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Details for Patent: 6,268,358

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Details for Patent: 6,268,358

Title: Compounds for the treatment of Alzheimer's disease
Abstract:Analogs of galanthamine having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydroxyl, alkoxy, aryloxy, alkyl carbonate, phenyl carbonate, benzyl carbonate, aliphatic carbamate, aryl carbamate and alkanoyloxy groups wherein said phenyl, aryl or benzyl groups may optionally be substituted by an R.sup.5 group selected from the group consisting of alkyl, alkoxy, fluoro, chloro, bromo and trifluoromethyl groups and R.sub.3 is selected from the group consisting of hydrogen and straight or branched chain carbon atoms of from one to six carbon atoms and alkyl phenyl groups are useful in the treatment of Alzheimer's disease and related dementias.
Inventor(s): Davis; Bonnie (Syosset, NY), Joullie; Madeleine M. (Philadelphia, PA)
Assignee: Davis; Bonnie (Syosset, NY)
Filing Date:Jun 07, 1995
Application Number:08/473,712
Claims:1. A method for treating patients suffering from Alzheimer's disease or a related dementia characterized by a cholinergic deficiency or dementias accompanied by plaques and tangles in the brain which comprises administering to a patient suffering from such a disease a therapeutically effective amount of a compound other than galanthamine of the formula: ##STR55##

wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen, hydroxyl alkoxy of 1-6 carbon atoms, aryloxy, alkyl carbamate, aryl carbamate and alkanoyloxy groups, wherein said aryl groups may optionally be substituted by an R.sup.5 group selected from the group consisting of alkyl, alkoxy, fluoro, chloro, bromo and trifluoromethyl groups and R.sub.3 is selected from the group consisting of hydrogen and straight or branched chain alkyl groups of from one to six carbon atoms and alkyl phenyl groups.

2. A method according to claim 1 wherein R.sub.1 is hydroxy.

3. A method according to claim 1 wherein at least one of R.sub.1 and R.sub.2 is alkanoyloxy.

4. A method according to claim 3 wherein at least one of R.sub.1 and R.sub.2 is acetoxy.

5. A method according to claim 1 wherein at least one of R.sub.1 and R.sub.2 is a carbamate, group.

6. A method according to claim 1 wherein the compound is galanthamine acetate.

7. A method according to claim 1 wherein at least one of R.sub.1 and R.sub.2 is alkoxy.

8. A method as claimed in claim 1 wherein R.sub.1 is selected from the group consisting of hydrogen, methoxy, ethoxy and alkanoyloxy R.sub.2 is selected from the group consisting of methoxy, ethoxy and alkanoyloxy and R.sub.3 is selected from the group consisting of straight or broad chain alkyl groups of from one to six carbon atoms and alkyl phenyl groups.

9. A method of inhibiting acetylcholinesterase in a mammalian host which comprises administering to said host an acetylcholinesterase inhibiting amount of a compound other than galanthamine of the formula: ##STR56##

wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen, hydroxyl, alkoxy of 1-6 carbon atoms, aryloxy, aryl carbamate, aryl carbamate and alkanoyloxy groups, wherein said aryl groups may optionally be substituted by an R.sup.5 group selected from the group consisting of alkyl, alkoxy, fluoro, chloro, bromo and trifluoromethyl groups and R.sub.3 is selected from the group consisting of hydrogen and straight or branched chain alkyl groups of from one to six carbon atoms and alkyl phenyl groups.

10. A method according to claim 9 wherein R.sub.1 is hydroxy.

11. A method according to claim 9 wherein at least one of R.sub.1 and R.sub.2 is alkanoyloxy.

12. A method according to claim 9 wherein at least one of R.sub.1 and R.sub.2 is acetoxy.

13. A method according to claim 9 wherein at least one of R.sub.1 and R.sub.2 is a carbamate group.

14. A method according to claim 9 wherein the compound is galanthamine acetate.

15. A method for treating patients suffering from Alzheimer's disease which comprises administering to a patient suffering from such a disease a therapeutically effective amount of a compound other than galanthamine of the formula: ##STR57##

wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen, hydroxyl, alkoxy of 1-6 carbon atoms, aryloxy, alkyl carbamate, aryl carbamate and alkanoyloxy groups, wherein said aryl groups may optionally be substituted by an R.sup.5 group selected from the group consisting of alkyl, alkoxy, fluoro, chloro, bromo and trifluoromethyl groups and R.sub.3 is selected from the group consisting of hydrogen and straight or branched chain alkyl groups of from one to six carbon atoms and alkyl phenyl groups.

16. A method according to claim 15 wherein R.sub.1 is hydroxy.

17. A method according to claim 15 wherein at least one of R.sub.1 and R.sub.2 is alkanoyloxy.

18. A method according to claim 17 wherein at least one of R.sub.1 and R.sub.2 is acetoxy.

19. A method according to claim 15 wherein at least one of R.sub.1 and R.sub.2 is a carbamate group.

20. A method according to claim 15 wherein the compound is galanthamine acetate.

21. A method according to claim 15 wherein at one of R.sub.1 and R.sub.2 is alkoxy.

22. A method for treating patients suffering from Alzheimer's disease or a related dementia characterized by a cholinergic deficiency or dementias accompanied by plaques and tangles in the brain which comprises administering to a patient suffering from such a disease a therapeutically effective amount of a compound other than galanthamine of the formula: ##STR58##

wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen, hydroxyl, alkoxy of 1-6 carbon atoms, C.sub.1-6 alkyl carbonate, phenyl carbonate, benzyl carbonate, alkyl carbamate of from 1-6 carbon atoms, phenyl carbamate and alkanoyloxy groups, wherein said phenyl or benzyl groups may optionally be substituted by an R.sup.5 group selected from the group consisting of alkyl, alkoxy, fluoro, chloro, bromo and trifluoromethyl groups and R.sub.3 is selected from the group consisting of hydrogen and straight or branched chain alkyl groups of from one to six carbon atoms and alkyl phenyl groups.

23. A method of inhibiting acetylcholinesterase in a mammalian host which comprises administering to said host an acetylcholinesterase inhibiting amount of a compound other than galanthamine of the formula: ##STR59##

wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen, hydroxyl, alkoxy of 1-6 carbon atoms, C.sub.1-6 alkyl carbonate, phenyl carbonate, benzyl carbonate, alkyl carbamate of from 1-6 carbon atoms, phenyl carbamate and alkanoyloxy groups, wherein said phenyl or benzyl groups may optionally be substituted by an R.sup.5 group selected from the group consisting of alkyl, alkoxy, fluoro, chloro, bromo and trifluoromethyl groups and R.sub.3 is selected from the group consisting of hydrogen and straight or branched chain alkyl groups of from one to six carbon atoms and alkyl phenyl groups.

24. A method for treating patients suffering from Alzheimer's disease which comprises administering to a patient suffering from such a disease a therapeutically effective amount of a compound other than galanthamine of the formula: ##STR60##

wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen, hydroxyl, alkoxy of 1-6 carbon atoms, C.sub.1-6 alkyl carbonate, phenyl carbonate, benzyl carbonate, alkyl carbamate of from 1-6 carbon atoms, phenyl carbamate and alkanoyloxy groups, wherein said phenyl or benzyl groups may optionally be substituted by an R.sup.5 group selected from the group consisting of alkyl, alkoxy, fluoro, chloro, bromo and trifluoromethyl groups and R.sub.3 is selected from the group consisting of hydrogen and straight or branched chain alkyl groups of from one to six carbon atoms and alkyl phenyl groups.

25. A method according to claim 4 wherein at least one of R.sub.1 and R.sub.2 is a carbonate.

26. A method according to claim 24 wherein at least one of R.sup.1 and R.sup.2 is a carbonate.
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