Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
2001-10-23
2003-03-25
Criares, Theodore J. (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
C514S649000, C514S642000, C514S643000
Reexamination Certificate
active
06538035
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention is a new use for tolterodine and a few other similar compounds to treat asthma, a group of breathing disorders termed Chronic Obstructive Pulmonary Disease (COPD) and allergic rhinitis.
2. Description of the Related Art
U.S. Pat. No. 5,382,600 discloses 2-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-methylphenol also known as N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine with the generic name of tolterodine as being useful to treat urinary incontinence.
Drug Metabolism and Disposition,
26(4), 289-293 (1998) discloses that tolterodine is a muscarinic receptor antagonist.
U.S. Pat. No. 5,559,269 and
Drug Metabolism and Disposition,
26(4), 289-293 (1998) disclose hydroxytolterodine. U.S. Pat. No. 5,559,269 discloses this compound as useful to treat urinary incontinence.
Pharmacol. Toxicol.,
81, 169-172 (1997) discloses that hydroxytolterodine has antimuscarinic activity.
U.S. Pat. No. 6,124,354 discloses 2-(diisopropylamino)ethyl-1-phenylcyclopentanecarboxylate, see Example 99, and its use in treating urinary incontinence and irritable bowel syndrome.
Can. J. Chem.,
40, 1909-1916 (1962) refers to this compound as a potential antidote for treatment of anticholinesterase poisoning.
J. Am. Chem. Soc.,
69, 2902-2906 (1947) while not mentioning the diisopropylamino compound but a diethylamino analog, discusses that the diethylamino compound has antispasmolytic action against acetylcholine.
It is known that antimuscarinic compounds are used in the treatment of asthma and COPD.
The antimuscarinic compound ipratroprium has been approved for use in treating allergic rhinitis.
SUMMARY OF INVENTION
Disclosed is a method of treating a mammal selected from the group consisting of humans and horses that have asthma and are in need of such treatment by inhaling an anti-asthma effective amount of a compound selected from the group consisting of tolterodine, hydroxytolterodine and 2-(diisopropylamino)ethyl-1-phenylcyclopentanecarboxylate or a pharmaceutically acceptable salt thereof.
Also disclosed is a method of treating a mammal selected from the group consisting of humans and horses that have COPD and are in need of such treatment by inhaling an anti-COPD effective amount of a compound selected from the group consisting of tolterodine, hydroxytolterodine and 2-(diisopropylamino)ethyl-1-phenylcyclopentanecarboxylate or a pharmaceutically acceptable salts thereof.
Further disclosed is a method of treating a mammal selected from the group consisting of humans and horses that has allergic rhinitis and is in need of such treatment by inhaling an anti-allergic rhinitis effective amount of a compound selected from the group consisting of tolterodine, hydroxytolterodine and 2-(diisopropylamino)ethyl-1-phenylcyclopentanecarboxylate or a pharmaceutically acceptable salt thereof.
DETAILED DESCRIPTION OF THE INVENTION
U.S. Pat. No. 5,382,600 discloses tolterodine (Example 22) and that it is useful to treat urinary incontinence. Tolterodine is presently being sold in a number of different countries for that purpose. When tolterodine is used to treat urinary incontinence it is administered orally. It is preferred that tolterodine be prepared by the process of International Publication WO98/29402.
Hydroxytolterodine and 2-(diisopropylamino)ethyl-1-phenylcyclopentanecarboxylate are also known compounds. For convenience, these three compounds collectively will be referred to as ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENTS. It is preferred that the ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENT be tolterodine.
The present invention is the use of the ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENTS to treat asthma, COPD and allergic rhinitis.
The method of the present invention is used to treat mammals including humans and horses. It is preferred that the mammal be a human.
The compounds of the present invention are administered by inhalation. The inhalation can be by either an aerosol or a powder.
An anti-asthma, anti-COPD and anti-allergic rhinitis effective amount of ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENTS is from about 0.05 mg to about 12 mg. It is preferred that the anti-asthma, anti-COPD and anti-allergic rhinitis effective amount is from about 0.1 to about 6 mg; it is more preferred that the anti-asthma, anti-COPD and anti-allergic rhinitis effective amount is from about 0.2 to about 5 mg.
The ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENTS can be administered from one thru four times daily. It is preferable to administer the ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENTS two or three times daily, more preferable twice daily.
The minimum amount of an aerosol delivery is about 0.2 ml and the maximum aerosol delivery is about 5 ml. The concentration of the ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENTS is not critical so long as the total amount of spray delivered is within the about 0.2 to about 5 ml amount and it delivers an anti-asthma, anti-COPD and anti-allergic rhinitis effective amount. It is well known to those skilled in the art that if the concentration is higher, one gives a smaller dose to deliver the same “effective amount”. The non-active ingredient or carrier can be (sterile) water with the pH adjusted to where the active anti-asthma pharmaceutical agent is very soluble. It is preferred that the pH be at or near 7. Alternatively and preferably, the non-active carrier agent should be physiological saline with the pH adjusted appropriately. Aerosols for inhalation of various pharmaceutical agents are well known to those skilled in the art including many aerosols for treating asthma, COPD and allergic rhinitis. There is nothing special in the present invention regarding the aerosol.
Alternatively the dosage form for inhalation can be a powder. Powders for inhalation of various pharmaceutical agents are well known to those skilled in the art including many powders for treating asthma, COPD and allergic rhinitis. There is nothing special in the present invention regarding the powder. When the dosage form is a powder, the active pharmaceutical agent can be administered in pure form or diluted with an inert carrier. When an inert carrier is used, the ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENT pharmaceutical agent is compounded such that the total amount of powder delivered delivers an “effective amount” of the ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENT. The actual concentration of the ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENT is not critical. If the concentration is lower, then more powder must be delivered; if the concentration is higher, less total material must be delivered to provide an effective amount of one of the ANTI-ASTHMA/ANTI-COPD/ANTI-ALLERGIC RHINITIS AGENTS.
Various devices are on the market for administering powders for inhalation for asthma, COPD and allergic rhinitis and these devices are suitable for administering the compounds of the present invention.
Pharmaceutically acceptable salts include salts of both inorganic and organic acids. The pharmaceutically acceptable salts are preferred over the corresponding free amines since they produce compounds that are more water soluble and more crystalline. The preferred pharmaceutically acceptable salts include salts of the following acids hydrochloric, hydrobromic, sulfuric, phosphoric, nitric, citric, methanesulfonic CH
3
—(CH
2
)
n1
—COOH where n
1
is 0 thru 4, HOOC—(CH
2
)n
1
—COOH where n is as defined above, HOOC—CH═CH—COOH, &phgr;-COOH. For other acceptable salts, see
Int. J. Pharm.,
33, 201-217 (1986).
DEFINITIONS
All temperatures are in degrees Celsius.
COPD refers to Chronic Obstructive Pulmonary Disease.
Allergic rhinitis refers to acute rhinitis or nasal rhinitis.
Tolterodine refers to 2-[(1R)-3-(diisopropylamino)-1-phenylpropyl]-4-methylphenol also known as N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine, a compound of the formula:
Hydroxytolterodine refers to 2-[(1R)-3-(diisopropylamino)-1-phenylpropyl&rsq
Cammarata Sue K.
Gillberg Per-Goran
Sundquist Staffan
Criares Theodore J.
Pharmacia & Upjohn Company
Zhang Austin W.
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