US4307103A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Dihydropyridine derivative, processes for preparation thereof and pharmaceutical composition comprising the same
Assignee: Astellas Pharma Inc
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Filing: 1979-08-27
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Granted: 1981-12-22
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Expires: 1999-08-27
Abstract
Abstract This invention relates to a dihydropyridine derivative and a salt thereof. More particularly, it relates to a new dihydropyridine derivative and a pharmaceutically acceptable salt thereof which have vasodilating and anti-hypertensive activities, to processes for the preparation thereof, and to pharmaceutical composition comprising the same for therapeutical treatment of cardiovascular disorder and hypertension in human being.
Inventors
- 👤 Yoshinari Sato
- 👤 Tsutomu Teraji
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 19:17
CPC Classifications
C; C07; C07D; C07D401/00; C07D401/02; C07D401/12; A; A61; A61P; A61P9/00; A61P9/08; A61P9/10; A61P9/12; C07C; C07C323/00; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/90
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
93 words
A compound of the formula: ##STR17## wherein R 1 is nitro, halogen, cyano, trihalo(lower)alkyl or phenyl, R 2 is lower alkyl; [N-lower alkyl-N-mono or di halophenyl(lower)alkyl]amino(lower)alkyl; [N-lower alkyl-N-lower alkylphenyl(lower)alkyl]amino(lower)alkyl; [N-lower alkyl-N-lower alkoxyphenyl(lower)alkyl]amino(lower)alkyl; phthalimido(lower)alkyl; lower alkanoyloxy(lower)alkyl; lower alkylthio(lower)alkyl, phenyl(lower)alkylthio(lower)alkyl; or phenylthio(lower)alkyl; R 3 and R 4 are each lower alkyl, and R 5 is cyano or 2-cyanovinyl with a proviso that when R 1 is nitro, halogen, cyano or trihalo(lower)alkyl and R 2 is lower alkyl, R 3 and R 4 is lower alkyl, then R 5 is 2-cyanovinyl, and pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
93 words
A compound of the formula: ##STR17## wherein R 1 is nitro, halogen, cyano, trihalo(lower)alkyl or phenyl, R 2 is lower alkyl; [N-lower alkyl-N-mono or di halophenyl(lower)alkyl]amino(lower)alkyl; [N-lower alkyl-N-lower alkylphenyl(lower)alkyl]amino(lower)alkyl; [N-lower alkyl-N-lower alkoxyphenyl(lower)alkyl]amino(lower)alkyl; phthalimido(lower)alkyl; lower alkanoyloxy(lower)alkyl; lower alkylthio(lower)alkyl, phenyl(lower)alkylthio(lower)alkyl; or phenylthio(lower)alkyl; R 3 and R 4 are each lower alkyl, and R 5 is cyano or 2-cyanovinyl with a proviso that when R 1 is nitro, halogen, cyano or trihalo(lower)alkyl and R 2 is lower alkyl, R 3 and R 4 is lower alkyl, then R 5 is 2-cyanovinyl, and pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
26 words
A compound according to claim 1, wherein R 1 is nitro, cyano or trihalo(lower)alkyl, R 2 is [N-lower alkyl-N-mono- or dihalophenyl(lower)alkyl]amino(lower)alkyl, and R 5 is cyano.
Claim 4
Dependent Claim
14 words
A compound according to claim 2, wherein R 2 is [N-lower alkyl-N-mono- or dihalobenzyl]amino(lower)alkyl.
Claim 5
Dependent Claim
29 words
A compound according to claim 3, wherein R 1 is 3-nitro, 2-cyano or 2-trifluoromethyl, R 2 is 2-(N-methyl-N-4-mono- or 3,4-dichlorobenzylamino)ethyl, R 3 is ethyl, and R 4 is methyl.
Claim 6
Dependent Claim
18 words
A compound according to claim 4, wherein R 1 is 3-nitro, R 2 is 2-(N-methyl-N-4-chlorobenzylamino)ethyl, and its hydrochloride.
Claim 7
Dependent Claim
18 words
A compound according to claim 4, wherein R 1 is 3-nitro, R 2 is 2-(N-methyl-N-3,4-dichlorobenzylamino)ethyl, and its hydrochloride.
Claim 8
Dependent Claim
18 words
A compound according to claim 4, wherein R 1 is 2-cyano, R 2 is 2-(N-methyl-N-4-chlorobenzylamino)ethyl, and its hydrochloride.
Claim 9
Dependent Claim
18 words
A compound according to claim 4, wherein R 1 is 2-cyano, R 2 is 2-(N-methyl-N-3,4-dichlorobenzylamino)ethyl, and its hydrochloride.
Claim 10
Dependent Claim
18 words
A compound according to claim 4, wherein R 1 is 2-trifluoromethyl, R 2 is 2-(N-methyl-N-4-chlorobenzylamino)ethyl, and its hydrochloride.
Claim 11
Dependent Claim
18 words
A compound according to claim 4, wherein R 1 is 2-trifluoromethyl, R 2 is 2-(N-methyl-N-3,4-dichlorobenzylamino)ethyl, and its hydrochloride.
Claim 12
Dependent Claim
39 words
A compound according to claim 1, wherein R 1 is nitro, cyano, trihalo(lower)alkyl or phenyl, R 2 is lower alkyl, [N-lower alkyl-N-lower alkylphenyl(lower)alkyl]amino(lower)alkyl, [N-lower alkyl-N-lower alkoxyphenyl(lower)alkyl]amino(lower)alkyl, phthalimido(lower)alkyl, lower alkanoyloxy(lower)alkyl, lower alkylthio(lower)alkyl, phenyl(lower)alkylthio(lower)alkyl or phenylthio(lower)alkyl, and R 5 is cyano.
Claim 13
Dependent Claim
29 words
A compound according to claim 1, wherein R 1 is halogen, R 2 is lower alkyl, R 3 and R 4 are lower alkyl and R 5 is 2-cyanovinyl.
Claim 14
Dependent Claim
30 words
A pharmacuetical composition for treatment of cardiovascular disease or hypertension comprising an effective amount of the compound of claim 1 in association with a non-toxic, pharmaceutically acceptable carrier or excipient.
References Cited (Backward Citations)
US3974278A
Cited
DE2629892A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-12-21 | 1985-06-22 | 1985-12-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-12-21 | 1989-06-22 | 1989-12-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-12-21 | 1993-06-22 | 1993-12-22 | $7700.00 | Window Closed / Lapsed |