EP0138505A2
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Dihydropyridine derivatives, their production and use
Assignee: Takeda Pharmaceutical Co Ltd
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Filing: 1984-10-02
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Granted: —
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Expires: 2004-10-02
Abstract
Abstract Dihydropyridine derivatives and acid addition salts thereof which are of use as prophylactic or/and therapeutic drugs for cardiovascular diseases, said dihydropyridine derivatives having the formula wherein R 1 is a hydrogen atom or an aryl, R 2 and R 3 are the same or different and each is an aryl, R 4 and R 6 are the same of different and each is a lower alkyl, R 5 is amino or a lower alkyl, A is an alkylene, X is N or CH and m and n are the same or different and each is 0 or 1, with the proviso that when X is N, R 5 is amino.
Inventors
- 👤 Kanji Meguro
- 👤 Akinobu Nagaoka
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-27 16:56
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/04; C07D295/08; C07D295/084; C07D295/088; C07D211/00; C07D211/04; C07D211/06; C07D211/08; C07D211/10; C07D211/14; C07D211/80; C07D211/84; C07D211/90
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
95 words
A dihydropyridine derivative of the formula wherein R 1 is a hydrogen atom or an aryl, R and R are the same or different and each is an aryl, R 4 and R 6 are the same or different and each is a lower alkyl, R 5 is amino or a lower alkyl, A is an alkylene, X is N or CH and m and n are the same or different and each is O or 1, with the proviso that when X is N, R 5 is amino, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
95 words
A dihydropyridine derivative of the formula wherein R 1 is a hydrogen atom or an aryl, R and R are the same or different and each is an aryl, R 4 and R 6 are the same or different and each is a lower alkyl, R 5 is amino or a lower alkyl, A is an alkylene, X is N or CH and m and n are the same or different and each is O or 1, with the proviso that when X is N, R 5 is amino, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
26 words
A dihydropyridine derivative claimed in Claim 1, wherein R l , R 2 and R 3 are the same or different and each is a phenyl.
Claim 4
Dependent Claim
18 words
A dihydropyridine derivative claimed in Claim 1, wherein R 3 is a phenyl which may optionally be substituted.
Claim 5
Dependent Claim
11 words
A dihydropyridine derivative claimed in Claim 1, wherein A is ethylene.
Claim 6
Dependent Claim
11 words
A dihydropyridine derivative claimed in Claim 1, wherein X is N.
Claim 7
Dependent Claim
12 words
A dihydropyridine derivative claimed in Claim 1, which is 5-[2-(4-benzhydryl-1-piperazinyl)ethyl] 3-ethyl 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 8
Dependent Claim
12 words
A dihydropyridine derivative claimed in Claim 1, which is 5-[2-[4-(4,4'-dimethylbenzhydryl)-1-piperazinyl]-ethyl] 3-ethyl 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 9
Dependent Claim
12 words
A dihydropyridine derivative claimed in Claim 1, which is 5-[2-[4-(4,4'-difluorobenzhydryl)-1-piperazinyl]ethyl] 3-isopropyl 2-amino-l,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 10
Dependent Claim
12 words
A dihydropyridine derivative claimed in Claim 1, which is 5-[2-[4-(4,4'-dichlorobenzhydryl)-1-piperazinyl]ethyl] 3-ethyl 2-amino-4-(2,3-dichlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate.
Claim 11
Dependent Claim
12 words
A dihydropyridine derivative claimed in Claim 1, which is 3-ethyl 5-[2-[4-(4,4'-difluorobenzhydryl)-1-piperazinyl]-ethyl] 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 12
Dependent Claim
12 words
A dihydropyridine derivative claimed in Claim 1, which is 2-(4-diphenylmethylpiperidino)ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 13
Dependent Claim
32 words
A pharmaceutical composition which comprises, an effective amount of a dihydropyridine derivative or its salt as defined in any of claims 1 to 11, and a pharmaceutically acceptable carrier or diluent therefor.
Claim 14
Dependent Claim
133 words
A process for producing a dihydropyridine derivative of the formula wherein R 1 is a hydrogen atom or an aryl, R 2 and R 3 are the same or different and each is an aryl, R 4 and R 6 are the same or different and each is a lower alkyl, R 5 is amino or a lower alkyl, A is an alkylene, X is N or CH and m and n are the same or different and each is O or 1, with the proviso that when X is N, R 5 is amino, or a pharmaceutically acceptable salt thereof which comprises subjecting any one of the fra q ments capable of constituting the said derivative to cyclodehydration reaction with the remaining fragment(s), and if desired converting to said pharmaceutically acceptable salt.
Claim 15
Dependent Claim
133 words
A process for producing a dihydropyridine derivative of the formula wherein R 1 is a hydrogen atom or an aryl, R 2 and R 3 are the same or different and each is an aryl, R 4 and R 6 are the same or different and each is a lower alkyl, R 5 is amino or a lower alkyl, A is an alkylene, X is N or CH and m and n are the same or different and each is O or 1, with the proviso that when X is N, R 5 is amino, or a pharmaceutically acceptable salt thereof which comprises subjecting any one of the fra q ments capable of constituting the said derivative to cyclodehydration reaction with the remaining fragment(s), and if desired converting to said pharmaceutically acceptable salt.
Claim 16
Dependent Claim
114 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative of the formula: wherein R 1 is a hydrogen atom or an aryl R 2 and R 3 are the same or different and each is an aryl, R 4 and R 6 are the same or different and each is a lower alkyl, R 5 is amino or a lower alkyl, A is an alkylene, X is N or CH and m and n are the same or different and each is 0 or 1, with the proviso that when X is N, R 5 is amino, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent therefor.
Claim 17
Dependent Claim
114 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative of the formula: wherein R 1 is a hydrogen atom or an aryl R 2 and R 3 are the same or different and each is an aryl, R 4 and R 6 are the same or different and each is a lower alkyl, R 5 is amino or a lower alkyl, A is an alkylene, X is N or CH and m and n are the same or different and each is 0 or 1, with the proviso that when X is N, R 5 is amino, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent therefor.
Claim 18
Dependent Claim
36 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, wherein R 1 , R 2 and R 3 are the same or different and each is a phenyl.
Claim 19
Dependent Claim
28 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, wherein R 3 is a phenyl which may optionally be substituted.
Claim 20
Dependent Claim
21 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, wherein A is ethylene.
Claim 21
Dependent Claim
21 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, wherein X is N.
Claim 22
Dependent Claim
22 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, which is 5-[2-(4-benzhydryl-l-piperazinyl)ethyl] 3-ethyl 2-amino-l,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 23
Dependent Claim
23 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, which is 5-[2-[4-(4,4'-dimethylbenzhydryl)-l-piperazinyl]-ethyl] 3-ethyl 2-amino-l, 4-dihydro-6-methyl-4-)3-nitro-phenyl-3,5-pyridinedicarboxylate..
Claim 24
Dependent Claim
23 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, which is 5-[2-[4-)4,4'-difluorobenzhydryl)-l-piperazinyl)ethyl] 3-isopropyl 2-amino-1, 4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 25
Dependent Claim
23 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, which is 5-[2-[4-(4,4'-dichlorobenzhydryl)-l-piperazinyl]ethyl] 3-ethyl 2 amino-4-(2,3-dichlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate.
Claim 26
Dependent Claim
22 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, which is 3-ethyl 5-[2-[4-(4,4'-difluorobenzhydryl)-l-piperazinyl]-ethyl] 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 27
Dependent Claim
23 words
A pharmaceutical composition which comprises an effective amount of a dihydropyridine derivative as defined in Claim 1, which is 2-(4-diphenylmethylpiperidino) ethyl methyl 1,4-dihydro-2,6,-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 28
Dependent Claim
133 words
A process for producing a novel dihydropyridine derivative of the formula wherein R 1 is a hydrogen atom or an aryl, R 2 and R 3 are the same or different and each is an aryl, R 4 and R 6 are the same or different and each is a lower alkyl, R 5 is amino or a lower alkyl, A is an alkylene, X is N or CH and m and n are the same or different and each is 0 or 1, with the proviso that when X is N , R 5 is amino, or a pharmaceutically acceptable salt thereof which comprises subjecting any one of the fragments capable of constituting the said derivative to cyclodehydration reaction with the remaining fragment(s), and if desired, converting to said pharmaceutically acceptable salt.
Claim 29
Dependent Claim
133 words
A process for producing a novel dihydropyridine derivative of the formula wherein R 1 is a hydrogen atom or an aryl, R 2 and R 3 are the same or different and each is an aryl, R 4 and R 6 are the same or different and each is a lower alkyl, R 5 is amino or a lower alkyl, A is an alkylene, X is N or CH and m and n are the same or different and each is 0 or 1, with the proviso that when X is N , R 5 is amino, or a pharmaceutically acceptable salt thereof which comprises subjecting any one of the fragments capable of constituting the said derivative to cyclodehydration reaction with the remaining fragment(s), and if desired, converting to said pharmaceutically acceptable salt.
References Cited (Backward Citations)
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