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Substituted piperazinyl alkyl esters of 2-amino-4-aryl-1,4-dihydro-6-alkyl-3,5-pyridinedicarboxylates

Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1984-09-25
•
Granted: 1986-07-29
•
Expires: 2004-09-25
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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 <IMAGE> wherein R1 is a hydrogen atom or an aryl, R2 and R3 are the same or different and each is an aryl, R4 and R6 are the same or different and each is a lower alkyl, R5 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, R5 is amino.

Inventors

  • 👤 Kanji Meguro
  • 👤 Akinobu Nagaoka

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-26 15:07
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: 13
Claim 1
Independent Claim 81 words
A compound of the formula ##STR17## wherein R 1 is hydrogen or phenyl optionally substituted by one or two halo, nitro, trifluoromethyl, C 1-6 -alkyl or C 1-3 -alkoxy groups, R 2 and R 3 are phenyl optionally aubstituted by one or two halo, nitro, trifluoromethyl, C 1-6 -alkyl or C 1-3 -alkoxy groups, R 4 and R 6 are C 1-6 -alkyl, A is C 2-4 -alkylene, m and n are 0 or 1, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim 81 words
A compound of the formula ##STR17## wherein R 1 is hydrogen or phenyl optionally substituted by one or two halo, nitro, trifluoromethyl, C 1-6 -alkyl or C 1-3 -alkoxy groups, R 2 and R 3 are phenyl optionally aubstituted by one or two halo, nitro, trifluoromethyl, C 1-6 -alkyl or C 1-3 -alkoxy groups, R 4 and R 6 are C 1-6 -alkyl, A is C 2-4 -alkylene, m and n are 0 or 1, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim 25 words
A compound claimed in claim 1, wherein R 1 , R 2 and R 3 are the same or different and each is a phenyl.
Claim 4
Dependent Claim 18 words
A compound claimed in claim 1, wherein R 3 is a phenyl which may be optionally be substituted.
Claim 5
Dependent Claim 10 words
A compound claimed claimed claim 1, wherein A is ethylene.
Claim 6
Dependent Claim 11 words
A compound 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 7
Dependent Claim 11 words
A compound 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 8
Dependent Claim 10 words
A compound claimed in claim 1, which is 5-[2-[4-(4,4'-difluorobenzhydryl)-1-piperazinyl]ethyl]3-isopropyl 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.
Claim 9
Dependent Claim 10 words
A compound 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 10
Dependent Claim 10 words
A compound 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 11
Dependent Claim 26 words
Coronary dilator composition which comprises an effective coronary dilator amount of a compound as defined in claim 1 and a pharmaceutically acceptable carrier or diluent therefor.
Claim 12
Dependent Claim 100 words
An anti-hypertensive pharmaceutically composition which comprises an effect anti-hypertensive amount of a compound of the formula ##STR18## wherein R 1 is hydrogen or phenyl optionally substituted by one or two halo, nitro, trifluromethyl, C 1-6 -alkyl or C 1-3 -alkoxy groups, R 2 and R 3 are phenyl optionally substituted by one or two halo, nito, trifluoromethyl, C 1-6 -alkyl or C 1-3 -alkoxy grouns, R 4 and R 6 are C 1-6 -alkyl, A is C 2-4 -alkylene, m and m are 0 or 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent therefor.
Claim 13
Dependent Claim 100 words
An anti-hypertensive pharmaceutically composition which comprises an effect anti-hypertensive amount of a compound of the formula ##STR18## wherein R 1 is hydrogen or phenyl optionally substituted by one or two halo, nitro, trifluromethyl, C 1-6 -alkyl or C 1-3 -alkoxy groups, R 2 and R 3 are phenyl optionally substituted by one or two halo, nito, trifluoromethyl, C 1-6 -alkyl or C 1-3 -alkoxy grouns, R 4 and R 6 are C 1-6 -alkyl, A is C 2-4 -alkylene, m and m are 0 or 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent therefor.

References Cited (Backward Citations)

US3485847A Cited
US3472853A Cited
GB1369401A Cited
US3905970A Cited
US3974275A Cited
US3996234A Cited
US4031104A Cited
US4038399A Cited
US3959292A Cited
US3985758A Cited
US4430333A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1989-07-28 1990-01-27 1990-07-29 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1993-07-28 1994-01-27 1994-07-29 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1997-07-28 1998-01-27 1998-07-29 $7700.00 Window Closed / Lapsed

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