Diester prodrugs of a decahydroisoquinoline-3-carboxylic acid
AssigneeEli Lilly and Company
InventorsThomas John Bleisch, Edward Louis Mattiuz, Paul Leslie Ornstein, Robert Eugene Stratford
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Abstract
The present invention relates to novel prodrug forms of 3S,4aR,6S,8aR-6-(((4-carboxy)phenyl)methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid, to pharmaceutical compositions containing the prodrug forms, and to methods of using the prodrug forms.
Claims13
A compound of the formula:
- wherein R1 and R2 are each independently C1-C20 alkyl, C2-C6 alkenyl, C1-C6 alkylaryl, C1-C6 alkyl(C3-C10)cycloalkyl, C1-C6 alkyl-N,N—C1-C6 dialkylamine, C1-C6 alkyl-pyrrolidine, C1-C6 alkyl-piperidine, or C1-C6 alkyl-morpholine;
- or a pharmaceutically acceptable salt thereof.
A compound which is 3S,4aR,6S, 8aR-6-(((4-carboxy)phenyl)methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid, diethyl ester or a pharmaceutically acceptable salt thereof.
A compound which is 3S,4aR,6S,8aR-6-(((4-carboxy)phenyl)methyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid, diethyl ester.
A method of treating pain, which comprises administering to a patient an effective amount of a compound of the formula:
- wherein R1 and R2 are each independently C1-C20 alkyl, C2-C6 alkenyl, C1-C6 alkylaryl, C1-C8 alkyl(C3-C10)cycloalkyl, C1-C6 alkyl-N,N—C1-C6 dialkylamine, C1-C6 alkyl-pyrrolidine, C1-C6 alkyl-piperidine, or C1-C6 alkyl-morpholine;
- or a pharmaceutically acceptable salt thereof.
A method of treating migraine, which comprises administering to a patient an effective amount of a compound of the formula:
- wherein R1 and R2 are each independently C1-C20 alkyl, C2-C6 alkenyl, C1-C6 alkylaryl, C1-C6 alkyl(C3-C10)cycloalkyl, C1-C6 alkyl-N,N—C1-C6 dialkylamine, C1-C6 alkyl-pyrrolidine, C1-C6 alkyl-piperidine, or C1-C6 alkyl-morpholine;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.