US4351832A
Expired / Lapsed
US
⏱️ 0.0 years remaining
2-(Piperazinyl)-4-pyrimidinamines
Assignee: Wyeth LLC
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Filing: 1981-03-20
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Granted: 1982-09-28
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Expires: 2001-03-20
Abstract
Abstract Herein is disclosed 2-(1-piperazinyl)-4-pyrimidinamine derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are distinguished most readily by having novel substituents at position 4 of the piperazinyl radical, the substituents being selected from the group consisting of 2-thiazoylyl, oxazolo(4,5-b)pyridin-2-yl and optionally substituted 1-(lower alkyl)-1H-benzimidazol-2-yl. The derivatives are useful for treating hypertension in a mammal.
Inventors
- 👤 Sumanas Rakhit
- 👤 Jehan F. Bagli
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 10:13
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/48; A; A61; A61K; A61K45/00; A61K45/06; C07D239/70; C07D239/72; C07D239/95
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
121 words
A compound of the formula ##STR32## in which R 1 and R 2 are hydrogen, or R 1 and R 2 together form a chain of the formula ##STR33## wherein R 6 , R 7 , R 8 and R 9 each is hydrogen or lower alkoxy; R 3 is selected from the group consisting of ##STR34## wherein R 10 is hydrogen, halo, lower alkyl, lower alkoxy, hydroxy, 1-oxo(lower)alkoxy or NR 11 R 12 wherein R 11 and R 12 each is hydrogen or lower alkyl; A is NR 13 wherein R 13 is lower alkyl; R 4 and R 5 each is hydrogen or lower alkyl; and n is 1 or 2; or a therapeutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim
121 words
A compound of the formula ##STR32## in which R 1 and R 2 are hydrogen, or R 1 and R 2 together form a chain of the formula ##STR33## wherein R 6 , R 7 , R 8 and R 9 each is hydrogen or lower alkoxy; R 3 is selected from the group consisting of ##STR34## wherein R 10 is hydrogen, halo, lower alkyl, lower alkoxy, hydroxy, 1-oxo(lower)alkoxy or NR 11 R 12 wherein R 11 and R 12 each is hydrogen or lower alkyl; A is NR 13 wherein R 13 is lower alkyl; R 4 and R 5 each is hydrogen or lower alkyl; and n is 1 or 2; or a therapeutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim
78 words
A compound of claim 1 of the formula ##STR35## in which R 4 , R 5 and R 6 are hydrogen, R 7 and R 8 each is lower alkoxy, R 9 is hydrogen or lower alkoxy, R 3 is selected from the group consisting of ##STR36## wherein a is NR 13 wherein R 13 is lower alkyl; R 10 is hydrogen, halo or lower alkoxy; and n is 1; or a therapeutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim
70 words
A compound of claim 1 of the formula ##STR37## in which R 4 , R 5 and R 6 are hydrogen, R 7 and R 8 each is lower alkoxy, R 9 is hydrogen or lower alkoxy, R 3 is selected from the group consisting of ##STR38## wherein A is NR 13 wherein R 13 is lower alkyl; and n is 1; or a therapeutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim
6 words
6,7-Dimethoxy-2-[4-(1-methyl-2-benzimidazolyl)-1-piperazinyl]-4-quinazolinamine, as claimed in claim 1.
Claim 6
Dependent Claim
6 words
6,7-Dimethoxy-2-[4-[1-(1-methylethyl)-1H-benzimidazol-2-yl]-1-piperazinyl]-4-quinazolinamine, as claimed in claim 1.
Claim 7
Dependent Claim
6 words
6,7-Dimethoxy-2-[4-(1-propyl-1H-benzimidazol-2-yl)-1-piperazinyl]-4-quinazolinamine, as claimed in claim 1.
Claim 8
Dependent Claim
6 words
6,7-Dimethoxy-2-[4-(2-thiazolyl)-1-piperazinyl]-4-quinazolinamine, as claimed in claim 1.
Claim 9
Dependent Claim
6 words
6,7-Dimethoxy-2-[4-(oxazolo[4,5-b]pyridin-2-yl)-1-piperazinyl]-4-quinazolinamine, as claimed in claim 1.
Claim 10
Dependent Claim
19 words
A pharmaceutical composition for treating hypertension, which comprises a compound of claim 1, and a pharmaceutically acceptable carrier therefor.
Claim 11
Dependent Claim
25 words
A method of treating hypertension in a hypertensive mammal, which comprises administering to said mammal an effective antihypertensive amount of a compound of claim 1.
Claim 12
Dependent Claim
52 words
A method of treating hypertension in a hypertensive mammal, which comprises administering to said mammal an antihypertensive effective amount of a compound of claim 1, in combination with an effective amount of a second therapeutic agent comprising a diuretic, an antihypertensive agent of a combination of a diuretic and an antihypertensive agent.
Claim 13
Dependent Claim
24 words
The method of claim 11 in which the second therapeutic agent is diuretic thiazide, a mineralocorticoid antagonizing diuretic agent or a β-adrenergic blocking agent.
Claim 14
Dependent Claim
16 words
The method of claim 11 in which the second therapeutic agent is chlorothiazide, hydrochlorothiazide or propranolol.
Claim 15
Dependent Claim
22 words
The method of claim 11 in which the compound of formula I, and the second therapeutic agent are administered sequentially or simultaneously.
Claim 16
Dependent Claim
20 words
A pharmaceutical composition comprising a compound of claim 1, and a second therapeutic agent comprising a diuretic or antihypertensive agent.
Claim 17
Dependent Claim
26 words
The pharmaceutical composition of claim 15 in which the second therapeutic agent is a diuretic thiazide, a mineralocorticoid antagonizing diuretic agent or a β-adrenergic blocking agent.
Claim 18
Dependent Claim
15 words
The pharmaceutical composition of claim 15 in which the agent is chlorothiazide, hydrochlorothiazide or propranolol.
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) | 1985-09-27 | 1986-03-29 | 1986-09-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-09-27 | 1990-03-29 | 1990-09-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-09-27 | 1994-03-29 | 1994-09-28 | $7700.00 | Window Closed / Lapsed |