N-(2-benzimidazolyl)-piperazines
AssigneeAbbott Laboratories
InventorsMartin Winn, Jaroslav Kyncl
Life of this patent
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Abstract
Disclosed are compounds of the formula ##STR1## wherein n is 2 or 3, R is hydrogen or methyl, R' is C.sub.1 -C.sub.6 alkyl, acyl, aryl, aroyl, alkoxycarbonyl, tetrahydrofuroyl, dialkylaminocarbonyl, or furoyl, and R" is hydrogen and methoxy. These compounds are useful as antihypertensive agents.
Claims13
A compound of the formula:
- ##STR13## wherein:
- n is 2;
- R is selected from the group consisting of hydrogen or methyl;
- R' is C.sub.1 -C.sub.6 alkyl, 4-methyl valeroyl, phenyl, dimethoxyphenyl, CF.sub.3 -phenyl, tetrahydrofuroyl, Furoyl, ##STR14## or C.sub.2 -C.sub.4 alkoxy carbonyl and R" is selected from the group consisting of hydrogen or methoxy.
A compound selected from the group consisting of 1-(5,6-Dimethoxy-2-benzimidazolyl)-4-(2-furoyl) piperazine, 4-(5,6-Dimethoxy-2-benzimidazolyl) piperazine-1-carboxylic ethyl ester, 1-(5,6-Dimethoxy-1-methyl-2-benzimidazolyl)-4-(2-furoyl) piperazine, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4 (tetrahydro-2-furoyl) piperazine, 4-(5,6-Dimethoxy-2-benzimidazolyl) piperazine-1-carboxylic acid isobutyl ester, N,N-Dimethyl 4-(5,6-dimethoxy-2-benzimidazole piperazine-1-carboxamide, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4 (3,4-dimethoxy-phenyl) piperazine, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4(4-methylvaleroyl) piperazine, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4(3-trifluoromethyl phenyl) piperazine, 1-methyl 4(2-benzimidazolyl) piperazine and pharmaceutically acceptable acid addition salts thereof.
A compound selected from the group consisting of:
- 1-(5,6-Dimethoxy-2-benzimidazolyl)-4-(2-furoyl) piperazine, 4-(5,6-Dimethoxy-2-benzimidazolyl) piperazine-1-carboxylic ethyl ester, 4-(5,6-Dimethoxy-2-benzimidazolyl) piperazine-1-carboxylic acid isobutyl ester, and 1-(5,6-Dimethoxy-2-benzimidazolyl)-4(3,4-dimethoxy-phenyl) piperazine.
An antihypertensive pharmaceutical composition comprising a compound selected from the group consisting of 1-(5,6-Dimethoxy-2-benzimidazolyl)-4-(2-furoyl) piperazine, 4-(5,6-Dimethoxy-2-benzimidazolyl) piperazine-1-carboxylic ethyl ester, 1-(5,6-Dimethoxy-1-methyl-2-benzimidazolyl)-4-(2-furoyl) piperazine, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4 (tetrahydro-2-furoyl) piperazine, 4-(5,6-Dimethoxy-2-benzimidazolyl) piperazine-1-carboxylic acid isobutyl ester, N,N-Dimethyl 4-(5,6-dimethoxy-2-benzimidazolyl) piperazine-1-carboxamide, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4(3,4-dimethoxy-phenyl) piperazine, N (4-methyl valeroyl) piperazine, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4(4-methylvaleroyl) piperazine, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4(3-trifluoromethyl phenyl) piperazine, 1-methyl 4(2-benzimidazolyl) piperazine and pharmaceutically acceptable acid addition salts thereof and a pharmaceutically acceptable carrier.
A method of treating hypertension in a mammal comprising administering to a mammal so afflicted a therapeutically effective amount of a compound selected from the groups consisting of:
- 1-(5,6-Dimethoxy-2-benzimidazolyl)-4-(2-furoyl) piperazine, 4-(5,6-Dimethoxy-2-benzimidazolyl) piperazine-1-carboxylic ethyl ester, 1-(5,6-Dimethoxy-1-methyl-2-benzimidazolyl)-4-(2-furoyl) piperazine, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4 (tetrahydro-2-furoyl) piperazine, 4-(5,6-Dimethoxy-2-benzimidazolyl) piperazine-1-carboxylic acid isobutyl ester, N,N-Dimethyl 4-(5,6-dimethoxy-2-benzimidazolyl) piperazine-1-carboxamide, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4(3,4-dimethoxy-phenyl) piperazine, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4(4-methylvaleroyl) piperazine, 1-(5,6-Dimethoxy-2-benzimidazolyl)-4(3-trifluoromethyl phenyl) piperazine, 1-methyl 4(2-benzimidazolyl) piperazine and pharmaceutically acceptable acid addition salts thereof.
A compound of the formula:
- ##STR15## wherein:
- R is selected from the group consisting of hydrogen or methyl;
- R' is C.sub.2 -C.sub.4 alkoxy carbonyl or N,N-dimethylamino carbonyl and
- R" is selected from the group consisting of hydrogen or methoxy.
Dependencies are inferred from the claim text.