US4123533A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Fused pyrimidine derivatives and compositions for treating atherosclerosis containing them
Assignee: Chinoin Private Co Ltd
•
Filing: 1977-02-04
•
Granted: 1978-10-31
•
Expires: 1997-02-04
Abstract
Abstract Compounds of the formula: <IMAGE> or pharmaceutically acceptable salts thereof are disclosed wherein R is hydrogen or C1 to C6 alkyl; R2 and R3 are each hydrogen or together form a valency bond; R6 is carboxy or C1 to C6 alkoxycarbonyl; R7 and R8 are each hydrogen or together form a valency bond; R10 is carboxy or C1 to C6 alkoxycarbonyl and the dotted line represents two hydrogen atoms or a valency bond. The compounds are useful in the treatment of atherosclerosis.
Inventors
- 👤 Istvan Hermecz
- 👤 Zoltan Meszaros
- 👤 Sandor Virag
- 👤 Lelle Vasvari nee Debreczy
- 👤 Agnes Horvath
- 👤 Jozsef Knoll
- 👤 Gyula Sebestyen
- 👤 Agoston David
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 15:30
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/02; C07D471/04; A; A61; A61P; A61P25/00; A61P25/28; A61P3/00; A61P3/06; A61P9/00; A61P9/10
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
85 words
A compound of the formula: ##STR10## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or C 1 to C 6 alkyl; R 2 and R 3 are each hydrogen or together form a valency bond; R 6 is carboxy or C 1 to C 6 alkoxycarbonyl; R 7 and R 8 are each hydrogen or together form a valency bond; R 10 is carboxy or C 1 to C 6 alkoxycarbonyl and the dotted line represents two hydrogen atoms or a valency bond.
Claim 2
Dependent Claim
85 words
A compound of the formula: ##STR10## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or C 1 to C 6 alkyl; R 2 and R 3 are each hydrogen or together form a valency bond; R 6 is carboxy or C 1 to C 6 alkoxycarbonyl; R 7 and R 8 are each hydrogen or together form a valency bond; R 10 is carboxy or C 1 to C 6 alkoxycarbonyl and the dotted line represents two hydrogen atoms or a valency bond.
Claim 3
Dependent Claim
7 words
(±) 3-alkoxycarbonyl-6-methyl-9-(carboxymethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine, as defined in claim 1.
Claim 4
Dependent Claim
7 words
(-) 3-alkoxycarbonyl-6-methyl-9-(carboxymethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 5
Dependent Claim
7 words
(+) 3-alkoxycarbonyl-6-methyl-9-(carboxymethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 6
Dependent Claim
7 words
(±) 3-ethoxycarbonyl-6-methyl-9-(carboxymethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 7
Dependent Claim
7 words
(-) 3-ethoxycarbonyl-6-methyl-9-(carboxymethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 8
Dependent Claim
7 words
(+) 3-ethoxycarbonyl-6-methyl-9-(carboxymethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 9
Dependent Claim
7 words
(±) 3-alkoxycarbonyl-6-methyl-9-(alkoxycarbonylmethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 10
Dependent Claim
7 words
(-) 3-alkoxycarbonyl-6-methyl-9-(alkoxycarbonylmethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 11
Dependent Claim
7 words
(+) 3-alkoxycarbonyl-6-methyl-9-(alkoxycarbonylmethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 12
Dependent Claim
7 words
(±) 3-ethoxycarbonyl-6-methyl-9-(ethoxycarbonylmethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 13
Dependent Claim
7 words
(-) 3-ethoxycarbonyl-6-methyl-9-(ethoxycarbonylmethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 14
Dependent Claim
7 words
(+) 3-ethoxycarbonyl-6-methyl-9-(ethoxycarbonylmethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 15
Dependent Claim
6 words
3-ethoxycarbonyl-9-(ethoxycarbonyl-methylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine, as defined in claim 1.
Claim 16
Dependent Claim
6 words
3-ethoxycarbonyl-7-methyl-9-(ethoxycarbonylmethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)-pyrimidine, as defined in claim 1.
Claim 17
Dependent Claim
8 words
(±) 3-alkoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine-9-acetic acid, as defined in claim 1.
Claim 18
Dependent Claim
8 words
(-) 3-alkoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine-9-acetic acid, as defined in claim 1.
Claim 19
Dependent Claim
8 words
(+) 3-alkoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine-9-acetic acid, as defined in claim 1.
Claim 20
Dependent Claim
8 words
(±) 3-ethoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine-9-acetic acid, as defined in claim 1.
Claim 21
Dependent Claim
8 words
(-) 3-ethoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimdine-9-acetic acid, as defined in claim 1.
Claim 22
Dependent Claim
8 words
(+) 3-ethoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine-9-acetic acid, as defined in claim 1.
Claim 23
Dependent Claim
7 words
3-ethoxycarbonyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine-9-acetic acid, as defined in claim 1.
Claim 24
Dependent Claim
7 words
3-ethoxycarbonyl-7-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine-9-acetic acid, as defined in claim 1.
Claim 25
Dependent Claim
8 words
3-alkoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine-9-acetic acid alkylester, as defined in claim 1.
Claim 26
Dependent Claim
9 words
3-ethoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido(1,2a)pyrimidine-9-acetic acid ethyl ester, as defined in claim 1.
Claim 27
Dependent Claim
6 words
3-ethoxycarbonyl-7-methyl-9(carboxy-methylene)-4-oxo-6,7,8,9tetrahydro-4H-pyrido(1,2a)pyrimidine as defined in claim 1.
Claim 28
Dependent Claim
100 words
A pharmaceutical composition for treating atherosclerosis consisting essentially of a compound of the formula: ##STR11## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or C 1 to C 6 alkyl; R 2 and R 3 are hydrogen or together form a valency bond; R 6 is carboxy or C 1 to C 6 alkoxycarbonyl; R 7 and R 8 are each hydrogen or together form a valency bond; R 10 is carboxy or C 1 to C 6 alkoxycarbonyl; and the dotted line represents two hydrogen atoms or a valency bond, in combination with a pharmaceutically acceptable carrier.
Claim 29
Dependent Claim
100 words
A pharmaceutical composition for treating atherosclerosis consisting essentially of a compound of the formula: ##STR11## or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or C 1 to C 6 alkyl; R 2 and R 3 are hydrogen or together form a valency bond; R 6 is carboxy or C 1 to C 6 alkoxycarbonyl; R 7 and R 8 are each hydrogen or together form a valency bond; R 10 is carboxy or C 1 to C 6 alkoxycarbonyl; and the dotted line represents two hydrogen atoms or a valency bond, in combination with a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
US3696197A
Cited
US3898224A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-10-30 | 1982-05-01 | 1982-10-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-10-30 | 1986-05-01 | 1986-10-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-10-30 | 1990-05-01 | 1990-10-31 | $7700.00 | Window Closed / Lapsed |