US4912108A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Pyridoquinoxaline compounds and their preparation and use as glutamate antagonists
Assignee: Novo Nordisk AS
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Filing: 1989-05-03
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Granted: 1990-03-27
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Expires: 2009-05-03
Abstract
Abstract Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein --A-- together with the two carbon atoms denoted as 1 and 2 is selected from ##STR2## R 1 , R 2 and R 3 are independently H, halogen, CN, NH 2 , NO 2 , SO 3 H, SO 2 NH 2 , or CONH 2 The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use. The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.
Inventors
- 👤 Poul Jacobsen
- 👤 Flemming E. Nielsen
- 👤 Tage Honore
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 11:46
CPC Classifications
C; C07; C07D; C07D241/00; C07D241/36; C07D241/38; C07D241/40; C07D241/44; C07D471/00; C07D471/02; C07D471/04
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
55 words
A heterocyclic compound having the formula I ##STR20## wherein -A- together with the two carbon atoms denoted as 1 and 2 is ##STR21## wherein R 1 , R 2 and R 3 are independently H, halogen, CN, NH 2 , NO 2 , SO 3 H, SO 2 NH 2 , or CONH 2 .
Claim 2
Dependent Claim
55 words
A heterocyclic compound having the formula I ##STR20## wherein -A- together with the two carbon atoms denoted as 1 and 2 is ##STR21## wherein R 1 , R 2 and R 3 are independently H, halogen, CN, NH 2 , NO 2 , SO 3 H, SO 2 NH 2 , or CONH 2 .
Claim 3
Dependent Claim
77 words
A pharmaceutical composition comprising as active glutamate antagonistic component an effective amount of a heterocyclic compound having the formula I ##STR22## wherein -A- together with the two carbon atoms denoted as 1 and 2 is ##STR23## wherein R 1 , R 2 and R 3 are independently H, halogen, CN, NH 2 , NO 2 , SO 3 H, SO 2 NH 2 , or CONH 2 , or a pharmaceutically-acceptable salt thereof, and a pharmaceutically-acceptable carrier.
Claim 4
Dependent Claim
77 words
A pharmaceutical composition comprising as active glutamate antagonistic component an effective amount of a heterocyclic compound having the formula I ##STR22## wherein -A- together with the two carbon atoms denoted as 1 and 2 is ##STR23## wherein R 1 , R 2 and R 3 are independently H, halogen, CN, NH 2 , NO 2 , SO 3 H, SO 2 NH 2 , or CONH 2 , or a pharmaceutically-acceptable salt thereof, and a pharmaceutically-acceptable carrier.
Claim 5
Independent Claim
92 words
A method of treating hyperactivity of the excitatory neurotransmitters, in a subject in need thereof, which comprises the the step of administering to the said subject a neurologically-effective, glutamate antagonistic, amount of a heterocyclic compound having the formula I ##STR24## wherein -A- together with the two carbon atoms denoted as 1 and 2 is ##STR25## wherein R 1 , R 2 and R 3 are independently H, halogen, CN, NH 2 , NO 2 , SO 3 H, SO 2 NH 2 , or CONH 2 , or a pharmaceutically-acceptable salt thereof.
Claim 6
Independent Claim
92 words
A method of treating hyperactivity of the excitatory neurotransmitters, in a subject in need thereof, which comprises the the step of administering to the said subject a neurologically-effective, glutamate antagonistic, amount of a heterocyclic compound having the formula I ##STR24## wherein -A- together with the two carbon atoms denoted as 1 and 2 is ##STR25## wherein R 1 , R 2 and R 3 are independently H, halogen, CN, NH 2 , NO 2 , SO 3 H, SO 2 NH 2 , or CONH 2 , or a pharmaceutically-acceptable salt thereof.
Claim 7
Dependent Claim
30 words
The method of claim 3 wherein the compound is administered in the form of a pharmaceutical composition thereof, in which it is present together with a pharmaceutically-acceptable carrier or diluent.
Claim 8
Dependent Claim
11 words
A compound according to claim 1 which is 2,3-dihydroxy-6-nitropyrido (2,3-f) quinoxaline.
Claim 9
Dependent Claim
11 words
A pharmaceutical composition of claim 2 wherein the compound is 2,3dihydroxy-6-nitropyrido(2,3-f)quinoxaline.
Claim 10
Dependent Claim
23 words
A pharmaceutical composition according to claim 2 in the form of an oral dosage unit containing about 10-200 mg of the active compound.
Claim 11
Dependent Claim
10 words
A method of claim 3 wherein the compound is 2,3-dihydroxy-6-nitropyrido(2,3-f)quinoxaline.
References Cited (Backward Citations)
US3431111A
Cited
US4764518A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-03-26 | 1993-09-25 | 1994-03-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-03-26 | 1997-09-25 | 1998-03-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-03-26 | 2001-09-25 | 2002-03-27 | $7700.00 | Window Closed / Lapsed |