Patent US4515799A successfully refreshed from Google Patents.
US4515799A
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Dihydropyridine anti-ischaemic and antihypertensive agents
Assignee: Pfizer Inc
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Filing: 1983-07-19
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Granted: 1985-05-07
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Expires: 2003-07-19
Abstract
Abstract 1,4-Dihydropyridine derivatives of the formula: <IMAGE> (I) wherein R is aryl or heteroaryl; R1 and R2 are each independently C1-C4 alkyl or 2-methoxyethyl; Y is -(CH2)n-, -CH2CH(CH3)- or -CH2C(CH3)213 ; n is 1 to 3; and X is a 5 or 6 membered nitrogen containing aromatic heterocyclic ring which may optionally be substituted by one or more C1-C4 alkyl, phenyl, benzyl, CN, -N(R3)2, (CH2)mCO2H, (CH2)mCO2(C1-C4 alkyl) or (CH2)mCON(R3)2 group wherein each R3 is independently H or C1-C4 alkyl and m is 0 or 1; and their pharmaceutically acceptable acid addition salts, and pharmaceutical preparation containing such compounds, have utility as anti-ischaemic and antihypertensive agents.
Inventors
- 👤 Simon F. Campbell
- 👤 Peter E. Cross
- 👤 John K. Stubbs
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 06:49
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/90; C07D233/00; C07D233/54; C07D233/56; C07D249/00; C07D249/02; C07D249/08; C07D401/00; C07D401/02; C07D401/12; C07D413/00; C07D413/02; C07D413/12; C07D417/00; C07D417/02; C07D417/12
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
154 words
A 1,4-dihydropyridine compound having the formula: ##STR57## or a pharmaceutically acceptable acid addition salt thereof wherein: R is aryl; R 1 and R 2 are each independently C 1 -C 4 alkyl or 2-methoxyethyl; Y is --(CH 2 ) n --, --CH 2 CH(CH 3 )-- or --CH 2 C(CH 3 ) 2 --; n is an integer from 1 to 3; and X is imidazolyl or imidazolyl substituted by one or more C 1 -C 4 alkyl, phenyl, benzyl, cyano, --N(R 3 ) 2 , (CH 2 ) m CO 2 H, (CH 2 ) m CO 2 (C 1 -C 4 alkyl) or (CH 2 ) m CON(R 3 ) 2 groups wherein each R 3 is independently H or C 1 -C 4 alkyl and m is 0 or 1; with the proviso that if the imidazolyl is linked to Y by a ring nitrogen atom n is 2 or 3.
Claim 2
Dependent Claim
154 words
A 1,4-dihydropyridine compound having the formula: ##STR57## or a pharmaceutically acceptable acid addition salt thereof wherein: R is aryl; R 1 and R 2 are each independently C 1 -C 4 alkyl or 2-methoxyethyl; Y is --(CH 2 ) n --, --CH 2 CH(CH 3 )-- or --CH 2 C(CH 3 ) 2 --; n is an integer from 1 to 3; and X is imidazolyl or imidazolyl substituted by one or more C 1 -C 4 alkyl, phenyl, benzyl, cyano, --N(R 3 ) 2 , (CH 2 ) m CO 2 H, (CH 2 ) m CO 2 (C 1 -C 4 alkyl) or (CH 2 ) m CON(R 3 ) 2 groups wherein each R 3 is independently H or C 1 -C 4 alkyl and m is 0 or 1; with the proviso that if the imidazolyl is linked to Y by a ring nitrogen atom n is 2 or 3.
Claim 3
Dependent Claim
32 words
A compound according to claim 1, wherein X is imidazolyl, or imidazolyl substituted by one or more C 1 -C 4 alkyl, carbamoyl, carbamoylmethyl, amino or di-(C 1 -C 4 alkyl)amino groups.
Claim 4
Dependent Claim
12 words
A compound according to claim 2 wherein X is 2,4,5-trimethyl-1-imidazolyl or 1-methyl-2-imidazolyl.
Claim 5
Dependent Claim
16 words
A compound according to claim 1 wherein R 1 and R 2 are methyl or ethyl.
Claim 6
Dependent Claim
32 words
A compound according to claim 4 wherein X is imidazolyl, or imidazolyl substituted by one or more C 1 -C 4 alkyl, carbamoyl, carbamoylmethyl, amino or di-(C 1 -C 4 alkyl)amino groups.
Claim 7
Dependent Claim
12 words
A compound according to claim 5 wherein X is 2,4,5-trimethyl-1-imidazolyl, or 1-methyl-2-imidazolyl.
Claim 8
Dependent Claim
42 words
A compound according to claim 1 wherein R is phenyl; phenyl substituted by one or two substituents selected from the group consisting of nitro, halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, hydroxy, trifluoromethyl and cyano; 1-naphthyl; or 2-naphthyl.
Claim 9
Dependent Claim
32 words
A compound according to claim 7 wherein X is imidazolyl, or imidazolyl substituted by one or more C 1 -C 4 alkyl, carbamoyl, carbamoylmethyl, amino or di-(C 1 -C 4 alkyl)amino groups.
Claim 10
Dependent Claim
12 words
A compound according to claim 8 wherein X is 2,4,5-trimethyl-1-imidazolyl, or 1-methyl-2-imidazolyl.
Claim 11
Dependent Claim
16 words
A compound according to claim 7 wherein R 1 and R 2 are methyl or ethyl.
Claim 12
Dependent Claim
33 words
A compound according to claim 10 wherein X is imidazolyl, or imidazolyl substituted by one or more C 1 -C 4 alkyl, carbamoyl, carbamoylmethyl, amino or di-(C 1 -C 4 alkyl amino groups.
Claim 13
Dependent Claim
12 words
A compound according to claim 11 wherein X is 2,4,5-trimethyl-1-imidazolyl, or 1-methyl-2-imidazolyl.
Claim 14
Dependent Claim
12 words
A compound according to claim 7 wherein R is 2-chlorophenyl or 2,3-dichlorophenyl.
Claim 15
Dependent Claim
32 words
A compound according to claim 13 wherein X is imidazolyl, or imidazolyl substituted by one or more C 1 -C 4 alkyl, carbamoyl, carbamoylmethyl, amino or di(C 1 -C 4 alkyl)amino groups.
Claim 16
Dependent Claim
12 words
A compound according to claim 14 wherein X is 2,4,5-trimethyl-1-imidazolyl, or 1-methyl-2-imidazolyl.
Claim 17
Dependent Claim
16 words
A compound according to claim 13 wherein R 1 and R 2 are methyl or ethyl.
Claim 18
Dependent Claim
32 words
A compound according to claim 16 wherein X is imidazolyl, or imidazolyl substituted by one or more C 1 -C 4 alkyl, carbamoyl, carbamoylmethyl, amino or di-(C 1 -C 4 alkyl)amino groups.
Claim 19
Dependent Claim
12 words
A compound according to claim 17 wherein X is 2,4,5-trimethyl-1-imidazolyl, or 1-methyl-2-imidazolyl.
Claim 20
Dependent Claim
9 words
A compound according to claim 1 which is 4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-2-[2-(2,4,5-trimethyl-1-imidazolyl)ethoxymethyl]-1,4-dihydropyridine.
Claim 21
Dependent Claim
24 words
A pharmaceutical composition comprising an anti-ischameic or antihypertensive effective amount of a compound according to claim 1 and a pharmaceutically acceptable diluent or carrier.
Claim 22
Dependent Claim
35 words
A method of treating ischaemia in an animal in need of treatment comprising administering to said animal an effective anti-ischaemic a cardiac condition in man comprising administering amount of a compound according to claim 1.
Claim 23
Dependent Claim
28 words
A method of treating hypertension in an animal in need of treatment comprising administering to said animal an effective antihypertensive amount of a compound according to claim 1.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1988-05-06 | 1988-11-05 | 1989-05-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-05-06 | 1992-11-05 | 1993-05-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-05-06 | 1996-11-05 | 1997-05-07 | $7700.00 | Window Closed / Lapsed |