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Generated: November 19, 2017

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Title: Medicament compositions derived from quinolizine and quinolizinone and methods of use thereof
Abstract:The present invention is directed to the use of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and hexahydro-8-hydroxy-2,6-methano-2H-quinolizines in the manufacture of a medicament for the treatment of anxiety, psychosis, glaucoma and for the stimulation of gastric motility.
Inventor(s): Gittos; Maurice W. (Plobsheim, FR), Miller; Francis P. (Loveland, OH), Sorensen; Stephen M. (Cincinnati, OH), Fozard; John R. (Hegenheim, FR), Moser; Paul (Strasbourg, FR), Palfreyman; Michael G. (Cincinnati, OH), Cheng; Hsien (Cincinnati, OH)
Assignee: Merrell Dow Pharmaceuticals Inc. (Cincinnati, OH)
Filing Date:May 16, 1990
Application Number:07/527,676
Claims:1. A pharmaceutical composition suitable for use in the treatment of anxiety, psychosis, glaucoma, and for stimulating gastric motility comprising a pharmaceutically acceptable carrier in admixture with a compound of the formula ##STR7## wherein A is H.sub.2, O, (H)(OH), (OH).sub.2 or N--OH; B is H.sub.2, (H)(CH.sub.3), (H)(CH.sub.2 NR.sub.3 R.sub.4) or CH.sub.2 wherein R.sub.3 and R.sub.4 are C.sub.2-4 alkyl or are combined to give tetramethylene, pentamethylene or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 ; R.sub.1 is ##STR8## wherein Z is NR.sub.9, O or S; R.sub.5, R.sub.6 and R.sub.8 are each hydrogen, halogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxy; R.sub.7 is hydrogen, amino, (C.sub.1-4 alkyl)amino, (C.sub.1-4 alkyl).sub.2 amino, alkoxy, or nitro; R.sub.9 is hydrogen, C.sub.1-4 alkyl or phenyl (C.sub.1-2 alkyl); R.sub.10 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl, cyano or --CONH.sub.2 ; R.sub.11 is hydrogen, halogen, C.sub.1-4 alkyl or phenyl; the wavy line indicates that the configuration of the oxygen substituent on the ring can be endo or exo; and the pharmaceutically acceptable acid addition and quarternary ammonium salts of the aforesaid compounds.

2. A pharmaceutical composition according to claim 1 wherein said compound is endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-on e.

3. A method for the treatment of anxiety comprising administering to a patient in need thereof of an effective amount of a compound of the formula ##STR9## wherein A is H.sub.2, O, (H)(OH), (OH).sub.2 or N--OH; B is H.sub.2, (H)(CH.sub.3), (H)(CH.sub.2 NR.sub.3 R.sub.4) or CH.sub.2 wherein R.sub.3 and R.sub.4 are C.sub.2-4 alkyl or are combined to give tetramethylene, pentamethylene or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --; R.sub.1 is ##STR10## wherein Z is NR.sub.9, O or S; R.sub.5, R.sub.6 and R.sub.8 are each hydrogen, halogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxy; R.sub.7 is hydrogen, amino, (C.sub.1-4 alkyl)amino, (C.sub.1-4 alkyl).sub.2 amino, alkoxy or nitro; R.sub.9 is hydrogen, C.sub.1-4 alkyl or phenyl (C.sub.1-2 alkyl); R.sub.10 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, cyano or --CONH.sub.2 ; R.sub.11 is hydrogen, halogen, C.sub.1-4 alkyl or phenyl; the wavy line indicates that the configuration of the oxygen substituent on the ring can be endo or exo; and the pharmaceutically acceptable acid addition and quarternary ammonium salts of the aforesaid compounds.

4. A method according to claim 3 wherein said compound is endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-on e.

5. A method for the treatment of psychosis comprising administering to a patient in need thereof an effective amount of a compound of the formula ##STR11## wherein A is H.sub.2, O, (H)(OH), (OH).sub.2 or N--OH; B is H.sub.2, (H)(CH.sub.3), (H)(CH.sub.2 NR.sub.3 R.sub.4) or CH.sub.2 wherein R.sub.3 and R.sub.4 are C.sub.2-4 alkyl or are combined to give tetramethylene, pentamethylene or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --; R.sub.1 is ##STR12## wherein Z is NR.sub.9, O or S; R.sub.5, R.sub.6 and R.sub.8 are each hydrogen, halogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxy; R.sub.7 is hydrogen, amino, (C.sub.1-4 alkyl)amino, (C.sub.1-4 alkyl).sub.2 amino, alkoxy or nitro; R.sub.9 is hydrogen, C.sub.1-4 alkyl or phenyl (C.sub.1-2 alkyl); R.sub.10 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, cyano or --CONH.sub.2 ; R.sub.11 is hydrogen, halogen, C.sub.1-4 alkyl or phenyl; the wavy line indicates that the configuration of the oxygen substituent on the ring can be endo or exo; and the pharmaceutically acceptable acid addition and quarternary ammonium salts of the aforesaid compounds.

6. A method according to claim 5 wherein said compound is endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-on e.

7. A method for stimulating gastric motility comprising administering to a patient in need thereof an effective amount of a compound of the formula: ##STR13## wherein A is H.sub.2, O, (H)(OH), (OH).sub.2 or N--OH; B is H.sub.2, (H)(CH.sub.3), (H)(CH.sub.2 NH.sub.3 R.sub.4) or CH.sub.2 wherein R.sub.3 and R.sub.4 are C.sub.2-4 alkyl or are combined to give tetramethylene, pentamethylene or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --; R.sub.1 is ##STR14## wherein Z is NR.sub.9, O or S; R.sub.5, R.sub.6 and R.sub.8 are each hydrogen, halogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxy; R.sub.7 is hydrogen, amino, (C.sub.1-4 alkyl)amino, (C.sub.1-4 alkyl).sub.2 amino, alkoxy or nitro; R.sub.9 is hydrogen, C.sub.1-4 alkyl or phenyl (C.sub.1-2 alkyl); R.sub.10 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, cyano or --CONH.sub.2 ; R.sub.11 is hydrogen, halogen, C.sub.1-4 alkyl or phenyl; the wavy line indicates that the configuration of the oxygen substituent on the ring can be endo or exo; and the pharmaceutically acceptable acid addition and quarternary ammonium salts of the aforesaid compounds.

8. A method according to claim 7 wherein said compound is endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-on e.

9. A method for the treatment of glaucoma comprising administering to a patient in need thereof an effective amount of a compound of the formula: ##STR15## wherein A is H.sub.2, O, (H)(OH), (OH).sub.2 or N--OH; B is H.sub.2, (H)(CH.sub.3), (H)(CH.sub.2 NR.sub.3 R.sub.4) or CH.sub.2 wherein R.sub.3 and R.sub.4 are C.sub.2-4 alkyl or are combined to give tetramethylene, pentamethylene or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --; R.sub.1 is ##STR16## wherein Z is NR.sub.9, O or S; R.sub.5, R.sub.6 and R.sub.8 are each hydrogen, halogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxy; R.sub.7 is hydrogen, amino, (C.sub.1-4 alkyl)amino, (C.sub.1-4 alkyl).sub.2 amino, alkoxy or nitro; R.sub.9 is hydrogen, C.sub.1-4 alkyl or phenyl (C.sub.1-2 alkyl); R.sub.10 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, cyano or --CONH.sub.2 ; R.sub.11 is hydrogen, halogen, C.sub.1.varies.4 alkyl or phenyl; the wavy line indicates that the configuration of the oxygen substituent on the ring can be endo or exo; and the pharmaceutically acceptable acid addition and quarternary ammonium salts of the aforesaid compounds.

10. A method according to claim 9 wherein said compound is endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-on e.

11. A pharmaceutical composition according to claim 1 wherein said compound is endo-8-(3-indolylcarbonyl-oxy)-2,6-methanooctahydro-2H-quinolizin-3-ol.

12. A method according to claim 3 wherein said compound is endo-8-(3-indolylcarbonyl-oxy)-2,6-methanooctahydro-2H-quinolizin-3-ol.

13. A method according to claim 5 wherein said compound is endo-8-(3-indolylcarbonyl-oxy)-2,6-methanooctahydro-2H-quinolizin-3-ol.

14. A method according to claim 7 wherein said compound is endo-8-(3-indolylcarbonyl-oxy)-2,6-methanooctahydro-2H-quinolizin-3-ol.

15. A method according to claim 9 wherein said compound is endo-8-(3-indolylcarbonyl-oxy)-2,6-methanooctahydro-2H-quinolizin-3-ol.
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