EP0151006A2
Expired / Lapsed
EP
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Dihydropyridine compounds, their production, pharmaceutical compositions containing them, and methods of producing these compositions
Assignee: Astellas Pharma Inc
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Filing: 1985-01-25
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Granted: —
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Expires: 2005-01-25
Abstract
Abstract Novel dihydropyridine compounds of the general formula (I) and salts thereof: wherein A represents a straight or branched carbon chain alkylene group having 1 to 10 carbon atoms which may be interrupted by one or more oxygen atoms; R 1 and R 4 are the same or different lower alkyl groups; R 2 represents an amino group. branched carbon chain alkyl group having 1 to 10 carbon atoms which may be interrupted by one or more oxygen atoms, or R 5 and R 6 which may be the same or different, each represents a hydrogen atom, a nitro group, a halogen atom, a trifluoromethyl group, a cyano group, a lower alkyl group, a lower alkoxy group or a lower alkenyloxy group; R 7 represents a hydrogen atom, a cyano group, a halogen atom, a lower alkoxy group or a lower alkanoyl group; R 8 and R 9 , which may be the same or different, each represents a lower alkyl group or an aralkyl group; and n is 1 or 2. These compounds possess both Ca 2+ -antagonistic and adrenergic β-receptor blocking activities.
Inventors
- 👤 Takashi Fujikura
- 👤 Noriki Ito
- 👤 Yuzo Matsumoto
- 👤 Masaharu Asano
- 👤 Toichi Takenaka
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-24 04:35
CPC Classifications
C; C07; C07D; C07D401/00; C07D401/02; C07D401/12; A; A61; A61P; A61P25/00; A61P25/02; A61P3/00; A61P3/12; A61P3/14; A61P9/00; A61P9/08; A61P9/10; A61P9/12; C07D211/00; C07D211/04; C07D211/80; C07D211/84; C07D211/90
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
199 words
1 . A dihydropyridine compound of the following general formula (I) or a salt thereof: wherein A represents a straight or branched carbon chain alkylene group having 1 to 10 carbon atoms which may be interrupted by one or more oxygen atoms; R 1 and R 4 are the same or different C 1 to C 4 alkyl groups; R 2 represents an amino group, or R 3 represents a straight or branched carbon chain alkyl group having 1 to 10 carbon atoms which may be interrupted by one or more oxygen atoms, or R 5 and R 6 are the same or different and selected from a hydrogen atom, a nitro group, halogen atoms, a trifluoromethyl group, a cyano group, C 1 to C 4 alkyl groups, C 1 to C 4 alkoxy groups, and C2 to C4 alkenyloxy groups; R 7 represents a hydrogen atom, a cyano group, a halogen atom, a C 1 to C 4 alkoxy group or a C 1 to C 5 alkanoyl group; R 8 and R 9 are the same or different and selected from C 1 to C 4 alkyl groups and aralkyl groups; and n is 1 or 2.
Claim 2
Dependent Claim
199 words
1 . A dihydropyridine compound of the following general formula (I) or a salt thereof: wherein A represents a straight or branched carbon chain alkylene group having 1 to 10 carbon atoms which may be interrupted by one or more oxygen atoms; R 1 and R 4 are the same or different C 1 to C 4 alkyl groups; R 2 represents an amino group, or R 3 represents a straight or branched carbon chain alkyl group having 1 to 10 carbon atoms which may be interrupted by one or more oxygen atoms, or R 5 and R 6 are the same or different and selected from a hydrogen atom, a nitro group, halogen atoms, a trifluoromethyl group, a cyano group, C 1 to C 4 alkyl groups, C 1 to C 4 alkoxy groups, and C2 to C4 alkenyloxy groups; R 7 represents a hydrogen atom, a cyano group, a halogen atom, a C 1 to C 4 alkoxy group or a C 1 to C 5 alkanoyl group; R 8 and R 9 are the same or different and selected from C 1 to C 4 alkyl groups and aralkyl groups; and n is 1 or 2.
Claim 3
Dependent Claim
72 words
A compound according to claim 1 wherein A is a straight or branched carbon chain alkylene group having 1 to 10 carbon atoms; R 2 is ; R 3 represents a straight or branched carbon chain alkyl group having 1 to 4 carbon atoms; and R 5 and R 6 are the same or different and selected from a hydrogen atom, a nitro group and C 1 to C 4 alkoxy groups.
Claim 4
Dependent Claim
29 words
At least one of the following compounds according to claim 1, or a salt thereof: 6-(2-hydroxy-3- p henoxypropylamino)hexyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate; 6-(2-hydroxy-3-phenoxypropylamino)hexyl methyl 2,6-dimethyl-4-(o-nitrophenyl)-1;4-dihydropyridine-3,5-dicarboxylate; 6-(2-hydroxy-3-phenoxypropylamino)hexyl methyl 2,6-dimethyl-4-(m-methoxyphenyl)-1,4-dihydropyridine-3,5-dicarboxylate; 6-(2-hydroxy-3-phenoxypropylamino)hexyl methyl 2,6-dimcthyl-4-(o-methoxyphenyl)-1,4-dihydropyridine-3,5-dicarboxylate.
Claim 5
Dependent Claim
22 words
4 . A pharmaceutical composition containing as an active ingredient thereof at least one compound according to claim 1, 2 or 3.
Claim 6
Dependent Claim
43 words
The use of a compound according to claim 1 for the manufacture of a medicament having both Ca 2+ - antagonistic action and adrenergic beta-receptor blocking activity, and/or at least one of intrinsic sympathomimetic activity, cerebral vasoconstriction-depressing activity, and central nervous system-improving activity.
Claim 7
Dependent Claim
36 words
The use of a compound according to claim 1 for the manufacture of a medicament for the treatment or prevention of at least one of ischemic heart-disease, cardiovascular disorder, cerebral vasoconstriction, and central nervous system disorder.
Claim 8
Dependent Claim
119 words
A process for producing a compound according to claim 1 which is characterised by reacting a compound of the formula: with a compound of the formula: wherein A, R 1 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , and n are as defined in claim 1;X represents a halogen atom; B represents an amino group or a protected amino group; and R 2 a represents a hydrogen atom, (wherein R 7 is as defined in claim 1) and may be a potassium atom when B represents a phthalimide group as protected amino; and further releasing the protective group when B is a protected amino group.
Claim 9
Dependent Claim
74 words
A process for producing a compound according to claim 1 which is characterised by reacting a compound of the formula: with a compound of the formula: . H 2 N- R 2 b wherein Z represents an organic sulfonic acid radical, R 2 b represents a hydrogen atom, and R 1 , R 3 , R 4 , R 5 , R 6 , R 7 and A are as defined in claim 1.
Claim 10
Dependent Claim
81 words
A process for producing a compound of the formula: which is characterised by reacting a compound of the formula: with a compound of the formula wherein R 2 c represents a phenyl group, a phenoxymethyl group which may be substituted by R 7 ,or a naphthyloxymethyl group; Z is an organic sulfonic acid radical; and R 1 , R 3 , R 4 , R 5 , R 6 , R 7 , and A are as defined in claim 1.
Claim 11
Dependent Claim
155 words
A process for producing a compound of the formula: which is characterised by [a] reacting a compound of the formula with a compound of the formula HO-A-protected amino [b] reacting the resulting compound of formula R 1 COCH 2 COO-A-protected amino with a compound of the formula [c] reacting the resulting compound of formula with a compound of the formula and [d] releasing the amino-protecting group of the resulting compound of formula wherein A, R 1 , R 3 , R 4 , R 5 , R 6 are as defined in claim 1 and R x represent a hydrogen atom or an alkyl group of lower carbon content than R 1 , the process for example producing the compound by (a) reacting the compound with the compound (b) reacting the resulting compound with the compound (c) reacting the resulting compound with the compound and (d) releasing the amino-protective groups of the resulting phthalimido compound-
References Cited (Backward Citations)
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