Piperazine derivatives and their acid addition salts
First Claim
1. A piperazine compound of formula (I):
- ##STR63## wherein R1 is --OH, --OR3, --SR3, --SOR3 or --SO2 R3, wherein R3 is an alkyl group having 1 to 3 carbon atoms;
R2 is --SO2 NH2, --SO2 NHR4, --SO2 NR4 R5, --COOH, --COOR4, --CONH2, --CONHR4, --CONR4 R5, --NHCONH2, --NHCSNH2, --NHCONHR4, --NHCOR4 or --NHSO2 R4, wherein R4 and R5 are independently alkyl groups having 1 to 3 carbon atoms;
orR1 and R2 together with the carbon atoms to which they are attached form ##STR64## Z is --CO-- or --CH(OH)--;
Ar is pyridyl, phenyl, or halogen, C1-3 alkyl or C1-3 alkoxy substituted phenyl;
n is an integer of 3 to 5; and
therapeutically active acid addition salts thereof.
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Abstract
A piperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R1 is --OH, --OR3, --SR3, --SOR3 or --SO2 R3 wherein R3 is alkyl group having 1 to 3 carbon atoms;
R2 is --SO2 NH2, --SO2 NHR4, --SO2 NR4 R5, --COOH, --COOR4, --CONH2, --CONHR4, --CONR4 R5, --NHCONH2, --NHCSNH2, --NHCONHR4, --NHCOR4 or --NHSO2 R4 wherein R4 and R5 are independently alkyl group having 1 to 3 carbon atoms; or
R1 and R2 together with carbon atoms to which they are attached form ##STR2## Z is --CO-- or --CH(OH)--; Ar is pyridyl or substituted or unsubstituted phenyl; and
n is an integer of 3 to 5.
An acid addition salt of the piperazine derivative having the above formula [I] is included in the present invention. The piperazine derivative as well as its acid addition salt according to the present invention have the ability to reduce the blood pressure.
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Citations
9 Claims
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1. A piperazine compound of formula (I):
- ##STR63## wherein R1 is --OH, --OR3, --SR3, --SOR3 or --SO2 R3, wherein R3 is an alkyl group having 1 to 3 carbon atoms;
R2 is --SO2 NH2, --SO2 NHR4, --SO2 NR4 R5, --COOH, --COOR4, --CONH2, --CONHR4, --CONR4 R5, --NHCONH2, --NHCSNH2, --NHCONHR4, --NHCOR4 or --NHSO2 R4, wherein R4 and R5 are independently alkyl groups having 1 to 3 carbon atoms;
orR1 and R2 together with the carbon atoms to which they are attached form ##STR64## Z is --CO-- or --CH(OH)--;
Ar is pyridyl, phenyl, or halogen, C1-3 alkyl or C1-3 alkoxy substituted phenyl;n is an integer of 3 to 5; and therapeutically active acid addition salts thereof. - View Dependent Claims (2, 3, 4, 5, 6)
- ##STR63## wherein R1 is --OH, --OR3, --SR3, --SOR3 or --SO2 R3, wherein R3 is an alkyl group having 1 to 3 carbon atoms;
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7. A pharmaceutical composition which is effective in the treatment of hypertension, comprising:
at least one piperazine compound of the formula (I);
##STR65## wherein R1 is --OH,--OR3, --SR3, --SOR3 or --SO2 R3, wherein R3 is an alkyl group having 1 to 3 carbon atoms;R2 is --SO2 NH2, --SO2 NHR4, --SO2 NR4 R5, --COOH, --COOR4, --CONH2, --CONHR4, --CONR4 R5, --NHCONH2, --NHCSNH2, --NHCONHR4, --NHCOR4 or --NHSO2 R4, wherein R4 and R5 are indepedently alkyl groups having 1 to 3 carbon atoms;
orR1 and R2 together with the carbon atoms to which they are attached form ##STR66## Z is --CO-- or --CH(OH)--;
Ar is pyridyl, phenyl, or halogen, C1-3 alkyl or C1-3 alkoxy substituted phenyl;n is an integer of 3 to 5; and therapeutically active acid addition salts thereof in combination with a pharmaceutically acceptable carrier. - View Dependent Claims (8)
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9. The composition according to claim 14, wherein said composition is in a liquid dosage unit form intended for parenteral administration.
Specification