US4590274A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Antihypertensive 1-[bis-(substituted phenyl)methyl]-4[2-(1,2,3,4-tetrahydro-substituted naphthalen-1-ylidene)ethyl]piperazines
Assignee: Bristol Myers Squibb Pharma Co
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Filing: 1985-01-03
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Granted: 1986-05-20
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Expires: 2005-01-03
Abstract
Abstract Antihypertensive piperazineethylidenebenzocycloalkanes are provided. These compounds have the formula: ##STR1## wherein R 1 , R 2 and R 3 are independently C 1 -C 6 alkyl, hydrogen, C 1 -C 6 alkoxy, hydroxy, or halo, or R 1 and R 2 or R 2 and R 3 together can form a methylenedioxy bridge; R 4 is H or C 1 -C 6 alkyl; n is 0, 1 or 2; m is 0, 1, 2 or 3; and Ar 1 and Ar 2 are independently phenyl optionally substituted with one or two of halogen, hydroxy, or C 1 -C 6 alkoxy groups, or a pharmaceutically acceptable salt thereof.
Inventors
- 👤 Anthony J. Cocuzza
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 01:57
CPC Classifications
C; C07; C07D; C07D295/00; C07D295/02; C07D295/027; C07D295/03; C07D295/04; C07D295/06; C07D295/073; C07D295/08; C07D295/096
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
100 words
A compound having the formula: ##STR35## wherein R 1 , R 2 and R 3 are independently n-C 1 -C 6 alkyl, hydrogen, C 1 -C 6 alkoxy, F,Cl,Br, or R 1 and R 2 or R 2 and R 3 together can form a methylenedioxy bridge; R 4 is H or C 1 -C 6 alkyl; n is 0, 1 or 2; m is 0, 1, 2 or 3; and Ar 1 and Ar 2 are independently phenyl optionally substituted with one or two of halogen, or C 1 -C 6 alkoxy groups, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
100 words
A compound having the formula: ##STR35## wherein R 1 , R 2 and R 3 are independently n-C 1 -C 6 alkyl, hydrogen, C 1 -C 6 alkoxy, F,Cl,Br, or R 1 and R 2 or R 2 and R 3 together can form a methylenedioxy bridge; R 4 is H or C 1 -C 6 alkyl; n is 0, 1 or 2; m is 0, 1, 2 or 3; and Ar 1 and Ar 2 are independently phenyl optionally substituted with one or two of halogen, or C 1 -C 6 alkoxy groups, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
28 words
A compound of claim 1 wherein R 1 , R 2 and R 3 are independently H, CH 3 or OCH 3 with at least one being H.
Claim 4
Dependent Claim
20 words
A compound of claim 1 wherein at least two of R 1 , R 2 and R 3 are H.
Claim 5
Dependent Claim
14 words
A compound of claim 1 wherein R 4 is H or CH 3 .
Claim 6
Dependent Claim
16 words
A compound of claim 1 wherein Ar 1 and Ar 2 are independently phenyl or fluorophenyl.
Claim 7
Dependent Claim
47 words
A compound of claim 1 wherein R 1 , R 2 and R 3 are independently H, CH 3 or OCH 3 with at least one being H; R 4 is H or CH 3 ; and Ar 1 and Ar 2 are independently phenyl or fluorophenyl.
Claim 8
Dependent Claim
10 words
A compound of claim 6 wherein R 4 is H.
Claim 9
Dependent Claim
9 words
The compound of claim 1 which is 1-[bis-(4-fluorophenyl)methyl]-4-[2-(1,2,3,4-tetrahydro-5-methoxynaphthalen-1-ylidene)ethyl]piperazine dihydrochloride.
Claim 10
Dependent Claim
24 words
A pharmaceutical composition for treating hypertension consisting essentially of a pharmaceutically acceptable carrier and an effective antihypertensive amount of a compound of claim 1.
Claim 11
Dependent Claim
20 words
A pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an antihypertensive amount of a compound of claim 2.
Claim 12
Dependent Claim
20 words
A pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an antihypertensive amount of a compound of claim 3.
Claim 13
Dependent Claim
20 words
A pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an antihypertensive amount of a compound of claim 4.
Claim 14
Dependent Claim
20 words
A pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an antihypertensive amount of a compound of claim 5.
Claim 15
Dependent Claim
20 words
A pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an antihypertensive amount of a compound of claim 6.
Claim 16
Dependent Claim
20 words
A pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an antihypertensive amount of a compound of claim 7.
Claim 17
Dependent Claim
20 words
A pharmaceutical composition consisting essentially of a pharmaceutically acceptable carrier and an antihypertensive amount of the compound of claim 8.
Claim 18
Dependent Claim
25 words
A method of treating hypertension in a mammal comprising essentially of administering to a hypertensive mammal an antihypertensive amount of a compound of claim 1.
Claim 19
Dependent Claim
25 words
A method of treating hypertension in a mammal consisting essentially of administering to a hypertensive mammal an antihypertensive amount of a compound of claim 2.
Claim 20
Dependent Claim
25 words
A method of treating hypertension in a mammal consisting essentially of administering to a hypertensive mammal an antihypertensive amount of a compound of claim 3.
Claim 21
Dependent Claim
25 words
A method of treating hypertension in a mammal comprising essentially of administering to a hypertensive mammal an antihypertensive amount of a compound of claim 4.
Claim 22
Dependent Claim
25 words
A method of treating hypertension in a mammal consisting essentially of administering to a hypertensive mammal an antihypertensive amount of a compound of claim 5.
Claim 23
Dependent Claim
25 words
A method of treating hypertension in a mammal consisting essentially of administering to a hypertensive mammal an antihypertensive amount of a compound of claim 6.
Claim 24
Dependent Claim
25 words
A method of treating hypertension in a mammal consisting essentially of administering to a hypertensive mammal an antihypertensive amount of a compound of claim 7.
Claim 25
Dependent Claim
25 words
A method of treating hypertension in a mammal consisting essentially of administering to a hypertensive mammal an antihypertensive amount of the compound of claim 8.
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Cited
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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) | 1989-05-19 | 1989-11-18 | 1990-05-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-05-19 | 1993-11-18 | 1994-05-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-05-19 | 1997-11-18 | 1998-05-20 | $7700.00 | Window Closed / Lapsed |