US4377580A
Expired / Lapsed
US
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Tricyclic quinazoline derivatives
Assignee: Astellas Pharma Inc
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Filing: 1980-11-25
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Granted: 1983-03-22
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Expires: 2000-11-25
Abstract
Abstract Quinazoline derivatives of the formulae: <IMAGE> wherein A1 is <IMAGE> A2 is <IMAGE> R1 is hydrogen, carboxy or esterified carboxy, Ra1 and Rb1 are esterified carboxy, R2 and R3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy, R4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylamino Ra4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino, R5 is alkyl or alkenyl, and R6 is carboxy or esterified carboxy.
Inventors
- 👤 Ikuo Ueda
- 👤 Masayuki Kato
- 👤 Masanobu Nagano
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 10:30
CPC Classifications
C; C07; C07D; C07D265/00; C07D265/04; C07D265/12; C07D265/14; C07D265/24; C07D265/26; A; A61; A61P; A61P37/00; A61P37/08; C07D239/00; C07D239/70; C07D239/72; C07D239/86; C07D239/94; C07D239/95; C07D239/96; C07D487/00; C07D487/02; C07D487/04
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
157 words
A pyrimidoquinazoline compound of the formula: ##STR35## wherein A 2 is a group of the formula: ##STR36## R 1 is hydrogen, carboxy or C 2 -C 7 alkoxycarbonyl, R 2 and R 3 are hydrogen, C 1 -C 6 alkyl, halogen, nitro amino, C 1 -C 6 alkoxy, phenyloxy, C 1 -C 6 alkylthio, C 1 -C 6 alkylpiperazinyl, C 1 -C 18 alkanoylamino, di(C 1 -C 6 )alkanoylamino, C 3 -C 9 alkoxalylamino, C 4 -C 8 cycloalkanecarbonylamino, C 3 -C 7 cycloalkyl(C 1 -C 6 )alkanoylamino, benzamido, phenyl(C 1 -C 6 )alkanoylamino, C 1 -C 6 alkanesulfonylamino or di(C 1 -C 6 )alkylamino which may be substituted with hydroxy, R 4 is hydrogen, C 1 -C 6 alkyl, hydroxy, C 1 -C 6 alkoxy, C 2 -C 6 alkenyloxy or di(C 1 -C 6 )alkylamino, and R 5 is C 1 -C 6 alkyl or C 2 -C 6 alkenyl, or pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
157 words
A pyrimidoquinazoline compound of the formula: ##STR35## wherein A 2 is a group of the formula: ##STR36## R 1 is hydrogen, carboxy or C 2 -C 7 alkoxycarbonyl, R 2 and R 3 are hydrogen, C 1 -C 6 alkyl, halogen, nitro amino, C 1 -C 6 alkoxy, phenyloxy, C 1 -C 6 alkylthio, C 1 -C 6 alkylpiperazinyl, C 1 -C 18 alkanoylamino, di(C 1 -C 6 )alkanoylamino, C 3 -C 9 alkoxalylamino, C 4 -C 8 cycloalkanecarbonylamino, C 3 -C 7 cycloalkyl(C 1 -C 6 )alkanoylamino, benzamido, phenyl(C 1 -C 6 )alkanoylamino, C 1 -C 6 alkanesulfonylamino or di(C 1 -C 6 )alkylamino which may be substituted with hydroxy, R 4 is hydrogen, C 1 -C 6 alkyl, hydroxy, C 1 -C 6 alkoxy, C 2 -C 6 alkenyloxy or di(C 1 -C 6 )alkylamino, and R 5 is C 1 -C 6 alkyl or C 2 -C 6 alkenyl, or pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
14 words
A compound according to claim 1, which is a compound of the formula: ##STR37##
Claim 4
Dependent Claim
10 words
A compound according to claim 2, which is methyl 4-oxo-10-pivalamido-4H-pyrimido[1,2-c]quinazoline-3-carboxylate.
Claim 5
Dependent Claim
15 words
A compound according to claim 2, which is 4-oxo-10-pivalamido-4H-pyrimido[1,2-c]quinazoline-3-carboxylic acid or pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
15 words
A compound according to claim 2, which is 4-oxo-10-(3,3-dimethylbutyramido)-4H-pyrimido[1,2-c]quinazoline-3-carboxylic acid or pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
15 words
A compound according to claim 2, which is 4-oxo-10-(2-methylpropionamido)-4H-pyrimido[1,2-c]quinazoline-3-carboxylic acid or pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim
15 words
A compound according to claim 2, which is 4-oxo-10-(2-ethylbutyramido)-4H-pyrimido[1,2-c]quinazoline-3-carboxylic acid or pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
15 words
A compound according to claim 2, which is 4-oxo-10-(2,3-dimethylpentanamido)-4H-pyrimido[1,2-c]quinazoline-3-carboxylic acid or pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
14 words
A compound according to claim 1, which is a compound of the formula: ##STR38##
Claim 11
Dependent Claim
24 words
An anti-allergic pharmaceutical composition comprising a effective amount of the compound of claim 1 in association with a non-toxic, pharmaceutically acceptable carrier or excipient.
References Cited (Backward Citations)
GB1086666A
Cited
US3594379A
Cited
GB1349136A
Cited
US3891638A
Cited
US4167569A
Cited
US4105766A
Cited
US4192944A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1986-03-21 | 1986-09-20 | 1987-03-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-03-21 | 1990-09-20 | 1991-03-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-03-21 | 1994-09-20 | 1995-03-22 | $7700.00 | Window Closed / Lapsed |