Patent US4258042A successfully refreshed from Google Patents.
US4258042A
Expired / Lapsed
US
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Antihypertensive pyridines and compositions
Assignee: USV Pharmaceutical Corp
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Filing: 1980-04-11
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Granted: 1981-03-24
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Expires: 2000-04-11
Abstract
Abstract Antihypertensive compounds of the formula <IMAGE> wherein R5 is H, alkyl, aryl, halo, lower alkoxy, nitro amino, alkylmercapto, cyano, carboxy, carbalkoxy, sulfamyl, trifluoromethyl, hydroxy, acyloxy, methanesulfonyl, alkylamino or acylamino; and each R1 and R2 is alkyl; wherein the alkyl, alkoxy and aryl groups contain up to 10 carbon atoms and non-toxic, pharmaceutically-acceptable acid addition salts thereof.
Inventors
- 👤 Bernard Loev
- 👤 James R. Shroff
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 21:40
CPC Classifications
C; C07; C07D; C07D211/00; C07D211/04; C07D211/06; C07D211/08; C07D211/18; C07D211/30; A; A61; A61P; A61P9/00; A61P9/12
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
145 words
A compound of the formula: ##STR9## wherein Ar is heteroaryl, cycloalkyl having from 3 to 7 carbon atoms, naphthyl, indanyl, indenyl, tetrahydronaphthyl, or a radical of the formula ##STR10## wherein each of R 5 , R 6 and R 7 is independently H, alkyl, aryl, halo, lower alkoxy, nitro, amino, alkylmercapto, cyano, carboxy, carbalkoxy, sulfamyl, trifluoromethyl, hydroxy, acyloxy, methanesulfonyl, alkylamino or acylamino; and R 5 and R 6 , when taken together, form a methylenedioxy; Z is alkylene containing 1 to about 5 carbon atoms in the principal chain; each R 1 is independently hydrogen, alkyl or alkoxyalkyl, with the proviso that only one R 1 may be hydrogen; R 2 is lower alkyl; and R 3 and R 4 are independently hydrogen or alkyl; wherein the alkyl, alkoxy, and acyl groups contain up to 10 carbon atoms, and their non-toxic, pharmaceutically-acceptable acid addition salts.
Claim 2
Dependent Claim
145 words
A compound of the formula: ##STR9## wherein Ar is heteroaryl, cycloalkyl having from 3 to 7 carbon atoms, naphthyl, indanyl, indenyl, tetrahydronaphthyl, or a radical of the formula ##STR10## wherein each of R 5 , R 6 and R 7 is independently H, alkyl, aryl, halo, lower alkoxy, nitro, amino, alkylmercapto, cyano, carboxy, carbalkoxy, sulfamyl, trifluoromethyl, hydroxy, acyloxy, methanesulfonyl, alkylamino or acylamino; and R 5 and R 6 , when taken together, form a methylenedioxy; Z is alkylene containing 1 to about 5 carbon atoms in the principal chain; each R 1 is independently hydrogen, alkyl or alkoxyalkyl, with the proviso that only one R 1 may be hydrogen; R 2 is lower alkyl; and R 3 and R 4 are independently hydrogen or alkyl; wherein the alkyl, alkoxy, and acyl groups contain up to 10 carbon atoms, and their non-toxic, pharmaceutically-acceptable acid addition salts.
Claim 3
Dependent Claim
19 words
A compound according to claim 1 wherein the alkyl, alkoxy and acyl groups contain up to 6 carbon atoms.
Claim 4
Dependent Claim
21 words
The compound according to claim 2 wherein Ar is a monosubstituted phenyl group and Z is --CH 2 --CH 2 --.
Claim 5
Dependent Claim
15 words
The compound according to claim 1 wherein heteroaryl is thienyl, furyl, thiazolyl, pyridyl or quinolinyl.
Claim 6
Dependent Claim
11 words
The compound according to claim 2 wherein Ar is a trifluoromethylphenyl.
Claim 7
Dependent Claim
19 words
The compound according to claim 2 wherein Ar is a trifluoromethylphenyl and Z is --CH 2 --CH 2 --.
Claim 8
Dependent Claim
2 words
Diethyl 1,4-dihydro-4-(2-trifluoromethylphenyl)-2,6-dimethyl-1-(2-morpholinoethyl)-3,5-pyridinedicarboxylate.
Claim 9
Dependent Claim
2 words
Diethyl 1,4-dihydro-4-(2-trifluoromethylphenyl)-2,6-dimethyl-1-(2-morpholinoethyl)-3,5-pyridinedicarboxylate.
Claim 10
Dependent Claim
12 words
A non-toxic, pharmaceutically-acceptable acid addition salt of the compound of claim 7.
Claim 11
Dependent Claim
20 words
An anti-hypertensive composition comprising an effective amount of a compound according to claim 1 admixed with a pharmaceutically acceptable carrier.
Claim 12
Dependent Claim
60 words
An anti-hypertensive compound of the formula ##STR11## wherein R 5 is H, alkyl, aryl, halo, lower alkoxy, nitro, amino, alkylmercapto, cyano, carboxy, carbalkoxy, sulfamyl, trifluoromethyl, hydroxy, acyloxy, methanesulfonyl, alkylamino or acylamino; and each R 1 and R 2 is alkyl; wherein the alkyl, alkoxy and acyl groups contain up to 10 carbon atoms and non-toxic, pharmaceutically-acceptable acid addition salts thereof.
Claim 13
Dependent Claim
60 words
An anti-hypertensive compound of the formula ##STR11## wherein R 5 is H, alkyl, aryl, halo, lower alkoxy, nitro, amino, alkylmercapto, cyano, carboxy, carbalkoxy, sulfamyl, trifluoromethyl, hydroxy, acyloxy, methanesulfonyl, alkylamino or acylamino; and each R 1 and R 2 is alkyl; wherein the alkyl, alkoxy and acyl groups contain up to 10 carbon atoms and non-toxic, pharmaceutically-acceptable acid addition salts thereof.
Claim 14
Dependent Claim
28 words
The compound according to claim 10 wherein R 1 is ethyl and R 2 is methyl, R 3 and R 4 are hydrogen, and R 5 is trifluoromethyl.
References Cited (Backward Citations)
JPS5170767A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-03-23 | 1984-09-22 | 1985-03-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-03-23 | 1988-09-22 | 1989-03-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-03-23 | 1992-09-22 | 1993-03-24 | $7700.00 | Window Closed / Lapsed |