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US4500527A
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Antihypertensive 4[(3-alkylamino-2-hydroxypropyl)-oxyiminomethyl phenyl]-1,4-dihydropyridines
Assignee: USV Pharmaceutical Corp
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Filing: 1983-06-22
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Granted: 1985-02-19
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Expires: 2003-06-22
Abstract
Abstract Unsaturated heterocyclic dihydropyridines of the formula: <IMAGE> wherein the substituents defined herein have been found to have useful antihypertensive activity.
Inventors
- 👤 Bernard Loev
- 👤 James R. Shroff
- 👤 Rohit Desai
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 12:36
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/90
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
167 words
A compound of the formula ##STR13## wherein R is C 1 -C 10 alkyl, each R 1 is independently H, C 1 -C 4 alkyl, or C 1 -C 4 alkoxy C 1 -C 4 alkyl; each R 2 is independently H, C 1 -C 4 alkyl, formyl, CN, CH 2 OH, or di C 1 -C 4 alkylamino C 1 -C 4 alkyl; A is H, C 1 -C 10 alkyl, or X; X is ##STR14## Z is C 1 -C 15 alkylene; R 3 and R 4 are independently H, C 1 -C 4 alkyl, C 3 -C 4 cycloalkyl, hydroxy C 1 -C 4 alkyl, C 1 -C 4 alkoxy C 1 -C 4 alkyl, or phenyl C 1 -C 4 alkyl, or R 3 and R 4 together with the nitrogen to which they are attached form pyrrolyl, imidazolyl, pyrazolyl, dihydropyrazinyl, indolyl, isoindolyl, purinyl, carbazolyl, β-carbolinyl, phenthiazinyl, phenoxazinyl, pyrrolinyl, pyrazolinyl, (o) or (p) isoxazinyl, imidazolinyl, or morpholino; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
167 words
A compound of the formula ##STR13## wherein R is C 1 -C 10 alkyl, each R 1 is independently H, C 1 -C 4 alkyl, or C 1 -C 4 alkoxy C 1 -C 4 alkyl; each R 2 is independently H, C 1 -C 4 alkyl, formyl, CN, CH 2 OH, or di C 1 -C 4 alkylamino C 1 -C 4 alkyl; A is H, C 1 -C 10 alkyl, or X; X is ##STR14## Z is C 1 -C 15 alkylene; R 3 and R 4 are independently H, C 1 -C 4 alkyl, C 3 -C 4 cycloalkyl, hydroxy C 1 -C 4 alkyl, C 1 -C 4 alkoxy C 1 -C 4 alkyl, or phenyl C 1 -C 4 alkyl, or R 3 and R 4 together with the nitrogen to which they are attached form pyrrolyl, imidazolyl, pyrazolyl, dihydropyrazinyl, indolyl, isoindolyl, purinyl, carbazolyl, β-carbolinyl, phenthiazinyl, phenoxazinyl, pyrrolinyl, pyrazolinyl, (o) or (p) isoxazinyl, imidazolinyl, or morpholino; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
37 words
A compound of claim 1 wherein each R 1 is independently C 1 -C 4 alkyl, or C 1 -C 4 alkoxy C 1 -C 4 alkyl, each R 2 is independently C 1 -C 4 alkyl.
Claim 4
Dependent Claim
15 words
A compound of claim 1 wherein R is a branched alkyl of 3-10 carbon atoms.
Claim 5
Dependent Claim
12 words
A compound of claim 1 wherein ##STR15## is at the 4 position.
Claim 6
Dependent Claim
12 words
A compound of claim 1 wherein ##STR16## is at the 2 position.
Claim 7
Dependent Claim
12 words
A compound of claim 1 wherein ##STR17## is at the 3 position.
Claim 8
Dependent Claim
36 words
A compound of claim 4 wherein R 1 is C 1 -C 4 alkyl, R 2 is C 1 -C 4 alkyl, A is H, C 1 -C 4 alkyl or X, and X is ##STR18##
Claim 9
Dependent Claim
22 words
A compound of claim 7 wherein ##STR19## and Z is an alkylene containing C 1 -C 15 atoms in the principal chain.
Claim 10
Dependent Claim
16 words
A compound of claim 4 wherein A is H, C 1 -C 4 alkyl or morpholinoethyl.
Claim 11
Dependent Claim
5 words
Diethyl 4[4-(3-t-butylamino-2-hydroxypropyl)oxyiminomethyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate and its salts.
Claim 12
Dependent Claim
5 words
Diethyl 4[4-(3-t-butylamino-2-hydroxypropyl)oxyiminomethyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate and its salts.
Claim 13
Dependent Claim
29 words
A pharmaceutical dosage form for treating hypertension in mammals, said dosage form containing amount effective for treating hypertension of a compound of claim 1 and a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
26 words
A method for treating hypertension in mammals requiring said treatment, wherein the method comprises the administration of an effective amount of a compound of claim 1.
References Cited (Backward Citations)
US3959296A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-02-19 | 1988-08-20 | 1989-02-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-02-19 | 1992-08-20 | 1993-02-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-02-19 | 1996-08-20 | 1997-02-19 | $7700.00 | Window Closed / Lapsed |