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Last Updated: April 19, 2024

Claims for Patent: 6,444,708


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Summary for Patent: 6,444,708
Title: Treatment using venlafaxine
Abstract:This invention provides a method of treating obesity, generalized anxiety disorder, post-traumatic stress disorder, late luteal phase disphoric disorder (premenstrual syndrome), attention deficit disorder, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa or Shy Drager Syndrome in a mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine of the following structural formula: ##STR1## in which A is a moiety of the formula ##STR2## where the dotted line represents optional unsaturation; R.sub.1 is hydrogen or alkyl; R.sub.2 is alkyl; R.sub.4 is hydrogen, alkyl, formyl, or alkanol; R.sub.5 and R.sub.6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy; R.sub.7 is hydrogen or alkyl; and n is 0, 1, 2, 3, or 4; or a pharmaceutically acceptable salt thereof.
Inventor(s): Rudolph; Richard L. (Berwyn, PA), Derivan; Albert T. (Villanova, PA), Upton; G. Virginia (Radnor, PA)
Assignee: Wyeth (Madison, NJ)
Application Number:09/769,998
Patent Claims: 1. A method of treating generalized anxiety disorder in a mammal, the method comprising administering to a mammal in need thereof an effective amount of a compound of the structural formula: ##STR6##

in which A is a moiety of the formula ##STR7##

where the dotted line represents optional unsaturation; R.sub.1 is hydrogen or alkyl of 1 to 6 carbon atoms; R.sub.2 is alkyl of 1 to 6 carbon atoms; R.sub.4 is hydrogen, alkyl of 1 to 6 carbon atoms, formyl, or alkanol of 2 to 7 carbon atoms; R.sub.5 and R.sub.6 are independently hydrogen, hydroxyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkanoyloxy of 2 to 7 carbon atoms, cyano, nitro, alkylmercapto of 1 to 6 carbon atoms, amino, alkyl-amino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group is of 1 to 6 carbon atoms, alkanamido of 2 to 7 carbon atoms, halo, trifluoromethyl, or when taken together, methylene dioxy; R.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms; and n is one of the integers 0, 1, 2, 3, or 4;

or a pharmaceutically acceptable salt thereof.

2. A method of treating generalized anxiety disorder in a human, the method comprising administering to a human in need thereof an effective amount of a compound of the structural formula: ##STR8##

in which A is a moiety of the formula ##STR9##

where the dotted line represents optional unsaturation; R.sub.1 is hydrogen or alkyl of 1 to 6 carbon atoms; R.sub.2 is alkyl of 1 to 6 carbon atoms; R.sub.4 is hydrogen, alkyl of 1 to 6 carbon atoms, formyl, or alkanol of 2 to 7 carbon atoms; R.sub.5 and R.sub.6 are independently hydrogen, hydroxyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkanoyloxy of 2 to 7 carbon atoms, cyano, nitro, alkylmercapto of 1 to 6 carbon atoms, amino, alkyl-amino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group is of 1 to 6 carbon atoms, alkanamido of 2 to 7 carbon atoms, halo, trifluoromethyl, or when taken together, methylene dioxy; R.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms; and n is one of the integers 0, 1, 2,3, or 4;

or a pharmaceutically acceptable salt thereof.

3. A method of treating generalized anxiety disorder in a human, the method comprising administering to a human in need thereof a pharmaceutical composition comprising an effective amount of a compound of the structural formula: ##STR10##

in which A is a moiety of the formula ##STR11##

where the dotted line represents optional unsaturation; R.sub.1 is hydrogen or alkyl of 1 to 6 carbon atoms; R.sub.2 is alkyl of 1 to 6 carbon atoms; R.sub.4 is hydrogen, alkyl of 1 to 6 carbon atoms, formyl, or alkanol of 2 to 7 carbon atoms; R.sub.5 and R.sub.6 are independently hydrogen, hydroxyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkanoyloxy of 2 to 7 carbon atoms, cyano, nitro, alkylmercapto of 1 to 6 carbon atoms, amino, alkyl-amino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group is of 1 to 6 carbon atoms, alkanamido of 2 to 7 carbon atoms, halo, trifluoromethyl, or when taken together, methylene dioxy; R.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms; and n is one of the integers 0, 1, 2, 3, or 4;

or a pharmaceutically acceptable salt thereof, and a carrier.

4. A method according to claim 3 wherein the effective amount comprises a daily dose of between about 50 mg/day and about 375 mg/day.

5. A method according to claim 3 wherein R4 is formyl or alkanoyl of 2 to 7 carbon atoms.

6. A method of treating generalized anxiety disorder in a human, the method comprising administering to a human in need thereof an effective amount of the compound 1-[(2-dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol or a pharmaceutically acceptable salt thereof.

7. A method of treating generalized anxiety disorder in a human, the method comprising administering to a human in need thereof a pharmaceutical composition containing an effective amount of 1-[(2-dimethylamino)-1-(4-methoxyphenyl)-ethyl]cyclohexanol or a pharmaceutically acceptable salt thereof and a carrier.

8. A method according to claim 3, wherein the pharmaceutical composition is in tablet form.

9. A method according to claim 3, wherein the pharmaceutical composition is in capsule form.

10. A method according to claim 1, wherein the effective amount comprises a daily dose of between about 50 mg/day and about 375 mg/day.

11. A method according to claim 1, wherein the effective amount comprises a daily dose of between about 75 mg/day and about 200 mg/day.

12. A method according to claim 1, wherein the effective amount comprises a daily dose of about 75 mg/day.

13. A method according to claim 1, wherein the compound is 1-[(2-dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride.

14. A method according to claim 1, wherein the compound is (R/S)-1-[(2-dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride.

15. A method of treating generalized anxiety disorder in a human, the method comprising administering orally to a human in need thereof an effective amount of 1-[(2-dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol or a pharmaceuticallly acceptable salt thereof.

16. A method of treating generalized anxiety disorder in a human, the method comprising administering orally to a human in need thereof a pharmaceutical composition containing an effective amount of 1-[(2-dimethylamino)-1-(4-methoxyphenyl)ethyl]-cyclohexanol or a pharmaceutically acceptable salt thereof, and a carrier.

17. A method according to claim 2, wherein the effective amount comprises a daily dose of between about 50 mg/day to and about 375 mg/day.

18. A method according to claim 2, wherein the effective amount comprises a daily dose of between about 75 mg/day and about 200 mg/day.

19. A method according to claim 2, wherein the effective amount comprises a daily dose of about 75 mg/day.

20. A method of treating generalized anxiety disorder in a mammal, the method comprising administering to a mammal in need thereof a pharmaceutical composition comprising an effective amount of a compound of the structural formula: ##STR12##

in which A is a moiety of the formula ##STR13##

where the dotted line represents optional unsaturation; R.sub.1 is hydrogen or alkyl of 1 to 6 carbon atoms; R.sub.2 is alkyl of 1 to 6 carbon atoms; R.sub.4 is hydrogen, alkyl of 1 to 6 carbon atoms, formyl, or alkanol of 2 to 7 carbon atoms; R.sub.5 and R.sub.6 are independently hydrogen, hydroxyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkanoyloxy of 2 to 7 carbon atoms, cyano, nitro, alkylmercapto of 1 to 6 carbon atoms, amino, alkyl-amino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group is of 1 to 6 carbon atoms, alkanamido of 2 to 7 carbon atoms, halo, trifluoromethyl, or when taken together, methylene dioxy; R.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms; and n is one of the integers 0, 1, 2, 3, or 4;

or a pharmaceutically acceptable salt thereof, and a carrier.

21. A method according to claim 20, wherein the pharmaceutical compositon is in tablet form.

22. A method according to claim 20, wherein the pharmaceutical composition is in capsule form.

23. A method according to claim 2, wherein the compound is 1-[(2-dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride.

24. A method according to claim 2, wherein the compound is (R/S)-1-[(2-dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride.

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