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US4459296A
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Piperazines and homopiperazines, N-substituted by an aromatic heterocyclic group, and their use in therapeutics
Assignee: Synthelabo SA
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Filing: 1982-04-20
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Granted: 1984-07-10
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Expires: 2002-04-20
Abstract
Abstract There are disclosed piperidinio, piperazino and homopiperazino derivatives wherein there is N-substitution by a heterocyclic compound taken from the group benzimidazole, indole, purine or benzotriazole and to the organic or mineral acid addition salts of these derivatives. The process for preparation of such compounds and their use is also disclosed.
Inventors
- 👤 Jean-Francois R. Ancher
- 👤 Patrick G. Guerret
- 👤 Michel Langlois
- 👤 Jacky A. Tisne-Versailles
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 18:05
CPC Classifications
C; C07; C07D; C07D235/00; C07D235/02; C07D235/04; C07D235/06; C07C; C07C205/00; C07C205/13; C07C205/19; C07C255/00; C07D209/00; C07D209/02; C07D209/04; C07D209/08; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/60; C07D211/62; C07D235/08; C07D249/00; C07D249/16; C07D249/18; C07D295/00; C07D295/16; C07D295/20; C07D295/205; C07D307/00; C07D307/02; C07D307/04; C07D307/18; C07D307/24; C07D307/34; C07D307/56; C07D307/68; C07D333/00; C07D333/02; C07D333/04; C07D333/26; C07D333/38; C07D333/40; C07D401/00; C07D401/02; C07D401/12; C07D405/00; C07D405/02; C07D405/12; C07D409/00; C07D409/02; C07D409/12; C07D413/00; C07D413/02; C07D413/12; C07D473/00; C07D473/26; C07D473/32; C07D473/34
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
120 words
Novel piperazines and homopiperazines corresponding to the formula: ##STR70## in which: n=1 or 2; R represents: a hydrogen atom, an alkylcarbonyl or alkyloxycarbonyl group where the alkyl residue is linear or branched and comprises 1 to 5 carbon atoms, a heterocyclic--carbonyl group (heterocyclic--CO) in which the heterocycle is a furyl, thienyl, tetrahydrofuryl, pyridyl or [(methylthio-2) oxadiazole-1,3,4, yl]-5 nucleus, a benzoyl, trimethoxy-3,4,5 cinnamoyl, allyloxycarbonyl, (methyl-2 propene-1 yl-3) oxycarbonyl, benzyloxycarbonyl or phenoxycarbonyl chain, or a phenylthio group, and Ar represents any one of the following nucleii: benzimidazolyl 4(7); (alkyl-2) benzimidazolyl-4(7) in which the alkyl residue comprises 1 to 4 carbon atoms; (phenyl-2) benzimidazolyl-4(7) ; (benzyl-2) benzimidazolyl-4(7); benzotriazolyl-4(7); indolyl-7; indolyl-4, but only in the case there n=1; and the acid addition salts thereof.
Claim 2
Dependent Claim
120 words
Novel piperazines and homopiperazines corresponding to the formula: ##STR70## in which: n=1 or 2; R represents: a hydrogen atom, an alkylcarbonyl or alkyloxycarbonyl group where the alkyl residue is linear or branched and comprises 1 to 5 carbon atoms, a heterocyclic--carbonyl group (heterocyclic--CO) in which the heterocycle is a furyl, thienyl, tetrahydrofuryl, pyridyl or [(methylthio-2) oxadiazole-1,3,4, yl]-5 nucleus, a benzoyl, trimethoxy-3,4,5 cinnamoyl, allyloxycarbonyl, (methyl-2 propene-1 yl-3) oxycarbonyl, benzyloxycarbonyl or phenoxycarbonyl chain, or a phenylthio group, and Ar represents any one of the following nucleii: benzimidazolyl 4(7); (alkyl-2) benzimidazolyl-4(7) in which the alkyl residue comprises 1 to 4 carbon atoms; (phenyl-2) benzimidazolyl-4(7) ; (benzyl-2) benzimidazolyl-4(7); benzotriazolyl-4(7); indolyl-7; indolyl-4, but only in the case there n=1; and the acid addition salts thereof.
Claim 3
Dependent Claim
28 words
The piperazines, homopiperazines and corresponding salts according to claim 1, wherein the pair (n,R) takes the value (1,H) and Ar represents a benzimidazolyl-4(7), benzotriazolyl-4(7), indolyl-4 or indolyl-7 group.
Claim 4
Dependent Claim
49 words
The piperazines, homopiperazines and corresponding salts according to claim 1, wherein Ar is a benzimidazolyl-4(7) nucleus and the pair (R,n) takes on any one of the values selected from: (H, 1), (COCH 3 , 1), ##STR71## (COOEt, 1), (COOEt, 2), (COOCH 3 , 1), ##STR72## (COOO, 1), (SO, 1).
Claim 5
Dependent Claim
19 words
A medicament exhibiting antihypertensive activity, formed by one of the compounds or pharmaceutically acceptable salts according to claim 1.
Claim 6
Dependent Claim
23 words
An antihypertensive pharmaceutical composition comprising, as active ingredient(s), at least one medicament according to claim 4, in association with a pharmaceutically acceptable support.
Claim 7
Dependent Claim
19 words
A compound according to claim 1 wherein n=1; R is a 2-thienylcarbonyl group; and Ar is a benzimidazolyl-4(7) group.
Claim 8
Dependent Claim
15 words
A compound according to claim 1 wherein n=1; R=H; and Ar is an indoyl-7 group.
Claim 9
Dependent Claim
4 words
(Carbethoxy-4 piperazino-1)-4(7) benzimidazole, maleate.
Claim 10
Dependent Claim
4 words
(Carbethoxy-4 piperazino-1)-4(7) benzimidazole, maleate.
Claim 11
Dependent Claim
3 words
(Piperazino-1)-4(7) benzimidazole, tribromhydrate.
Claim 12
Dependent Claim
3 words
(Piperazino-1)-4(7) benzimidazole, tribromhydrate.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-07-10 | 1988-01-09 | 1988-07-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-07-10 | 1992-01-09 | 1992-07-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-07-10 | 1996-01-09 | 1996-07-10 | $7700.00 | Window Closed / Lapsed |