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Claims for Patent: 4,761,418

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Claims for Patent: 4,761,418

Title: Novel compounds
Abstract:Neuromuscular blocking agents of formula (1) which are useful as skeletal muscle relaxants during surgery are disclosed. ##STR1## and X is an anion, preferably pharmaceutically acceptable.
Inventor(s): Swaringen, Jr.; Roy A. (Durham, NC), El-Sayad; Hassan A. (Nasr City, EG), Yeowell; David A. (Chapel Hill, NC), Savarese; John J. (Boxford, MA)
Assignee: Burroughs Wellcome Co. (Research Triangle Park, NC) General Hospital Corporation (Boston, MA)
Application Number:06/756,025
Patent Claims: 1. 2,2'[( E)-4-Octenedioylbis(oxytrimethylene)]bis[(trans)-1,2,3,4-tetrahydro-6,7-dim ethoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)isoquinolinium] cation in association with a pharmaceutically acceptable anion.

2. 2,2'-[(E)-4-Octenedioylbis(oxytrimethylene)]bis[(tr ans)-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)is oquinolinium]dichloride.

3. (+-)trans,trans-2,2'- (Z)-4-Octenedioylbis(oxytrimethylene))bis-(1,2,3,4-tetrahydro-6,7-dimethoxy -2-methyl-1-(3,4,5-trimethoxybenzyl)isoquinolinium cation in association with a pharmaceutically acceptable anion.

4. (+-)trans,trans-2,2'-(Z)-4-Octenedioylb is(oxytrimethylene))bis-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-(3,4,5 -trimethoxybenzyl)isoquinolinium dichloride.

5. (E)-(1R,1'R)-2,2'-[4-Octenedioylbis(oxytr imethylene)]bis[1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-(3,4,5-trimetho xybenzyl)isoquinolinium] cation in association with a pharmaceutically acceptable anion.

6. (E)-(1R,1'R)-2, 2'-[4-Octenedioylbis(oxytrimethylene)]bis[1,2,4,3-tetrahydro-6,7-dimethoxy- 2-methyl-1-(3,4,5-trimethoxybenzyl)isoquinolinium]dichloride.

7. (E)-(1R,1'R,2R,2'R)-2,2'-[4-Octenedioylbis(oxytrimethylene )]bis[1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)i soquinolinium]cation in association with a pharmaceutically acceptable anion.

8. (E)- (1R,1'R,2R,2'R)-2,2'-[4-Octenedioylbis(oxytrimethylene)]bis[1,2,3,4-tetrahy dro-6,7-dimethoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)isoquinolinium]dichlor ide.

9. ( E)-(1R,1'R,2R,2'S)-2,2'-[4-Octenedioylbis(oxytrimethylene)]bis[1,2,3,4-tetr ahydro-6,7-dimethoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)isoquinolinium] cation in association with a pharmaceutically acceptable anion.

10. (E)-(1R,1'R,2R,2'S)-2,2'-[4-Octenedioylbis(oxytrimethylene)] bis[1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)iso quinolinium]chloride.

11. (E)-(1R,1'R,2S,2' S)-2,2'-[4-Octenedioylbis(oxytrimethylene)]bis[1,2,3,4-tetrahydro-6,7-dimet hoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)isoquinolinium] dication in association with a pharmaceutically acceptable anion.

12. (E)-(1R,1'R,2S,2'S)-2,2'-[4-Octenedioylbis(oxytrim ethylene)]bis[1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-(3,4,5-trimethoxy benzyl)isoquinolinium]dichloride.

13. A method for producing muscle relaxation in a mammal which comprises parenterally administering to a mammal an effective muscle relaxant amount of the compound of claim 1, 3 or 5.

14. A sterile pharmaceutical composition comprising one or more of the compounds of claims 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 in an effective muscle relaxant amount and a pharmaceutically acceptable solvent therefor.

15. A method for producing muscle relaxation in a mammal which comprises parenterally administering to a mammal an effective muscle relaxant amount of one or more of the compounds of claims 9, 10, 11 or 12.
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