Patent EP0154969A2 successfully refreshed from Google Patents.
EP0154969A2
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EP
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Piperazine derivatives and their acid addition salts
Assignee: Mitsubishi Chemical Corp
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Filing: 1985-03-11
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Granted: —
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Expires: 2005-03-11
Abstract
Abstract A piperazine derivative according to the present invention has the following general formula (I): wherein R 1 is -OH,-OR 3 ,-SR 3 ,-SOR 3 or -SO 2 R 3 wherein R 3 is alkyl group having 1 to 3 carbon atoms; R 2 is -S0 2 NH 2 , -SO 2 NHR 4 , -SO 2 NR 4 W 5 , -COOH, -COOR 4 , -CONH 2 , -CONHR 4 , -CONR 4 R 5 , -NHCONH 2 , -NHCSNH 2 , - NHCONHR 4 , -NHCOR4 or -NHS0 2 R 4 wherein R 4 and R 5 are independently alkyl group havingl to 3 carbon atoms; or R 1 and R 2 together with carbon atoms to which they are Z is-CO-or-CH(OH)-; Ar is pyridyl or substituted or unsubstituted phenyl; and n is an integer of 3 to 5.
Inventors
- 👤 Harukazu No. 709 Nishiooji Garden-Heights Fukami
- 👤 Shinya Inoue
- 👤 Issei Nitta
- 👤 Kenichiro Nakao
- 👤 Ryoji Kikumoto
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-27 15:12
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: 18
Claim 1
Independent Claim
156 words
A piperazine derivative having the following general formula [I]: wherein R 1 is - OH , - OR 3 , -S R 3 , - SO R 3 or -SO 2 R 3 wherein R 3 is 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 group having 1 to 3 carbon atoms; or R 1 and R 2 together with carbon atoms to which they are attached form Z is -CO- or -CH(OH)-; Ar is pyridyl or substituted or unsubstituted phenyl; and n is an integer of 3 to 5, and an acid addition salt thereof.
Claim 2
Dependent Claim
156 words
A piperazine derivative having the following general formula [I]: wherein R 1 is - OH , - OR 3 , -S R 3 , - SO R 3 or -SO 2 R 3 wherein R 3 is 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 group having 1 to 3 carbon atoms; or R 1 and R 2 together with carbon atoms to which they are attached form Z is -CO- or -CH(OH)-; Ar is pyridyl or substituted or unsubstituted phenyl; and n is an integer of 3 to 5, and an acid addition salt 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
43 words
The compound according to claim 1, wherein R 1 is - OH or -OR 3 , R2 is - CO OH, -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
31 words
The compound according to claim 1, wherein R 1 and R 2 together with carbon atoms to which they are attached form and the others are as defined in claim 1.
Claim 7
Dependent Claim
32 words
The compound according to any one of claims 1 to 5, wherein phenyl is substituted with halogen, alkyl having 1 to 3 carbon atoms or alkoxy having 1 to 3 carbon atoms.
Claim 8
Dependent Claim
12 words
The compound according to claim 6, wherein phenyl is substituted with methoxy.
Claim 9
Dependent Claim
13 words
The compound according to claim 1, wherein Ar is phenyl, 2-methoxyphenyl or 2-pyridyl.
Claim 10
Dependent Claim
13 words
The compound according to claim 1, wherein the acid addition salt is dihydrochloride.
Claim 11
Dependent Claim
205 words
A process for preparing a piperazine derivative having the following general formula [I]: wherein R 1 is - OH , -OR 3 , - SR 3 , - SO R 3 or - SO2R 3 wherein R 3 is 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 - NH S 02R 4 wherein R 4 and R 5 are independently alkyl group having 1 to 3 carbon atoms; or R 1 and R 2 together with carbon atoms to which they are attached form Z is -CO- or -CH(OH)-; Ar is pyridyl or substituted or unsubstituted phenyl; and n is an integer of 3 to 5, comprising reacting halogeno-alkanoylbenzene or halogeno- alkylbenzene of the formula [II]: wherein R 1 , R 2 , Z and n are as defined in claim 1 and X is halogen atom, with a piperazine of the formula [III]: wherein Ar is defined in claim 1, and if required reducing the resultant product.
Claim 12
Dependent Claim
21 words
The process according to claim 10, wherein the reaction is carried out in the presence of a scavenger for hydrogen halide.
Claim 13
Dependent Claim
18 words
The process according to claim 11, wherein the scavenger is an inorganic salt or an organic tertiary amine.
Claim 14
Dependent Claim
16 words
The process according to claim 10, wherein the reaction is carried out in an inert solvent.
Claim 15
Dependent Claim
172 words
A pharmaceutical composition useful for treating hypertension comprising at least a piperazine derivative having the following general formula [I]: wherein R 1 is - OH , - OR 3 , -S R 3 , - SOR 3 or -SO 2 R 3 wherein R 3 is 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 group having 1 to 3 carbon atoms; or R 1 and R 2 together with carbon atoms to which they are attached form Z is -CO- or -CH(OH)-; Ar is pyridyl or substituted or unsubstituted phenyl; and n is an integer of 3 to 5, or an acid addition salt thereof in combination with a pharmaceutically acceptable carrier.
Claim 16
Dependent Claim
172 words
A pharmaceutical composition useful for treating hypertension comprising at least a piperazine derivative having the following general formula [I]: wherein R 1 is - OH , - OR 3 , -S R 3 , - SOR 3 or -SO 2 R 3 wherein R 3 is 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 group having 1 to 3 carbon atoms; or R 1 and R 2 together with carbon atoms to which they are attached form Z is -CO- or -CH(OH)-; Ar is pyridyl or substituted or unsubstituted phenyl; and n is an integer of 3 to 5, or an acid addition salt thereof in combination with a pharmaceutically acceptable carrier.
Claim 17
Dependent Claim
21 words
The composition according to claim 14, wherein it is in a solid or liquid dosage unit form intended for oral administration.
Claim 18
Dependent Claim
19 words
The composition according to claim 14, wherein it is in a liquid dosage unit form intended for parenteral administration.
References Cited (Backward Citations)
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