US4144344A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antihypertensive 1-substituted-4-(2-oxo-1-imidazolidinyl) piperidines
Assignee: Novartis Corp
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Filing: 1977-01-21
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Granted: 1979-03-13
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Expires: 1997-01-21
Abstract
Abstract A process known per se for the manufacture of oxygenated N-aryl-diazacyclic compounds of the formula ##STR1## wherein EACH OF R 1 and R 2 represents a substituted or unsubstituted aryl group and alk represents a lower alkylene group which separates both nitrogen atoms from each other by 2 or 3 carbon atoms, or salts thereof. The novel compounds can be used as antihypertensives, antitachycardiac agents and α-receptor blockers.
Inventors
- 👤 Kurt Eichenberger
- 👤 Hans Kuhnis
- 👤 Franz Ostermayer
- 👤 Herbert Schroter
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 14:54
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/72; C07D213/74; A; A61; A61P; A61P25/00; A61P25/02; A61P9/00; A61P9/06; A61P9/12; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/56; C07D211/58; C07D211/68; C07D211/72
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
183 words
Oxygenated N-aryldiazacyclic compounds of the formula ##STR13## wherein R 1 , represents a phenyl or naphthyl group which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonylamino-lower alkyl, lower alkenyl, hydroxyl, lower alkoxy, phenol-lower alkoxy, lower alkoxy-lower alkoxy, lower alkylthio-lower alkoxy, lower alkanoyl-lower alkoxy, lower alkenyloxy, lower alkinyloxy, lower alkylthio, halogen, lower alkanoyl, lower alkoxy-carbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, cyano, nitro, lower alkanoylamino, lower alkoxycarbonylamino, 3-lower alkylureido and/or 3-cycloalkyl-ureido, ore represents pyridyl which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio and/or halogen, R 2 represents a phenyl or naphthyl group which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, halogen-lower alkyl, lower alkoxy, halogen, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, nitro and/or di-lower alkylamino, or represents pyridyl which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, lower alkoxy and/or halogen, and alk represents ethylene, or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
183 words
Oxygenated N-aryldiazacyclic compounds of the formula ##STR13## wherein R 1 , represents a phenyl or naphthyl group which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonylamino-lower alkyl, lower alkenyl, hydroxyl, lower alkoxy, phenol-lower alkoxy, lower alkoxy-lower alkoxy, lower alkylthio-lower alkoxy, lower alkanoyl-lower alkoxy, lower alkenyloxy, lower alkinyloxy, lower alkylthio, halogen, lower alkanoyl, lower alkoxy-carbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, cyano, nitro, lower alkanoylamino, lower alkoxycarbonylamino, 3-lower alkylureido and/or 3-cycloalkyl-ureido, ore represents pyridyl which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, lower alkoxy, lower alkylthio and/or halogen, R 2 represents a phenyl or naphthyl group which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, halogen-lower alkyl, lower alkoxy, halogen, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, nitro and/or di-lower alkylamino, or represents pyridyl which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, lower alkoxy and/or halogen, and alk represents ethylene, or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
116 words
Oxygenated N-aryldiazacyclic compounds of the formula I according to claim 1, wherein R 1 represents a phenyl group which is unsubstituted or substituted by a member selected from group consisting of lower alkyl, lower alkenyl, hydroxyl, lower alkoxy, phenyl-lower alkoxy, lower alkanoyl-lower alkoxy, lower alkenyloxy, lower alkinyloxy, halogen and/or cyano, R 2 represents a phenyl or naphthyl group which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, trifluoromethyl, lower alkyloxy, halogen, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, nitro and/or N,N-di-lower alkylamino, or represents a pyridyl group which is unsubstituted or substituted by a member selected from the group consisting of lower alkyl, lower alkoxy and/or halogen, and alk represents ethylene.
Claim 4
Dependent Claim
109 words
Oxygenated N-aryldiazacyclic compounds of the formula I according to claim 1, wherein R 1 represents a phenyl group which is substituted in the ortho-position by a member selected from the group consisting of lower alkyl, lower alkenyl, lower alkoxy, hydroxyl, hydroxy, benzyloxy, lower alkenyloxy, lower alkinyloxy, lower alkanoyl-lower alkoxy, halogen or cyano, R 2 represents a phenyl group which is unsubsituted or substituted by a member selected from the group consisting of lower alkyl, trifluoromethyl, lower alkoxy, halogen, lower alkanoyl, lower alkoxycarbonyl, carbamoyl, nitro and/or di-lower alkylamino, or represents a pyridyl group which is unsubstituted or substituted by lower alkyl or lower alkoxy, and alk represents the ethylene group.
Claim 5
Dependent Claim
67 words
Oxygenated N-aryldiazacyclic compounds of the formula I according to claim 1, wherein R 1 represents phenyl which is substituted in the ortho-position by a member selected from the group consisting of lower alkyl, lower alkenyl, lower alkenyloxy, halogen, cyano or lower alkoxy, R 2 represents phenyl which is unsubstituted or substituted by lower alkyl, lower alkoxy or halogen, or represents pyridyl and alk represents the ethylene group.
Claim 6
Dependent Claim
9 words
A compound according to claim 1, which is 1-{1-[2-Hydroxy-3-(2-methoxyphenyloxy)-pyropyl]-4-piperidy}-3-phenyl-imidazolidin-2-one.
Claim 7
Dependent Claim
9 words
A compound according to claim 1, which is 1-{1-[2-Hydroxy-3-(2-methoxyphenoxy)propyl]-4-piperidyl}-3-(4-methoxy-phenyl)-imidazolidin-2-one.
Claim 8
Dependent Claim
39 words
A pharmaceutical composition useful in the treatment of hypertension in a warmblooded animal comprising a therapeutically effective amount of a compound according to claim 1 or of a pharmaceutically acceptable acid addition salt thereof together with a pharmaceutical carrier.
Claim 9
Dependent Claim
18 words
A pharmaceutical composition according to claim 7 which contains 1-{1-[2-hydroxy-3-(2-methoxyphenyloxy)-propyl]-4-piperidyl}-3-phenyl-imidazolidin-2-one, or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
34 words
A method of treating hypertension in a warm blooded animal which comprises administering to said animal a therapeutically effective amount of a compound according to claim 1, or a pharmacologically acceptable acid addition salt.
Claim 11
Dependent Claim
15 words
A method according to claim 9 which comprises administering a therapeutically effective amount of 1-{1-[2-hydroxy-3-(2-methoxyphenyloxy)-propyl]-4-piperidyl}-3-phenyl-imidazolidin-2-one.
References Cited (Backward Citations)
US3459757A
Cited
US3956335A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-03-12 | 1982-09-11 | 1983-03-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-12 | 1986-09-11 | 1987-03-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-12 | 1990-09-11 | 1991-03-13 | $7700.00 | Window Closed / Lapsed |