Patent US4886819A successfully refreshed from Google Patents.
US4886819A
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Dihydropyridine derivatives and pharmaceutical composition thereof
Assignee: Tanabe Pharma Corp
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Filing: 1987-08-20
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Granted: 1989-12-12
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Expires: 2007-08-20
Abstract
Abstract Dihydropyridine derivatives of the formula <IMAGE> (I) wherein R1, R2, R3, R4, R5, A, B are defined as in the specification and nontoxic acid-addition salts thereof, have an excellent calcium blocking action (Ca-antagonist), and antihypertensive action, a platelet aggregation-inhibiting action, a phosphodiesterase-inhibiting action and the like, and thus are useful as a medicine, such as a coronary vasocilator, a cerebral hyperkinemic, antihypertensive, thrombosis-preventing or -treating agents, phosphodiesterase-inhibitor or the like. Pharmaceutical compositions and methods of use are also disclosed.
Inventors
- 👤 Atsuyuki Ashimori
- 👤 Taizo Ono
- 👤 Yoshihisa Inoue
- 👤 Chikara Fukaya
- 👤 Kazumasa Yokoyama
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 14:29
CPC Classifications
C; C07; C07D; C07D401/00; C07D401/02; C07D401/04; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/90
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
211 words
A compound of the formula ##STR14## wherein each of R 1 , R 2 and R 3 is, independently, lower alkyl, C 3-6 cycloalkyl or lower alkoxy lower alkyl; each of R 4 and R 5 is, independently, a hydrogen atom, halogen, nitro, halogenated lower alkyl, lower alkylsulfonyl, halogenated lower alkoxy, lower alkylsulfinyl, lower alkyl, C 3-6 cycloalkyl, lower alkoxy, cyano, lower alkoxycarbonyl or lower alkylthio (wherein both R 4 and R 5 are not hydrogen atoms at the same time); X is a group represented by vinylene or azomethine; A is alkylene having from 2 to 4 carbon atoms; B is -N(R 6 ) 2 or ##STR15## each of R 6 and R 7 is, independently, a hydrogen atom, lower alkyl, C 3-6 cycloalkyl, aralkyl (the alkyl of which has from 1 to 3 carbon atoms), phenyl, substituted phenyl, naphthyl, substituted napthyl (any substituent of substituted phenyl or of substituted naphthyl having one of the meanings of R 4 ), or pyridyl; each of Ar and ar of aralkyl is phenyl, substituted phenyl, naphthyl, substituted naphthyl (any substitutent of substituted phenyl or of substituted naphthyl having one of the meanings of R 4 ) pyridyl and n is an integer from 0 to 2, inclusive. or an acid-addition salt thereof.
Claim 2
Dependent Claim
211 words
A compound of the formula ##STR14## wherein each of R 1 , R 2 and R 3 is, independently, lower alkyl, C 3-6 cycloalkyl or lower alkoxy lower alkyl; each of R 4 and R 5 is, independently, a hydrogen atom, halogen, nitro, halogenated lower alkyl, lower alkylsulfonyl, halogenated lower alkoxy, lower alkylsulfinyl, lower alkyl, C 3-6 cycloalkyl, lower alkoxy, cyano, lower alkoxycarbonyl or lower alkylthio (wherein both R 4 and R 5 are not hydrogen atoms at the same time); X is a group represented by vinylene or azomethine; A is alkylene having from 2 to 4 carbon atoms; B is -N(R 6 ) 2 or ##STR15## each of R 6 and R 7 is, independently, a hydrogen atom, lower alkyl, C 3-6 cycloalkyl, aralkyl (the alkyl of which has from 1 to 3 carbon atoms), phenyl, substituted phenyl, naphthyl, substituted napthyl (any substituent of substituted phenyl or of substituted naphthyl having one of the meanings of R 4 ), or pyridyl; each of Ar and ar of aralkyl is phenyl, substituted phenyl, naphthyl, substituted naphthyl (any substitutent of substituted phenyl or of substituted naphthyl having one of the meanings of R 4 ) pyridyl and n is an integer from 0 to 2, inclusive. or an acid-addition salt thereof.
Claim 3
Dependent Claim
16 words
A compound as claimed in claim 1, wherein A is ethylene, or an acid-addition salt thereof.
Claim 4
Dependent Claim
16 words
A compound as claimed in claim 1, wherein X is azomethine, or an acid-addition salt thereof
Claim 5
Dependent Claim
16 words
A compound as claimed in claim 1, wherein X is vinylene, or an acid-addition salt thereof.
Claim 6
Dependent Claim
16 words
A compound as claimed in claim 1, wherein Ar is phenyl, or an acid-addition salt thereof.
Claim 7
Dependent Claim
17 words
A compound as claimed in claim 1, wherein R 6 is benzyl, or an acid-addition salt thereof.
Claim 8
Dependent Claim
18 words
A compound as claimed in claim 1, wherein R 6 is lower alkyl, or an acid-addition salt thereof.
Claim 9
Dependent Claim
24 words
A compound as claimed in claim 1, wherein both R 7 and Ar are phenyl and n is 1, or an acid-addition salt thereof.
Claim 10
Dependent Claim
26 words
A compound as claimed in claim 1, wherein Ar is phenyl, X is vinylene, A is ethylene and n is 0, or an acid-addition salt thereof.
Claim 11
Dependent Claim
28 words
A compound as claimed in claim 1, wherein each of R 7 and Ar is phenyl, X is vinylene, and n is 1, or an acid-addition salt thereof.
Claim 12
Dependent Claim
45 words
A compound as claimed in claim 1, wherein X is azomethine, R 4 or R 5 is trifluoromethyl or cyano, A is ethylene, and B is ##STR16## wherein each of R 7 and Ar is phenyl and n is (1), or an acid-addition salt thereof.
Claim 13
Dependent Claim
43 words
A compound as claimed in claim 1, wherein X is vinylene, R 4 or R 5 is nitro, A is ethylene, and B is ##STR17## wherein, each of R 7 and Ar is phenyl, and n is (1), or an acid-addition salt thereof.
Claim 14
Dependent Claim
134 words
A compound as claimed in claim 1 wherein: each alkyl has from 1 to 6 carbon atoms, each cycloalkyl has from 3 to 6 ring carbon atoms, each alkoxyalkyl has from 3 to 7 atoms, each halogenated alkyl has from 1 to 4 carbon atoms, each alkylsulfonyl has from 1 to 6 carbon atoms, each halogenated alkoxy has from 1 to 3 carbon atoms, each alkysulfinyl has from 1 to 6 carbon atoms, each alkoxy has from 1 to 3 carbon atoms, each alkoxycarbonyl has from 2 to 4 carbon atoms, each alkylthio has from 1 to 3 carbon atoms, each alkylene has from 2 to 4 carbon atoms, the alkyl of each aralkyl has from 1 to 3 carbon atoms, and each aryl and the ar of each aralkyl is phenyl or naphthyl.
Claim 15
Dependent Claim
31 words
A compound according to claim 1 which is pharmacologically acceptable and wherein each of Ar and ar of aralkyl is phenyl, naphthyl or pyridyl, and each phenyl or naphthyl is unsubstituted.
Claim 16
Dependent Claim
32 words
A pharmaceutical composition for prophylaxis or treatment of hypertension which comprises an effective amount of at least one compound as claimed in claim 1 or an acid-addition salt thereof, and pharmaceutically-acceptable additive.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-12-11 | 1993-06-12 | 1993-12-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-12-11 | 1997-06-12 | 1997-12-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-12-11 | 2001-06-12 | 2001-12-12 | $7700.00 | Window Closed / Lapsed |