US4145432A
Expired / Lapsed
US
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6-acyloryalkyl-1,4-dihydropyridine derivatives and a method of effecting vasodilation therewith
Assignee: Astellas Pharma Inc
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Filing: 1976-07-01
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Granted: 1979-03-20
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Expires: 1996-07-01
Abstract
Abstract This invention relates to 1,4-dihydropyridine derivatives. More particularly, it relates to new 1,4-dihydropyridine derivatives thereof which have vasodilating and anti-hypertensive activity, to processes for the preparation thereof, and to pharmaceutical composition comprising the same for therapeutical treatment in cardiovascular diseases and hypertension in human being.
Inventors
- 👤 Yoshinari Sato
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 13:35
CPC Classifications
C; C07; C07D; C07D405/00; C07D405/02; C07D405/04; A; A61; A61P; A61P9/00; A61P9/08; A61P9/10; A61P9/12; C07C; C07C205/00; C07C205/49; C07C205/56; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/90; C07D307/00; C07D307/02; C07D307/34; C07D307/38; C07D307/54; C07D333/00; C07D333/02; C07D333/04; C07D333/06; C07D333/24; C07D405/06; C07D409/00; C07D409/02; C07D409/04; C07D471/00; C07D471/02; C07D471/04; C07D491/00; C07D491/02; C07D491/04
Claims Analysis
Total Claims: 34
Claim 1
Independent Claim
45 words
A compound of the formula: ##STR25## wherein R 1 is phenyl, nitrophenyl or halophenyl, R 2 and R 3 are each lower alkoxycarbonyl or N-lower alkyl-N-phenyl(lower)alkylamino(lower)alkoxycarbonyl, R 4 is lower alkanoyloxy(lower)alkyl, carboxyalkanoyloxy(lower)alkyl, lower alkoxycarbonyl(lower)alkanoyloxy(lower)alkyl, N-lower alkyl-N-phenyl(lower)alkylamino(lower)alkanoyloxy(lower)alkyl, chlorophenoxy(lower)alkanoyloxy(lower)alkyl and benzoyloxy(lower)alkyl, and R 5 is lower alkyl.
Claim 2
Dependent Claim
45 words
A compound of the formula: ##STR25## wherein R 1 is phenyl, nitrophenyl or halophenyl, R 2 and R 3 are each lower alkoxycarbonyl or N-lower alkyl-N-phenyl(lower)alkylamino(lower)alkoxycarbonyl, R 4 is lower alkanoyloxy(lower)alkyl, carboxyalkanoyloxy(lower)alkyl, lower alkoxycarbonyl(lower)alkanoyloxy(lower)alkyl, N-lower alkyl-N-phenyl(lower)alkylamino(lower)alkanoyloxy(lower)alkyl, chlorophenoxy(lower)alkanoyloxy(lower)alkyl and benzoyloxy(lower)alkyl, and R 5 is lower alkyl.
Claim 3
Dependent Claim
13 words
A compound according to claim 1, wherein R 1 is nitrophenyl or halophenyl.
Claim 4
Dependent Claim
20 words
A compound according to claim 2, wherein R 2 is lower alkoxycarbonyl, and R 3 is lower alkoxycarbonyl or N-(lower)alkyl-N-phenyl(lower)alkylamino(lower)alkoxycarbonyl.
Claim 5
Dependent Claim
12 words
A compound according to claim 3, wherein R 4 is lower alkanoyloxy(lower)alkyl.
Claim 6
Dependent Claim
16 words
A compound according to claim 4, wherein R 2 and R 3 are each lower alkoxycarbonyl.
Claim 7
Dependent Claim
11 words
A compound according to claim 5, wherein R 1 is nitrophenyl.
Claim 8
Dependent Claim
28 words
A compound according to claim 6, wherein R 1 is 2-nitrophenyl, R 2 and R 3 are each ethoxycarbonyl, R 4 is acetoxymethyl, and R 5 is methyl.
Claim 9
Dependent Claim
28 words
A compound according to claim 6, wherein R 1 is 3-nitrophenyl, R 2 and R 3 are each ethoxycarbonyl, R 4 is acetoxymethyl, and R 5 is methyl.
Claim 10
Dependent Claim
11 words
A compound according to claim 5, wherein R 1 is halophenyl.
Claim 11
Dependent Claim
28 words
A compound according to claim 9, wherein R 1 is 2-chlorophenyl, R 2 and R 3 are each ethoxycarbonyl, R 4 is acetoxymethyl, and R 5 is methyl.
Claim 12
Dependent Claim
11 words
A compound according to claim 3, wherein R 4 is carboxy(lower)alkanoyloxy(lower)alkyl.
Claim 13
Dependent Claim
20 words
A compound according to claim 11, wherein R 1 are each halophenyl, R 2 and R 3 is lower alkoxycarbonyl.
Claim 14
Dependent Claim
28 words
A compound according to claim 12, wherein R 1 is 2-chlorophenyl, R 2 and R 3 are each ethoxycarbonyl, R 4 is 3-carboxypropionyloxymethyl, and R 5 is methyl.
Claim 15
Dependent Claim
12 words
A compound according to claim 3, wherein R 4 is lower alkoxycarbonyl(lower)alkanoyloxy(lower)alkyl.
Claim 16
Dependent Claim
21 words
A compound according to claim 14, wherein R 1 is halophenyl, and R 2 and R 3 are each lower alkoxycarbonyl.
Claim 17
Dependent Claim
28 words
A compound according to claim 15, wherein R 1 is 2-chlorophenyl, R 2 and R 3 are each ethoxycarbonyl, R 4 is 5-(ethoxycarbonyl)valeryloxymethyl, and R 5 is methyl.
Claim 18
Dependent Claim
18 words
A compound according to claim 4, wherein R 2 is lower alkoxycarbonyl, and R 3 is N-lower alkyl-N-phenyl(lower)alkylamino(lower)alkoxycarbonyl.
Claim 19
Dependent Claim
11 words
A compound according to claim 3, wherein R 4 is N-(lower)-alkyl-N-phenyl(lower)alkylamino(lower)alkanoyloxy(lower)-alkyl.
Claim 20
Dependent Claim
21 words
A compound according to claim 18, wherein R 1 is halophenyl, and R 2 and R 3 are each lower alkoxycarbonyl.
Claim 21
Dependent Claim
28 words
A compound according to claim 19, wherein R 1 is 2-chlorophenyl, R 2 and R 3 are each ethoxycarbonyl, R 4 is 3-(N-benzyl-N-methylamino)propionyloxymethyl, and R 5 is methyl.
Claim 22
Dependent Claim
11 words
A compound according to claim 3, wherein R 4 is benzoyloxy(lower)alkyl.
Claim 23
Dependent Claim
21 words
A compound according to claim 21, wherein R 1 is nitrophenyl, and R 2 and R 3 are each lower alkoxycarbonyl.
Claim 24
Dependent Claim
28 words
A compound according to claim 22, wherein R 1 is 2-nitrophenyl, R 2 and R 3 are each ethoxycarbonyl, R 4 is benzoylmethyl, and R 5 is methyl.
Claim 25
Dependent Claim
11 words
A compound according to claim 3, wherein R 4 is chlorophenoxy(lower)alkanoyloxy(lower)alkyl.
Claim 26
Dependent Claim
21 words
A compound according to claim 24, wherein R 1 is nitrophenyl, and R 2 and R 3 are each lower alkoxycarbonyl.
Claim 27
Dependent Claim
28 words
A compound according to claim 25, wherein R 1 is 2-nitrophenyl, R 2 and R 3 are each ethoxycarbonyl, R 4 is 2-(4-chlorophenoxy)acetoxymethyl, and R 5 is methyl.
Claim 28
Dependent Claim
11 words
A compound according to claim 17, wherein R 1 is nitrophenyl.
Claim 29
Dependent Claim
28 words
A compound according to claim 27, wherein R 1 is 3-nitrophenyl, R 2 is ethoxycarbonyl, R 3 is 2-(N-methyl-N-benzylamino)ethoxycarbonyl, R 4 is acetoxymethyl, and R 5 is methyl.
Claim 30
Dependent Claim
22 words
A method for effecting vasodilation in humans and mammals which comprises administering thereto an effective amount of the compound of claim 1.
Claim 31
Dependent Claim
34 words
A method for effecting vasodilation in humans and mammals which comprises administering thereto an oral daily dose of 0.1 to 500 mg. or 10 to 25% thereof intravenously of the compound of claim 1.
Claim 32
Dependent Claim
34 words
A method for effecting vasodilation in humans and mammals which comprises administering thereto an oral daily dose of 1 to 50 mg. or 10 to 25% thereof intravenously of the compound of claim 1.
Claim 33
Dependent Claim
35 words
A method for effecting vasodilation in humans and mammals which comprises administering thereto an oral daily dose of 1 μg to 10 mg./kg. or 10 to 25% thereof intravenously of the compound of claim 1.
Claim 34
Dependent Claim
34 words
A method for effecting vasodilation in humans and mammals which comprises administering thereto an oral daily dose of 0.5 to 5 mg./kg. or 10 to 25% thereof intravenously of the compound of 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) | 1982-03-19 | 1982-09-18 | 1983-03-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-19 | 1986-09-18 | 1987-03-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-19 | 1990-09-18 | 1991-03-20 | $7700.00 | Window Closed / Lapsed |