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Medicaments for the treatment of chronic obstructive pulmonary disease

Medicaments for the treatment of chronic obstructive pulmonary disease description/claims

This application is a continuation of U.S. Ser. No. 11/275,730, filed Jan. 26, 2006, which in turn is a Continuation of U.S. Ser. No. 11/132,075, filed May 18, 2005, which in turn is a Continuation of U.S. Ser. No. 10/705,012, filed Nov. 10, 2003, which claims priority to U.S. Ser. No. 60/434,038, filed Dec. 17, 2002, and German Application No. 102 53 282.6 filed Nov. 15, 2003, each of which is hereby incorporated by reference in its entirety.

The present invention relates to the use of the compounds of general formula 1

wherein the groups R1, R2, and R3 may have the meanings given in the claims and in the specification, for preparing a pharmaceutical composition for the treatment of chronic obstructive pulmonary disease (COPD), as well as new compounds of general formula 1 and processes for preparing them.

Betamimetics (β-adrenergic substances) are known from the prior art. Reference may be made, for example, to the disclosures of U.S. Pat. No. 4,460,581, which is hereby incorporated by reference, which proposes betamimetics for the treatment of a variety of complaints.

For drug treatment of diseases it is often desirable to prepare medicaments with a longer duration of activity. As a rule, this ensures that the concentration of the active substance in the body needed to achieve the therapeutic effect is guaranteed for a longer period without the need to re-administer the drug at frequent intervals. Moreover, giving an active substance at longer time intervals contributes to the well-being of the patient to a high degree.

It is particularly desirable to prepare a pharmaceutical composition which can be used therapeutically by administration once a day (single dose). The use of a drug once a day has the advantage that the patient can become accustomed relatively quickly to taking the drug regularly at certain times of the day.

The aim of the present invention is therefore to provide betamimetics which have a therapeutic benefit in the treatment of COPD and are characterized by a longer duration of activity and can thus be used to prepare pharmaceutical compositions with a longer duration of activity. A particular aim of the invention is to prepare betamimetics which, by virtue of their long-lasting effect, can be used to prepare a drug for administration once a day for treating COPD. In addition to the above objectives, the present invention also sets out to provide betamimetics which are not only exceptionally potent but are also characterized by a high degree of selectivity with respect to the β2-adreno-receptor.

Surprisingly it has been found that the abovementioned problems are solved by compounds of general formula 1.

Accordingly, the present invention relates to compounds of general formula 1

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