Patent US6454781B1 successfully refreshed from Google Patents.
US4430333A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Dihydropyridine anti-ischaemic and antihypertensive agents
Assignee: Pfizer Inc
•
Filing: 1982-03-11
•
Granted: 1984-02-07
•
Expires: 2002-03-11
Abstract
Abstract Dihydropyridine anti-ischaemic and antihypertensive agents of the formula: <IMAGE> (I) where Y is -(CH2)2- or -(CH2)3-; R is aryl or heteroaryl; R1 and R2 are each independently C1-C4 alkyl or 2-methoxyethyl; and R3 and R4 are each independently C1-C4 alkyl or aryl-(C1-C4 alkyl); or R3 and R4 taken together with the nitrogen atom to which they are attached represent a group of the formula: <IMAGE> where R5 is C1-C4 alkyl, aryl, aryl-(C1-C4 alkyl), benzhydryl; 2-methoxyethyl, 2-(N,N-di[C1-C4 alkyl]amino) ethyl, or cyclopropylmethyl; their pharmaceutically acceptable acid addition salts, processes for the preparation of the compounds, and pharmaceutical compositions containing them.
Inventors
- 👤 Simon F. Campbell
- 👤 Peter E. Cross
- 👤 John K. Stubbs
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 00:09
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/54; C07D213/55; C07D401/00; C07D401/02; C07D401/04; A; A61; A61P; A61P9/00; A61P9/06; A61P9/08; A61P9/10; A61P9/12; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/90; C07D409/00; C07D409/02; C07D409/04
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
100 words
A compound of the formula ##STR68## or a pharmaceutically acceptable acid addition salt thereof, wherein Y is --(CH 2 ) 2 -- or --(CH 2 ) 3 --; R is aryl; R 1 and R 2 are each independently C 1 -C 4 alkyl or 2-methoxyethyl; and R 3 and R 4 are each independently C 1 -C 4 alkyl or aryl-(C 1 -C 4 alkyl); wherein said aryl is phenyl; phenyl substituted by one or two substituents selected from nitro, halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, trifluoromethyl, and cyano; or is 1- or 2-naphthyl.
Claim 2
Dependent Claim
100 words
A compound of the formula ##STR68## or a pharmaceutically acceptable acid addition salt thereof, wherein Y is --(CH 2 ) 2 -- or --(CH 2 ) 3 --; R is aryl; R 1 and R 2 are each independently C 1 -C 4 alkyl or 2-methoxyethyl; and R 3 and R 4 are each independently C 1 -C 4 alkyl or aryl-(C 1 -C 4 alkyl); wherein said aryl is phenyl; phenyl substituted by one or two substituents selected from nitro, halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, trifluoromethyl, and cyano; or is 1- or 2-naphthyl.
Claim 3
Dependent Claim
50 words
A compound of claim 1 wherein R is 1-naphthyl; phenyl; or phenyl monosubstituted by halo, trifluoromethyl, cyano or nitro; and R 3 and R 4 are each independently C 1 -C 4 alkyl, or benzyl optionally monosubstituted on the aromatic ring portion by halo or C 1 -C 4 alkoxy.
Claim 4
Dependent Claim
38 words
A compound of claim 2 wherein Y is (CH 2 ) 2 ; R is 1-naphthyl or 2-chlorophenyl; R 1 and R 2 are each independently methyl or ethyl; and R 3 and R 4 are both methyl.
Claim 5
Dependent Claim
18 words
A compound of claim 3 wherein R is 2-chlorophenyl, R 1 is methyl and R 2 is ethyl.
Claim 6
Dependent Claim
18 words
A compound of claim 3 wherein R is 1-naphthyl and R 1 and R 2 are each ethyl.
Claim 7
Dependent Claim
23 words
A pharmaceutical composition comprising an anti-ischaemic or antihypertensive effective amount of a compound of claim 1 and a pharmaceutically acceptable diluent or carrier.
Claim 8
Dependent Claim
39 words
A pharmaceutical composition of claim 6 wherein Y is (CH 2 ) 2 ; R is 1-naphthyl or 2-chlorophenyl; R 1 and R 2 are each independently methyl or ethyl; and R 3 and R 4 are both methyl.
Claim 9
Dependent Claim
27 words
A method of treating hypertension in an animal in need of treatment comprising administering to said animal an effective anti-hypertensive amount of a compound of claim 1.
Claim 10
Dependent Claim
27 words
A method of treating ischaemia in an animal in need of treatment comprising administering to said animal an effective anti-ischaemic amount of a compound of claim 1.
Claim 11
Dependent Claim
42 words
A method according to claim 8 or claim 9 wherein Y is (CH 2 ) 2 ; R is 1-naphthyl or 2-chlorophenyl; R 1 and R 2 are each independently methyl or ethyl; and R 3 and R 4 are both methyl.
References Cited (Backward Citations)
US3905983A
Cited
US3943140A
Cited
US3946028A
Cited
US3946027A
Cited
DE2248150A1
Cited
BE843576A
Cited
GB1552911A
Cited
BE862107A
Cited
US4188395A
Cited
BE865658A
Cited
US4177278A
Cited
DE2935772A1
Cited
GB2034693B
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-02-06 | 1987-08-08 | 1988-02-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-02-06 | 1991-08-08 | 1992-02-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-02-06 | 1995-08-08 | 1996-02-07 | $7700.00 | Window Closed / Lapsed |