US4060615A
Expired / Lapsed
US
⏱️ 0.0 years remaining
2-Piperazinyl-6,7-dimethoxyquinazolines
Assignee: Mead Johnson and Co LLC
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Filing: 1976-02-18
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Granted: 1977-11-29
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Expires: 1996-02-18
Abstract
Abstract A series of novel 4-amino or 4-hydrazino-2-(substituted piperazinyl)-6,7-dimethoxyquinazolines is disclosed having antihypertensive and phosphodiesterase inhibiting properties. Piperazinyl substituents include cycloalkenylcarbonyl, cycloalkylcarbonyl, and methylcycloalkylcarbonyl. A representative embodiment of the invention is 4-amino-2-[4-(cyclopentylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazo line.
Inventors
- 👤 William Lesley Matier
- 👤 John David Catt
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 18:50
CPC Classifications
C; C07; C07D; C07D403/00; C07D403/02; C07D403/04; C07D405/00; C07D405/02; C07D405/12
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
40 words
A compound having the formula ##STR11## or a pharmaceutically acceptable salt thereof wherein R is amino or hydrazino; R 1 is cycloalkyl having 3 to 8 ring carbon atoms inclusive and cycloalkenyl having 4 to 8 ring carbon atoms inclusive.
Claim 2
Dependent Claim
40 words
A compound having the formula ##STR11## or a pharmaceutically acceptable salt thereof wherein R is amino or hydrazino; R 1 is cycloalkyl having 3 to 8 ring carbon atoms inclusive and cycloalkenyl having 4 to 8 ring carbon atoms inclusive.
Claim 3
Dependent Claim
9 words
The compound defined in claim 1 which is 4-amino-2-[4-(cyclopentylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline.
Claim 4
Dependent Claim
10 words
The compound defined in claim 1 which is 4-amino-2-[4-(cyclopentylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline hydrochloride.
Claim 5
Dependent Claim
9 words
The compound defined in claim 1 which is 4-amino-2-[4-(cyclopropylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline.
Claim 6
Dependent Claim
9 words
The compound defined in claim 1 which is 4-amino-2-[4-(cyclohexylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline.
Claim 7
Dependent Claim
9 words
The compound defined in claim 1 which is 4-amino-2-[4-(1-cyclopenten-1-ylcarbonyl)piperazinyl]-6,7-dimethoxyquinazoline.
Claim 8
Dependent Claim
9 words
The compound defined in claim 1 which is 4-amino-2-[4-(3-cyclopentenylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline.
Claim 9
Dependent Claim
9 words
The compound defined in claim 1 which is 4-amino-2-[4-(3-cyclohexenylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline.
Claim 10
Dependent Claim
9 words
The compound defined in claim 1 which is 4-amino-2-[4-(cyclobutylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline.
Claim 11
Dependent Claim
10 words
The compound defined in claim 1 which is 4-amino-2-[4-(cyclobutylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline hydrochloride.
Claim 12
Dependent Claim
9 words
The compound defined in claim 1 which is 4-amino-2-[4-(cycloheptylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline.
Claim 13
Dependent Claim
10 words
The compound defined in claim 1 which is 4-amino-2-[4-(cycloheptylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline hydrochloride.
Claim 14
Dependent Claim
62 words
A process for treating hypertension which comprises systemically administering to a mammal in need of said treatment an antihypertensive effective amount of a compound having the formula ##STR12## or a pharmaceutically acceptable salt thereof wherein R is amino or hydrazino; R 1 is cycloalkyl having 3 to 8 ring carbon atoms inclusive and cycloalkenyl having 4 to 8 ring carbon atoms inclusive.
Claim 15
Dependent Claim
62 words
A process for treating hypertension which comprises systemically administering to a mammal in need of said treatment an antihypertensive effective amount of a compound having the formula ##STR12## or a pharmaceutically acceptable salt thereof wherein R is amino or hydrazino; R 1 is cycloalkyl having 3 to 8 ring carbon atoms inclusive and cycloalkenyl having 4 to 8 ring carbon atoms inclusive.
Claim 16
Dependent Claim
10 words
The process of claim 13 wherein said compound is 4-amino-2-[4-(cyclopentylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline.
Claim 17
Dependent Claim
11 words
The process of claim 13 wherein said compound is 4-amino-2-[4-(cyclopentylcarbonyl-1-piperazinyl]-6,7-dimethoxyquinazoline hydrochloride.
Claim 18
Dependent Claim
73 words
A pharmaceutical composition in dosage unit form adapted for the systemic administration to a mammal comprising a dose of from 0.001 to 50 mg. per kilogram of body weight of said mammal of a compound having the formula ##STR13## or a pharmaceutically acceptable salt thereof wherein R is amino or hydrazino; R 1 is cycloalkyl having 3 to 8 ring carbon atoms inclusive and cycloalkenyl having 4 to 8 ring carbon atoms inclusive.
Claim 19
Dependent Claim
73 words
A pharmaceutical composition in dosage unit form adapted for the systemic administration to a mammal comprising a dose of from 0.001 to 50 mg. per kilogram of body weight of said mammal of a compound having the formula ##STR13## or a pharmaceutically acceptable salt thereof wherein R is amino or hydrazino; R 1 is cycloalkyl having 3 to 8 ring carbon atoms inclusive and cycloalkenyl having 4 to 8 ring carbon atoms inclusive.
Claim 20
Dependent Claim
10 words
The composition of claim 16 wherein said compound is 4-amino-2-[4-(cyclopentylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline.
Claim 21
Dependent Claim
11 words
The compound of claim 16 wherein said compound is 4-amino-2-[4-(cyclopentylcarbonyl)-1-piperazinyl]-6,7-dimethoxyquinazoline hydrochloride.
Claim 22
Dependent Claim
3 words
The compound 4-amino-6,7-dimethoxy-2-[4-[(1-methylcyclohexyl)carbonyl]-1-piperazinyl]quinazoline.
Claim 23
Dependent Claim
3 words
The compound 4-amino-6,7-dimethoxy-2-[4-[(1-methylcyclohexyl)carbonyl]-1-piperazinyl]quinazoline.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-11-28 | 1981-05-30 | 1981-11-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-11-28 | 1985-05-30 | 1985-11-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-11-28 | 1989-05-30 | 1989-11-29 | $7700.00 | Window Closed / Lapsed |