Methods and compositions for treating pulmonary disorders using optically pure (R,R)-formoterol

• US 6,866,839 B2
• Filed: 06/09/2003
• Issued: 03/15/2005
• Est. Priority Date: 04/05/1991
• Status: Expired due to Fees

• Current Assignee: Sunovion Pharmaceuticals Inc. (Sumitomo Chemical Company Limited)
• Original Assignee: Sepracor Incorporated
• Inventors: Aberg, Gunnar, Morley, John
• Primary Examiner(s): Kunz, Gary
• Assistant Examiner(s): Haghighatian, Mina
• Application Number:
  US10/457,123
• Publication Number:
  US 20030203970A1
• Time in Patent Office: 645 Days
• Field of Search: 424/45, 424/46, 424/489, 424/400, 424/443, 424/464, 424/451, 514/826
• US Class Current: 424/45
• 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 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/16 Amides, e.g. hydroxamic acids
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/17 having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine isoureas, isothioureas A61K31/155; sulfonylureas A61K31/64
• CPC Class Codes: A61K 31/235 having an aromatic ring attached to a carboxyl group
• CPC Class Codes: A61K 31/27 of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/47 Quinolines; Isoquinolines
• CPC Class Codes: A61K 31/52 Purines, e.g. adenine
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

Abstract

A method and composition are disclosed utilizing the pure (R,R) isomer of formoterol, which is a potent bronchodilator with reduced adverse effects, a low incidence of the development of tolerance and an increased duration of action, as compared to racemic formoterol.

Claims

1. A method for treating chronic obstructive pulmonary disease in a human in need of such therapy, the method comprising administering to the human a therapeutically effective amount of (R,R)-formoterol, or a pharmaceutically acceptable salt thereof, the (R,R)-formoterol containing at least 90% by weight of (R,R)-formoterol and less than 10% by weight of (S,S)-formoterol.

2. The method of claim 1, wherein the (R,R)-formoterol is administered by subcutaneous injection, intravenous infusion, inhalation, transdermal delivery or oral administration.

3. The method of claim 2, wherein the (R,R)-formoterol or pharmaceutically acceptable salt thereof is administered together with a pharmaceutically acceptable carrier.

4. The method of claim 2, wherein the (R,R)-formoterol is administered as the fumarate dehydrate salt.

5. The method of claim 2, wherein the (R,R)-formoterol is administered by inhalation and the amount administered is about 1 μ

g to about 100 μ

g per day, in single or divided doses.

6. The method of claim 5, wherein the amount administered is about 6 μ

g to about 25 μ

g per day, in single or divided doses.

7. The method of claim 6, wherein the amount administered is about 12 μ

g to about 25 μ

g per day, in single or divided doses.

8. The method of claim 7, wherein the amount is administered in from two to four divided doses.

9. The method of claim 2, wherein the (R,R)-formoterol is administered by orally and the amount administered is about 0.1 mg to about 1 mg per day.

10. A method for treating chronic obstructive pulmonary disease in a human in need of such therapy, the method comprising administering to the human a therapeutically effective amount of (R,R)-formoterol, or a pharmaceutically acceptable salt thereof, the (R,R)-formoterol containing at least 90% by weight of (R,R)-formoterol and less than 10% by weight of (S,S)-formoterol, and wherein the amount of (R,R)-formoterol is sufficient to treat COPD, but insufficient to cause adverse effects associated with racemic formoterol.

11. The method of claim 10, wherein the (R,R)-formoterol is administered by subcutaneous injection, intravenous infusion, inhalation, transdermal delivery or oral administration.

12. The method of claim 11, wherein the (R,R)-formoterol or pharmaceutically acceptable salt thereof is administered together with a pharmaceutically acceptable carrier.

13. The method of claim 11, wherein the (R,R)-formoterol is administered as the fumarate dehydrate salt.

14. The method of claim 11, wherein the (R,R)-formoterol is administered by inhalation and the amount administered is about 1 μ

g to about 100 μ

g per day, in single or divided doses.

15. The method of claim 14, wherein the amount administered is about 6 μ

g to about 25 μ

g per day, in single or divided doses.

16. The method of claim 15, wherein the amount administered is about 12 μ

g to about 25 μ

g per day, in single or divided doses.

17. The method of claim 16, wherein the amount is administered in from two to four divided doses.

18. The method of claim 11, wherein the (R,R)-formoterol is administered by orally and the amount administered is about 0.1 mg to about 1 mg per day.