US4432981A
Expired / Lapsed
US
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2-(Pyridinyl or hydroxyphenyl)-8-substituted pyrido[2,3-d]pyrimidin-5(8H)-ones
Assignee: STWB Inc
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Filing: 1982-11-05
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Granted: 1984-02-21
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Expires: 2002-11-05
Abstract
Abstract 2-Q-6-Q'-8-R-pyrido[2,3-d]pyrimidin-5(8H)-ones (I), where Q is 4(or 3)-hydroxyphenyl, 4(or 3)-methoxyphenyl, 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower-alkyl substituents, R' is hydrogen or alkyl having one to four carbon atoms, Q is hydrogen, amino or nitro, and R is alkyl having from one to four carbon atoms, CH(C 2 H 5 ) 2 , (CH 2 ) n ═CHCH 2 where n is 1 or 2, or Y-Z where Y is alkylene having from two to four carbon atoms and having its connecting linkages on different carbon atoms and Z is hydroxy, OR 1 or NR 1 R 2 where R 1 and R 2 are each methyl or ethyl, or acid-addition salts thereof, and their preparation are shown. Also shown is the cardiotonic use of I where Q is 4(or 3)-hydroxyphenyl, 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower-alkyl substituents and Q' is hydrogen or amino.
Inventors
- 👤 George Y. Lesher
- 👤 Baldev Singh
- 👤 Stanley C. Laskowski
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 22:19
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/32; C07D239/42; A; A61; A61P; A61P9/00; A61P9/04; C07D319/00; C07D319/04; C07D319/06; C07D407/00; C07D407/02; C07D407/12; C07D407/14; C07D471/00; C07D471/02; C07D471/04
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
119 words
2-Q-4-R'-6-Q'-8-R-pyrido[2,3-d]pyrimidin-5(8H)-one having the formula ##STR4## or acid-addition salt thereof, where Q is 4(or 3)-hydroxyphenyl, 4(or 3)-methoxyphenyl, 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower-alkyl substituents, R' is hydrogen or alkyl having from one to four carbon atoms, Q' is hydrogen, nitro or amino, and R is alkyl having from one to four carbon atoms, CH(C 2 H 5 ) 2 , (CH 2 ) n CH═CH 2 where n is 1 or 2, or Y--Z where Y is alkylene having from two to four carbon atoms and having its connecting linkages on different carbon atoms and Z is hydroxy, OR 1 and NR 1 R 2 where R 1 and R 2 are each methyl or ethyl.
Claim 2
Dependent Claim
119 words
2-Q-4-R'-6-Q'-8-R-pyrido[2,3-d]pyrimidin-5(8H)-one having the formula ##STR4## or acid-addition salt thereof, where Q is 4(or 3)-hydroxyphenyl, 4(or 3)-methoxyphenyl, 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower-alkyl substituents, R' is hydrogen or alkyl having from one to four carbon atoms, Q' is hydrogen, nitro or amino, and R is alkyl having from one to four carbon atoms, CH(C 2 H 5 ) 2 , (CH 2 ) n CH═CH 2 where n is 1 or 2, or Y--Z where Y is alkylene having from two to four carbon atoms and having its connecting linkages on different carbon atoms and Z is hydroxy, OR 1 and NR 1 R 2 where R 1 and R 2 are each methyl or ethyl.
Claim 3
Dependent Claim
31 words
A compound according to claim 1 where Q' is hydrogen or amino, R' is hydrogen or methyl, Q is 4(or 3)-pyridinyl and R is ethyl, n-propyl, n-butyl, allyl, 3-butenyl and 1-ethylpropyl.
Claim 4
Dependent Claim
9 words
8-Ethyl-2-(4-pyridinyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 5
Dependent Claim
9 words
8-Ethyl-2-(3-pyridinyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 6
Dependent Claim
9 words
8-Ethyl-2-(4-hydroxyphenyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 7
Dependent Claim
9 words
8-n-Propyl-2-(4-pyridinyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 8
Dependent Claim
9 words
8-n-Butyl-2-(4-pyridinyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 9
Dependent Claim
9 words
8-n-Butyl-2-(3-pyridinyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 10
Dependent Claim
9 words
6-Amino-8-n-butyl-2-(4-pyridinyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 11
Dependent Claim
9 words
8-(1-Ethylpropyl)-2-(4-pyridinyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 12
Dependent Claim
9 words
8-(3-Butenyl)-2-(4-pyridinyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 13
Dependent Claim
9 words
8-Isopropyl-2-(4-pyridinyl)pyrido[2,3-d]pyrimidin-5(8H)-one according to claim 1 or acid-addition salt thereof.
Claim 14
Dependent Claim
145 words
A cardiotonic composition for increasing cardiac contractility, said composition comprising a pharmaceutically acceptable carrier and, as the active component thereof, a cardiotonically effective amount of the compound having the formula ##STR5## where R' is hydrogen or alkyl having from one to four carbon atoms, and R is alkyl having from one to four carbon atoms, CH(C 2 H 5 ) 2 , (CH 2 ) n CH═CH 2 where n is 1 or 2, or Y-Z where Y is alkylene having from two to four carbon atoms and having its connecting linkages on different carbon atoms and Z is hydroxy, OR, or NR 1 R 2 where R 1 and R 2 are each methyl or ethyl, Q' is amino or hydrogen and Q is 4(or 3)-hydroxyphenyl, 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower alkyl substituents, or pharmaceutically acceptable acid-addition salt thereof.
Claim 15
Dependent Claim
145 words
A cardiotonic composition for increasing cardiac contractility, said composition comprising a pharmaceutically acceptable carrier and, as the active component thereof, a cardiotonically effective amount of the compound having the formula ##STR5## where R' is hydrogen or alkyl having from one to four carbon atoms, and R is alkyl having from one to four carbon atoms, CH(C 2 H 5 ) 2 , (CH 2 ) n CH═CH 2 where n is 1 or 2, or Y-Z where Y is alkylene having from two to four carbon atoms and having its connecting linkages on different carbon atoms and Z is hydroxy, OR, or NR 1 R 2 where R 1 and R 2 are each methyl or ethyl, Q' is amino or hydrogen and Q is 4(or 3)-hydroxyphenyl, 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower alkyl substituents, or pharmaceutically acceptable acid-addition salt thereof.
Claim 16
Dependent Claim
38 words
A composition according to claim 13 where the active component is the compound where Q is 4(or 3)-pyridinyl, R' is hydrogen or methyl, Q' is hydrogen or amino, and R is ethyl, n-propyl, n-butyl, allyl, 3-butenyl and 1-ethylpropyl.
Claim 17
Dependent Claim
34 words
The method for increasing cardiac contractility in a patient requiring such treatment which comprises administering orally or parenterally in a solid or liquid dosage form to such patient a composition according to claim 13.
Claim 18
Dependent Claim
34 words
The method for increasing cardiac contractility in a patient requiring such treatment which comprises administering orally or parenterally in a solid or liquid dosage form to such patient a composition according to claim 14.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1987-02-20 | 1987-08-22 | 1988-02-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-02-20 | 1991-08-22 | 1992-02-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-02-20 | 1995-08-22 | 1996-02-21 | $7700.00 | Window Closed / Lapsed |