US4613598A
Expired / Lapsed
US
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Piperazine derivatives and their acid addition salts
Assignee: Mitsubishi Chemical Corp
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Filing: 1985-03-06
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Granted: 1986-09-23
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Expires: 2005-03-06
Abstract
Abstract A piperazine derivative according to the present invention has the following general formula [I]: <IMAGE> [I] wherein R1 is -OH, -OR3, -SR3, -SOR3 or -SO2R3 wherein R3 is alkyl group having 1 to 3 carbon atoms; R2 is -SO2NH2, -SO2NHR4, -SO2NR4R5, -COOH, -COOR4, -CONH2, -CONHR4, -CONR4R5, -NHCONH2, -NHCSNH2, -NHCONHR4, -NHCOR4 or -NHSO2R4 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 <IMAGE> +TR <IMAGE> 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.
Inventors
- 👤 Harukazu Fukami
- 👤 Shinya Inoue
- 👤 Issei Nitta
- 👤 Kenichiro Nakao
- 👤 Ryoji Kikumoto
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 23:37
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/10; C07D295/104; C07D295/108; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/72; C07D213/74; C07D265/00; C07D265/28; C07D265/34; C07D265/36; C07D267/00; C07D267/02; C07D267/08; C07D267/12; C07D267/14; C07D279/00; C07D279/10; C07D279/14; C07D279/16; C07D295/08; C07D295/084; C07D295/092; C07D417/00; C07D417/02; C07D417/12
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
160 words
A piperazine compound of formula (I): ##STR63## wherein R 1 is --OH, --OR 3 , --SR 3 , --SOR 3 or --SO 2 R 3 , wherein R 3 is an alkyl group having 1 to 3 carbon atoms; R 2 is --SO 2 NH 2 , --SO 2 NHR 4 , --SO 2 NR 4 R 5 , --COOH, --COOR 4 , --CONH 2 , --CONHR 4 , --CONR 4 R 5 , --NHCONH 2 , --NHCSNH 2 , --NHCONHR 4 , --NHCOR 4 or --NHSO 2 R 4 , wherein R 4 and R 5 are independently alkyl groups having 1 to 3 carbon atoms; or R 1 and R 2 together with the carbon atoms to which they are attached form ##STR64## Z is --CO-- or --CH(OH)--; Ar is pyridyl, phenyl, or halogen, C 1-3 alkyl or C 1-3 alkoxy substituted phenyl; n is an integer of 3 to 5; and therapeutically active acid addition salts thereof.
Claim 2
Dependent Claim
160 words
A piperazine compound of formula (I): ##STR63## wherein R 1 is --OH, --OR 3 , --SR 3 , --SOR 3 or --SO 2 R 3 , wherein R 3 is an alkyl group having 1 to 3 carbon atoms; R 2 is --SO 2 NH 2 , --SO 2 NHR 4 , --SO 2 NR 4 R 5 , --COOH, --COOR 4 , --CONH 2 , --CONHR 4 , --CONR 4 R 5 , --NHCONH 2 , --NHCSNH 2 , --NHCONHR 4 , --NHCOR 4 or --NHSO 2 R 4 , wherein R 4 and R 5 are independently alkyl groups having 1 to 3 carbon atoms; or R 1 and R 2 together with the carbon atoms to which they are attached form ##STR64## Z is --CO-- or --CH(OH)--; Ar is pyridyl, phenyl, or halogen, C 1-3 alkyl or C 1-3 alkoxy substituted phenyl; n is an integer of 3 to 5; and therapeutically active acid addition salts thereof.
Claim 3
Dependent Claim
35 words
The compound according to claim 1, wherein R 2 is --SO 2 NH 2 , --SO 2 NHR 4 or --SO 2 NR 4 R 5 and the others are as defined in claim 1.
Claim 4
Dependent Claim
41 words
The compound according to claim 1, wherein R 1 is --OH or --OR 3 , R 2 is --COOH, --COOR 4 , --CONH 2 , --CONHR 4 or --CONR 4 R 5 and the others are as defined in claim 1.
Claim 5
Dependent Claim
35 words
The compound according to claim 1, wherein R 2 is --NHCONH 2 , --NHCSNH 2 , --NHCONHR 4 , --NHCOR 4 or --NHSO 2 R 4 and the others are as defined in claim 1.
Claim 6
Dependent Claim
12 words
The compound according to claim 1, wherein phenyl is substituted with methoxy.
Claim 7
Dependent Claim
13 words
The compound according to claim 1, wherein the acid addition salt is dihydrochloride.
Claim 8
Dependent Claim
181 words
A pharmaceutical composition which is effective in the treatment of hypertension, comprising: at least one piperazine compound of the formula (I): ##STR65## wherein R 1 is --OH,--OR 3 , --SR 3 , --SOR 3 or --SO 2 R 3 , wherein R 3 is an alkyl group having 1 to 3 carbon atoms; R 2 is --SO 2 NH 2 , --SO 2 NHR 4 , --SO 2 NR 4 R 5 , --COOH, --COOR 4 , --CONH 2 , --CONHR 4 , --CONR 4 R 5 , --NHCONH 2 , --NHCSNH 2 , --NHCONHR 4 , --NHCOR 4 or --NHSO 2 R 4 , wherein R 4 and R 5 are indepedently alkyl groups having 1 to 3 carbon atoms; or R 1 and R 2 together with the carbon atoms to which they are attached form ##STR66## Z is --CO-- or --CH(OH)--; Ar is pyridyl, phenyl, or halogen, C 1-3 alkyl or C 1-3 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.
Claim 9
Dependent Claim
181 words
A pharmaceutical composition which is effective in the treatment of hypertension, comprising: at least one piperazine compound of the formula (I): ##STR65## wherein R 1 is --OH,--OR 3 , --SR 3 , --SOR 3 or --SO 2 R 3 , wherein R 3 is an alkyl group having 1 to 3 carbon atoms; R 2 is --SO 2 NH 2 , --SO 2 NHR 4 , --SO 2 NR 4 R 5 , --COOH, --COOR 4 , --CONH 2 , --CONHR 4 , --CONR 4 R 5 , --NHCONH 2 , --NHCSNH 2 , --NHCONHR 4 , --NHCOR 4 or --NHSO 2 R 4 , wherein R 4 and R 5 are indepedently alkyl groups having 1 to 3 carbon atoms; or R 1 and R 2 together with the carbon atoms to which they are attached form ##STR66## Z is --CO-- or --CH(OH)--; Ar is pyridyl, phenyl, or halogen, C 1-3 alkyl or C 1-3 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.
Claim 10
Dependent Claim
22 words
The composition according to claim 7, wherein said composition is in a solid or liquid dosage unit form intended for oral administration.
Claim 11
Dependent Claim
20 words
The composition according to claim 14, wherein said composition is in a liquid dosage unit form intended for parenteral administration.
References Cited (Backward Citations)
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1989-09-22 | 1990-03-24 | 1990-09-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-09-22 | 1994-03-24 | 1994-09-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-09-22 | 1998-03-24 | 1998-09-23 | $7700.00 | Window Closed / Lapsed |