US3998955A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antihypertensive compositions
Assignee: Novartis Corp
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Filing: 1975-04-16
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Granted: 1976-12-21
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Expires: 1995-04-16
Abstract
Abstract Pyridines of the formula I ##STR1## wherein R 1 is free hydroxyl, lower alkoxy, cycloalkoxy, amino-lower alkoxy or lower alkoxy-lower alkoxy, free amino, hydroxyamino, lower alkyleneamino, oxa-, aza- or thia-lower alkyleneamino or mono- or di-lower alkylamino, R 2 is oxygen or sulphur, R 3 and R 4 are each alkoxy, free amino, mono- or di-lower alkylamino, lower alkyleneamino, oxa-, aza- or thia-lower alkyleneamino, halogen or free hydroxyl, and either R 3 or R 4 can be hydrogen, and alk is an alkyl group with 3-10 carbon atoms, and their N-oxides, and salts are useful as dopamine-β-hydroxylase inhibitors.
Inventors
- 👤 Hans Kuhnis
- 👤 Christian Egli
- 👤 Kurt Eichenberger
- 👤 Phyllis Roberta Hedwall
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 07:28
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/62; C07D213/63; C07D213/64; C07D213/68; C07D213/78; C07D213/79; C07D213/81
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
78 words
A pharmaceutical preparation useful in the treatment of hypertension, which comprises an antihypertensively effective amount of a compound of the formula ##STR35## in which R represents hydrogen or lower alkyl, alk represents an alkyl group having 4 to 5 carbon atoms, R 3 and R 4 each represents chloro or lower alkoxy and one of the symbols R 3 and R 4 may also represent hydrogen or a therapeutically usable salt thereof, together with a therapeutically usable excipient.
Claim 2
Dependent Claim
78 words
A pharmaceutical preparation useful in the treatment of hypertension, which comprises an antihypertensively effective amount of a compound of the formula ##STR35## in which R represents hydrogen or lower alkyl, alk represents an alkyl group having 4 to 5 carbon atoms, R 3 and R 4 each represents chloro or lower alkoxy and one of the symbols R 3 and R 4 may also represent hydrogen or a therapeutically usable salt thereof, together with a therapeutically usable excipient.
Claim 3
Dependent Claim
18 words
The pharmaceutical preparation of claim 1, wherein the active compound is 2-carboxy-4-methoxy-5-n-butyl-pyridine or a therapeutically usable salt thereof.
Claim 4
Dependent Claim
93 words
A pharmaceutical preparation useful for the treatment of hypertension, which comprises an antihypertensively effective amount of a combination of a compound of the formula ##STR36## in which R represents hydrogen or lower alkyl, alk represents an alkyl group having 4 to 5 carbon atoms, R 3 and R 4 each represents chloro or lower alkoxy and one of the symbols R 3 and R 4 may also represent hydrogen or a therapeutically usable salt thereof together with a therapeutically usable excipient and an antihypertensively active amino acid together with a therapeutically usable excipient.
Claim 5
Dependent Claim
93 words
A pharmaceutical preparation useful for the treatment of hypertension, which comprises an antihypertensively effective amount of a combination of a compound of the formula ##STR36## in which R represents hydrogen or lower alkyl, alk represents an alkyl group having 4 to 5 carbon atoms, R 3 and R 4 each represents chloro or lower alkoxy and one of the symbols R 3 and R 4 may also represent hydrogen or a therapeutically usable salt thereof together with a therapeutically usable excipient and an antihypertensively active amino acid together with a therapeutically usable excipient.
Claim 6
Dependent Claim
14 words
The preparation of claim 3 wherein the amino acid is an α-methyldopa type compound.
Claim 7
Dependent Claim
20 words
The preparation of claim 4 wherein said amino acid is α-amino-α-methyl-B-hydroxypropionic acid or a pharmaceutically acceptable salt or ester thereof.
Claim 8
Dependent Claim
35 words
The preparation of claim 1 wherein said compound is 2-carboxy-4-methoxy-5-n-butyl pyridine or a non-toxic salt thereof and said amino acid is α-amino-α-methyl-β- (3,4-dihydroxy phenyl)-propionic acid or an alkali metal or alkaline earth metal salt thereof.
Claim 9
Dependent Claim
24 words
The preparation of claim 4 containing 100 to 200 mg of α-amino-α-methyl-β-(3,4-dihydroxy phenyl)-propionic acid and 50 to 200mg of the calcium salt of 2-carboxy-4-methoxy-5-n-butyl-pyridine.
References Cited (Backward Citations)
GB1219176A
Cited
US3862159A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-12-21 | 1980-06-21 | 1980-12-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-12-21 | 1984-06-21 | 1984-12-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-12-21 | 1988-06-21 | 1988-12-21 | $7700.00 | Window Closed / Lapsed |