N-DESMETHYL-DOXEPIN AND METHODS OF USING THE SAME TO TREAT SLEEP DISORDERS
The invention relates to desmethyldoxepin, isomers of desmethyldoxepin, and pharmaceutically acceptable salts and prodrugs of desmethyldoxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.
1 . A method for treating insomnia comprising administering to a patient desmethyldoxepin, a pharmaceutically acceptable salt thereof, or a prodrug thereof other than doxepin in a daily dosage ranging from about 0.01 to about 500 milligrams.
2 . The method of claim 1 , wherein the pharmaceutically acceptable salt of desmethyldoxepin is the hydrochloride salt thereof.
3 . The method of claim 1 , wherein the prodrug of desmethyldoxepin is a prodrug ester or amide.
4 . The method of claim 1 , wherein the daily dosage is about 20 to about 300 milligrams.
5 . The method of claim 1 , wherein the daily dosage is about 0.1 to about 20 milligrams.
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8 . The method of claim 1 , wherein the insomnia is a chronic insomnia or a non-chronic insomnia.
9 . The method of claim 8 , wherein the non-chronic insomnia is a transient or a short term insomnia.
10 . The method of claim 1 , wherein the insomnia is selected from the group consisting of onset insomnia and maintenance insomnia.
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13 . The method of claim 1 , wherein the desmethyldoxepin, the salt or the prodrug is administered in a cis-(Z) to trans-(E) isomer ratio of about 99:1, 98:2, 95:5, 90:10, 80:20, 70:30, 60:40, 50:50, 40:60, 30:70, 20:80, 10:90, 5:95, 2:98 or 1:99.
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24 . A composition comprising desmethyldoxepin, a pharmaceutically acceptable salt thereof, or a prodrug of desmethyldoxepin other than doxepin in an amount ranging from about 0.01 to about 500 milligrams.
25 . The composition of claim 24 , wherein the amount is about 20 to about 300 milligrams.
26 . The composition of claim 24 , wherein the amount is about 0.1 to about 20 milligrams.
27 . The composition of claim 24 , wherein the amount is about 0.1 to about 10 milligrams.
28 . The composition of claim 24 , wherein the amount is about 0.1 to about 5 milligrams.
29 . The composition of claim 24 , wherein the desmethyldoxepin, salt or prodrug is in a cis-(Z) to trans-(E) isomer ratio of about 99:1, 98:2, 95:5, 90:10, 80:20, 70:30, 60:40, 50:50, 40:60, 30:70, 20:80, 10:90, 5:95, 2:98 or 1:99.
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46 . A method for treating insomnia comprising administering to a patient an isomer of desmethyldoxepin, a pharmaceutically acceptable salt thereof, or a prodrug thereof other than doxepin in a daily dosage ranging from about 0.01 to about 500 milligrams.
47 . (canceled)
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53 . The method of claim 46 , wherein the isomer of desmethyldoxepin, the salt or the prodrug is administered in a cis-(Z) to trans-(E) isomer ratio of about 99:1, 98:2, 95:5, 90:10, 80:20, 70:30, 60:40, 50:50, 40:60, 30:70, 20:80, 10:90, 5:95, 2:98 or 1:99.
54 . (canceled)
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56 . The method of claim 46 , wherein the insomnia is a chronic insomnia or a non-chronic insomnia.
57 . The method of claim 56 , wherein the non-chronic insomnia is a transient or a short term insomnia.
58 . The method of claim 46 , wherein the insomnia is selected from the group consisting of onset insomnia and maintenance insomnia.
59 - 76 . (canceled)