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US4146630A
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Blood pressure lowering and adrenergic β-receptor inhibiting 3-(4-phenoxymethylpiperidino)-propyl-phenyl ethers
Assignee: Roche Diagnostics GmbH
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Filing: 1977-10-27
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Granted: 1979-03-27
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Expires: 1997-10-27
Abstract
Abstract A 3-(4-phenoxymethylpiperidino)-propyl-phenyl-ether of the formula ##STR1## wherein R 1 and R 2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO--Z, Z is hydroxy, lower alkyloxy or ##STR2## R 6 and R 7 each independently is hydrogen, lower alkyl or hydroxyalkyl, R 3 is hydrogen or --O--R 8 , R 8 is hydrogen, lower alkanoyl or aroyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl, R 4 and R 5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl, X and Y each independently is nitrogen or ##STR3## R 9 is hydrogen, lower allkyl optionally substituted by --O--R 8 , or --CO--Z, or a pharmacologically acceptable salt thereof. The compounds lower blood pressure and inhibit adrenergic β-receptors.
Inventors
- 👤 Wolfgang Kampe
- 👤 Walter-Gunar Friebe
- 👤 Fritz Wiedemann
- 👤 Gisbert Sponer
- 👤 Wolfgang Bartsch
- 👤 Karl Dietmann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 15:03
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/06; C07D211/08; C07D211/18; C07D211/20; C07D211/22; A; A61; A61P; A61P25/00; A61P25/02; A61P9/00; A61P9/08; A61P9/10; A61P9/12; C07D231/00; C07D231/54; C07D231/56
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
126 words
A 3-(4-phenoxymethylpiperidino)-propylphenyl-ether of the formula ##STR16## wherein R 1 and R 2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO-Z, Z is hydroxy, lower alkyloxy or ##STR17## R 6 and R 7 each independently is hydrogen, lower alkyl or hydroxyalkyl, R 3 is hydrogen or --O-R 8 , R 8 is hydrogen, lower alkanoyl or benzoyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl, R 4 and R 5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl, X and Y, each independently is nitrogen or ##STR18## R 9 is hydrogen, lower alkyl optionally substituted by --O-R 8 , or --CO-Z, or a pharmacologically acceptable salt thereof.
Claim 2
Dependent Claim
126 words
A 3-(4-phenoxymethylpiperidino)-propylphenyl-ether of the formula ##STR16## wherein R 1 and R 2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO-Z, Z is hydroxy, lower alkyloxy or ##STR17## R 6 and R 7 each independently is hydrogen, lower alkyl or hydroxyalkyl, R 3 is hydrogen or --O-R 8 , R 8 is hydrogen, lower alkanoyl or benzoyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl, R 4 and R 5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl, X and Y, each independently is nitrogen or ##STR18## R 9 is hydrogen, lower alkyl optionally substituted by --O-R 8 , or --CO-Z, or a pharmacologically acceptable salt thereof.
Claim 3
Dependent Claim
31 words
A compound according to claim 1, wherein the several alkyl, hydroxyalkyl, alkoxy and alkylthio moieties have up to 4 carbon atoms and, the alkanoyl moieties have up to 6 carbon atoms.
Claim 4
Dependent Claim
14 words
A compound according to claim 1, wherein X is ##STR19## and Y is nitrogen.
Claim 5
Dependent Claim
14 words
A compound according to claim 1, wherein X is nitrogen and Y is ##STR20##
Claim 6
Dependent Claim
11 words
A compound according to claim 1, wherein such compound is 4-[2-hydroxy-3-(4-phenoxymethylpiperidino)propoxy]-indole.
Claim 7
Dependent Claim
12 words
A compound according to claim 1, wherein such compound is 4-{2-hydroxy-3-[4-(3-chlorophenoxymethyl)-piperidino]-propoxy}-indole benzoate.
Claim 8
Dependent Claim
11 words
A compound according to claim 1, wherein such compound is 4-[2-hydroxy-3-(4-phenoxymethylpiperidino)-propoxy]-indazole.
Claim 9
Dependent Claim
11 words
A compound according to claim 1, wherein such compound is 4-{2-hydroxy-3-[2-methylphenoxymethyl)-piperidino]-propoxy}-indazole.
Claim 10
Dependent Claim
11 words
A compound according to claim 1, wherein such compound is 4-{2-hydroxy-3-[4-(3-methylphenoxymethyl)-piperidino]-propoxy}-indazole.
Claim 11
Dependent Claim
36 words
A blood pressure lowering and adrenergic β-receptor inhibiting composition comprising a blood pressure lowering and adrenergic β-receptor inhibiting effective amount of a compound or salt according to claim 1 in admixture with a pharmacologically acceptable diluent.
Claim 12
Dependent Claim
31 words
The method of lowering the blood pressure of a patient which comprises administering to said patient a blood pressure lowering effective amount of a compound or salt according to claim 1.
Claim 13
Dependent Claim
31 words
The method of inhibiting the adrenergic β-receptors of a patient which comprises administering to said patient an adrenergic β-receptor inhibiting effective amount of a compound or salt according to claim 1.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-03-26 | 1982-09-25 | 1983-03-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-26 | 1986-09-25 | 1987-03-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-26 | 1990-09-25 | 1991-03-27 | $7700.00 | Window Closed / Lapsed |