butlamino)ethanol and 1-(4-ethoxycarbonylamino-3-cyano-5-fluorophenyl)-2-(tert.-butylaminonethanol.

8. The pharmaceutical composition of matter as recited in claim 1, wherein the weight ratio of anticholinergic to corticosteroid is in the range from about 1:

300 to about 50;

1.

9. The pharmaceutical composition of matter as recited in claim 8, wherein the weight ratio of anticholinergic to corticosteroid is in the range from about 1:

250 to about 40;

1.

10. The pharmaceutical composition of matter as recited in claim 1, wherein the weight ratio of anticholinergic to betamimetic is in the range from about 1:

300 to about 30;

1.

11. The pharmaceutical composition of matter as recited in claim 10, wherein the weight ratio of anticholinergic to betamimetic is about 1:

230 to about 20;

1

12. The pharmaceutical composition of matter as recited in claim 11, wherein the weight ratio of anticholinergic to betamimetic Is about 1:

150 to about 10;

1.

13. The pharmaceutical composition of matter as recited in claim 1 which is suitable for inhalation.