Pharmacologically active piperazino derivatives
First Claim
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1. A piperazino compound of the formula ##STR33## in which:
- A is CO, CH2 or SO2 ;
R is 2-methoxy-5-sulphamoyl-phenyl, 2-sulphamoylimidazyl, 2-amino-1,3,4-thiadiazole or 2-acetamido-1,3,4-thiadiazole;
R'"'"' is H, linear or branched C1 -C6 alkyl;
linear or branched C2 -C6 alkenyl;
alkyl-phenyl or alkenyl-phenyl, wherein phenyl is optionally monosubstituted with halogen, trihalomethyl, C1 -C6 alkyl, C1 -C6 alkoxy, or sulphonamido;
C2 -C6 aliphatic acyl;
C3 -C6 alkylcarboxyalkoxy;
alkyl-carboxyamino in which the alkyl is C1 -C3 and the amine is mono or disubstituted by linear or branched C1 -C6 alkyl and;
R" is H, or together with R'"'"' forms a 5 or 6 membered ring condensed with the piperazine;
provided that when R is a substituted phenyl group and A is CO, R'"'"' is other than H, C1 -C4 alkyl or benzyl.
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Abstract
New piperazino derivatives of formula ##STR1## in which R is a phenyl radical substituted with at least one sulphonamido group or a substituted nitrogenated heterocyclic ring, and A is CO, CH2, SO2, possessing inhibiting activity towards carbonic anhydrase.
The new products are prepared from compounds of formula R-A-X in which X is OH, SH, halogen, OR"" or SR"" in which R"" is methyl, ethyl, phenyl, carbomethoxy, carboethoxy, and from a piperazino derivative of formula ##STR2## The R'"'"' group can also be introduced on termination of the reaction, by removing and substituting a protective group present at the nitrogen.
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1 Claim
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1. A piperazino compound of the formula ##STR33## in which:
- A is CO, CH2 or SO2 ;
R is 2-methoxy-5-sulphamoyl-phenyl, 2-sulphamoylimidazyl, 2-amino-1,3,4-thiadiazole or 2-acetamido-1,3,4-thiadiazole; R'"'"' is H, linear or branched C1 -C6 alkyl;
linear or branched C2 -C6 alkenyl;
alkyl-phenyl or alkenyl-phenyl, wherein phenyl is optionally monosubstituted with halogen, trihalomethyl, C1 -C6 alkyl, C1 -C6 alkoxy, or sulphonamido;
C2 -C6 aliphatic acyl;
C3 -C6 alkylcarboxyalkoxy;
alkyl-carboxyamino in which the alkyl is C1 -C3 and the amine is mono or disubstituted by linear or branched C1 -C6 alkyl and;R" is H, or together with R'"'"' forms a 5 or 6 membered ring condensed with the piperazine; provided that when R is a substituted phenyl group and A is CO, R'"'"' is other than H, C1 -C4 alkyl or benzyl.
- A is CO, CH2 or SO2 ;
Specification
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Current AssigneeRavizza SPA
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Original AssigneeRavizza SPA
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InventorsSignorini, Roberto, Botre, Francesco
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Primary Examiner(s)Shen, Cecilia
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Application NumberUS06/756,257Time in Patent Office1,818 DaysField of Search544/349, 544/366, 544/367, 544/372, 544/377, 544/386, 544/368, 544/370, 544/382, 544/383, 544/388, 544/390, 544/392, 544/391US Class Current544/349CPC Class CodesA61P 43/00 Drugs for specific purposes...C07D 233/42 Sulfur atomsC07D 285/135 Nitrogen atomsC07D 295/192 from aromatic carboxylic acidsC07D 317/58 Radicals substituted by nit...C07D 487/04 Ortho-condensed systemsY02P 20/55 Design of synthesis routes,...
