US4977155A
Expired / Lapsed
US
⏱️ 0.0 years remaining
1,2,3-triazolo compounds
Assignee: Novo Nordisk AS
•
Filing: 1989-06-22
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Granted: 1990-12-11
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Expires: 2009-06-22
Abstract
Abstract Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R 2 is hydrogen, NO 2 , NH 2 , CN, halogen, or SO 2 NH 2 ; --X--Y--Z-- is selected from --N═N--N 3 --,--NR 3 --N═N--,═N--NR 3 --N═, wherein R 3 is hydrogen, lower alkyl, or CF 3 . 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
- 👤 Jorgen Drejer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 14:02
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/02; C07D487/04; A; A61; A61P; A61P25/00; A61P43/00; C07D495/00; C07D495/02; C07D495/04; C07D513/00; C07D513/02; C07D513/04; C07D517/00; C07D517/02; C07D517/04
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
60 words
A heterocyclic compound selected from those having the formula I ##STR5## wherein R 2 is hydrogen, NO 2 , NH 2 , CN, halogen, or SO 2 NH 2 ; --X--Y--Z-- is selected from --N═N--NR 3 --, --NR 3 --N═N--, and ═N--NR 3 --N═, wherein R 3 is hydrogen, lower alkyl, or CF 3 , and a pharmaceutically-acceptable salt thereof.
Claim 2
Dependent Claim
60 words
A heterocyclic compound selected from those having the formula I ##STR5## wherein R 2 is hydrogen, NO 2 , NH 2 , CN, halogen, or SO 2 NH 2 ; --X--Y--Z-- is selected from --N═N--NR 3 --, --NR 3 --N═N--, and ═N--NR 3 --N═, wherein R 3 is hydrogen, lower alkyl, or CF 3 , and a pharmaceutically-acceptable salt thereof.
Claim 3
Dependent Claim
10 words
A compound according to claim 1 which is 7,8 dihydroxy-1-methyl-4-nitro-1H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 4
Dependent Claim
9 words
A compound according to claim 1 which is 7,8-dihydroxy-3-methyl-4-nitro-3H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 5
Dependent Claim
9 words
A compound according to claim 1 which is 4-amino-7,8-dihydroxy-3-methyl-3H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 6
Dependent Claim
9 words
A compound according to claim 1 which is 4-cyano-7,8-dihydroxy-3-methyl-3H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 7
Dependent Claim
20 words
A pharmaceutical composition comprising as active glutamate-antagonistic component a heterocyclic compound according to claim 1 and a pharmaceutically acceptable carrier.
Claim 8
Dependent Claim
23 words
A pharmaceutical composition according to claim 6 in the form of an oral dosage unit containing about 10-200 mg of the active compound.
Claim 9
Dependent Claim
37 words
A method of treating hyperactivity of the excitatory neurotransmitters, in a subject in need thereof, which comprises the step of administering to the said subject a neurologically-effective, glutamate antagonistic, amount of a heterocyclic compound of claim 1.
Claim 10
Dependent Claim
9 words
A compound according to claim 1 which is 7,8-dihydroxy-1H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 11
Dependent Claim
9 words
A compound according to claim 1 which is 7,8-dihydroxy-4-nitro-1H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 12
Dependent Claim
9 words
A compound according to claim 1 which is 4-amino-7,8-dihydroxy-1H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 13
Dependent Claim
9 words
A compound according to claim l which is 4-cyano-7,8-dihydroxy-1H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 14
Dependent Claim
9 words
A compound according to claim 1 which is 7,8-dihydroxy-1-methyl-1H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 15
Dependent Claim
9 words
A compound according to claim 1 which is 4-amino-7,8-dihydroxy-1-methyl-1H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 16
Dependent Claim
9 words
A compound according to claim 1 which is 7,8-dihydroxy-2-methyl-2H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 17
Dependent Claim
9 words
A compound according to claim 1 which is 7,8-dihydroxy-2-methyl-4-nitro-2H-1,2,3-triazolo[4,5-f]quinoxaline.
Claim 18
Dependent Claim
9 words
A compound according to claim 1 which is 7,8-dihydroxy-3-methyl-3H-1,2,3-triazolo[4,5-f]quinoxaline.
References Cited (Backward Citations)
US4912108A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-12-10 | 1994-06-11 | 1994-12-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-12-10 | 1998-06-11 | 1998-12-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-12-10 | 2002-06-11 | 2002-12-11 | $7700.00 | Window Closed / Lapsed |