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US4306065A Expired / Lapsed US ⏱️ 0.0 years remaining

2-Aryl-4-substituted quinazolines

Assignee: Wyeth LLC
•
Filing: 1979-12-19
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Granted: 1981-12-15
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Expires: 1999-12-19
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Abstract

Abstract Novel hypotensive agents are disclosed which are quinazolines substituted in the 2 and 4 position having the general formula: ##STR1## wherein Q is a secondary amine radical illustrated by loweralkanolylamino or a tertiary amine radical such as pyrrolidinyl, piperidinyl or piperazinyl, any of which may be substituted by various groups such as loweralkanolyl.

Inventors

  • 👤 Ying-Ho Chen

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 09:57
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/70; C07D239/72; C07D239/86; C07D239/94

Claims Analysis

Total Claims: 25
Claim 1
Independent Claim 155 words
A compound suitable for treating hypertension in warm blooded animals selected from the group having the formula: ##STR7## wherein Q is ##STR8## R is selected from hydrogen, hydroxy, loweralkoxy, loweralkanolyl, phenoxy or phenoxy substituted by loweralkyl, loweralkoxy, trifluoromethyl, amino, nitro or halo; Z is selected from ##STR9## and p is zero to one inclusive; R 1 is selected from loweralkyl, 2-pyridyl, loweralkenyloxy-loweralkanolyl, loweralkynyloxy-loweralkanolyl, loweralkanyloxy-lowralkanolyl, phenoxy-loweralkanolyl and phenoxy-loweralkanolyl having phenoxy substituted by loweralkoxy, loweralkyl, nitro, amino, trifluoromethyl and halo; R 2 is selected from hydrogen, hydroxy and loweralkyl, loweralkoxy, phenoxy or naphthoxy; R 3 is selected from 4-cyanocycloalkyl-loweralkyl, phenoxy-loweralkanolyl and phenoxy-loweralkanolyl having phenoxy substituted by loweralkoxy, loweralkyl, nitro, amino, trifluoromethyl and halo; R 4 is selected from hydrogen or loweralkyl, X is selected from hydrogen, loweralkyl, loweralkoxy, nitro, amino or halo and n is one to three; Y is loweralkyl and m is 0 to 2 inclusive and the pharmaceutically acceptable addition salts and hydrates thereof.
Claim 2
Dependent Claim 155 words
A compound suitable for treating hypertension in warm blooded animals selected from the group having the formula: ##STR7## wherein Q is ##STR8## R is selected from hydrogen, hydroxy, loweralkoxy, loweralkanolyl, phenoxy or phenoxy substituted by loweralkyl, loweralkoxy, trifluoromethyl, amino, nitro or halo; Z is selected from ##STR9## and p is zero to one inclusive; R 1 is selected from loweralkyl, 2-pyridyl, loweralkenyloxy-loweralkanolyl, loweralkynyloxy-loweralkanolyl, loweralkanyloxy-lowralkanolyl, phenoxy-loweralkanolyl and phenoxy-loweralkanolyl having phenoxy substituted by loweralkoxy, loweralkyl, nitro, amino, trifluoromethyl and halo; R 2 is selected from hydrogen, hydroxy and loweralkyl, loweralkoxy, phenoxy or naphthoxy; R 3 is selected from 4-cyanocycloalkyl-loweralkyl, phenoxy-loweralkanolyl and phenoxy-loweralkanolyl having phenoxy substituted by loweralkoxy, loweralkyl, nitro, amino, trifluoromethyl and halo; R 4 is selected from hydrogen or loweralkyl, X is selected from hydrogen, loweralkyl, loweralkoxy, nitro, amino or halo and n is one to three; Y is loweralkyl and m is 0 to 2 inclusive and the pharmaceutically acceptable addition salts and hydrates thereof.
Claim 3
Dependent Claim 8 words
The compound of claim 1 which is 4-{[(2-phenyl)-4-quinazolinyl)amino]methyl}cyclohexanecarbonitrile.
Claim 4
Dependent Claim 8 words
The compound of claim 1 which is 1-(2-phenyl-4-quinazolinyl)-4-piperidinol.
Claim 5
Dependent Claim 8 words
The compound of claim 1 which is 1-(2-phenyl-4-quinazolinyl)-3-pyrrolidinol.
Claim 6
Dependent Claim 9 words
The compound of claim 1 which is 1-(2-phenyl-4-quinazolinyl)-3-pyrrolidinol hemihydrate.
Claim 7
Dependent Claim 8 words
The compound of claim 1 which is 4-(4-hexyl-1-piperazinyl)-2-phenylquinazoline.
Claim 8
Dependent Claim 10 words
The compound of claim 1 which is 4-(4-hexyl-1-piperazinyl)-2-phenylquinazoline dihydrochloride, dihydrate.
Claim 9
Dependent Claim 9 words
The compound of claim 1 which is 1-(2-phenyl-4-quinazolinyl)-3-piperidine methanol.
Claim 10
Dependent Claim 8 words
The compound of claim 1 which is 4-[3-(2-methoxyphenoxy)-1-pyrrolidinyl]-2-phenylquinazoline.
Claim 11
Dependent Claim 8 words
The compound of claim 1 which is 3-phenyl-4-[cis-2,5-dimethyl-4-(2-pyridinyl)-1-piperazinyl]quinazoline.
Claim 12
Dependent Claim 8 words
The compound of claim 1 which is 2-phenyl-4-[4-(2-pyridinyl)-1-piperazinyl]quinazoline.
Claim 13
Dependent Claim 8 words
The compound of claim 1 which is 1-(2-methoxyphenoxy)-3-[(2-phenyl-4-quinazolinyl)-amino]-2-propanol.
Claim 14
Dependent Claim 9 words
The compound of claim 1 which is 1-(2-methoxyphenoxy)-3-[(2-phenyl-4-quinazolinyl)amino]-2-propanol monohydrate.
Claim 15
Dependent Claim 9 words
The compound of claim 1 which is 4-(2-phenyl-4-quinazolinyl)-α-[(2-propenyloxy)methyl]-1-piperazine ethanol.
Claim 16
Dependent Claim 8 words
The compound of claim 1 which is α-[(2-methoxyphenoxy)methyl]-4-(2-phenyl-4-quinazolinyl)-1-piperazinepropanol.
Claim 17
Dependent Claim 10 words
The compound of claim 1 which is α-[(2-methoxyphenoxy)methyl]-4-(2-phenyl-4-quinazolinyl)-1-piperazinepropanol, dihydrochloride, hemihydrate.
Claim 18
Dependent Claim 9 words
The compound of claim 1 which is 2,6-dimethyl-4-(2-phenyl-4-quinazolinyl)-α-[(2-propenyloxy)-methyl]-2-piperazine ethanol.
Claim 19
Dependent Claim 10 words
The compound of claim 1 which is 2,6-dimethyl-4-(2-phenyl-4-quinazolinyl)-α-[(2-propenyloxy)methyl]-1-piperazine ethanol, hemihydrate.
Claim 20
Dependent Claim 8 words
The compound of claim 1 which is 1-(2-ethoxyphenoxy)-3-[4-(2-phenyl-4-quinazolinyl)-1-piperazinyl]-2-propanol.
Claim 21
Dependent Claim 10 words
The compound of claim 1 which is 1-(2-ethoxyphenoxy)-3-[4-(2-phenyl-4-quinazolinyl)-1-piperazinyl]-2-propanol dihydrochloride monohydrate.
Claim 22
Dependent Claim 8 words
The compound of claim 1 which is 1-(4-chloro-3-methylphenoxy)-3-[N-ethyl-N-(2-phenyl-4-quinazolinyl)-amino]-2-propanol.
Claim 23
Dependent Claim 9 words
The compound of claim 1 which is 1-(4-chloro-3-methylphenoxy)-3-[N-ethyl-N-(2-phenyl-4-quinazolinyl)-amino]-2-propanol dihydrochloride.
Claim 24
Dependent Claim 8 words
The compound of claim 1 which is 1-(3,5-dimethylphenoxy)-3-[(2-phenylquinazolin-4-yl)amino]-2-propanol.
Claim 25
Dependent Claim 8 words
The compound of claim 1 which is 1-phenoxy-3-[(2-phenyl-4-quinazolin-4-yl)amino]-2-propanol.

References Cited (Backward Citations)

US3340260A Cited
US3819628A Cited
US3997538A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-12-14 1985-06-15 1985-12-15 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-12-14 1989-06-15 1989-12-15 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-12-14 1993-06-15 1993-12-15 $7700.00 Window Closed / Lapsed

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