Patent US4889855A successfully refreshed from Google Patents.
US4889855A
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Heterocyclic compounds and their preparation and use
Assignee: Novo Nordisk AS
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Filing: 1988-02-16
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Granted: 1989-12-26
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Expires: 2008-02-16
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 06:02
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: 16
Claim 1
Independent Claim
94 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 ##STR21## wherein --A-- together with the two carbon atoms denoted as 1 and 2 is selected from ##STR22## 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 2
Independent Claim
94 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 ##STR21## wherein --A-- together with the two carbon atoms denoted as 1 and 2 is selected from ##STR22## 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 3
Dependent Claim
9 words
A method according to claim 1 which is 2,3-dihydroxy-6,7-dinitrobenzo(f)quinoxaline.
Claim 4
Dependent Claim
9 words
A method according to claim 1 which is 2,3-dihydroxy-6,10-dinitrobenzo(f)quinoxaline.
Claim 5
Dependent Claim
9 words
A method according to claim 1 which is 6-bromo-2,3-dihydroxy-10-nitrobenzo(f)quinoxaline.
Claim 6
Dependent Claim
24 words
A heterocyclic compound selected from the group consisting of: 7-bromo-2,3-dihydroxybenzo(f)quinoxaline 6-bromo-2,3-dihydroxybenzo(f)quinoxaline 6-amino-2,3-dihydroxybenzo(f)quinoxaline 6-cyano-2,3-dihydroxybenzo(f)quinoxaline 10-amino-2,3-dihydroxybenzo(f)quinoxaline 10-cyano-2,3-dihydroxybenzo(f)quinoxaline 6-amino-7,8,9,10-tetrahydro-2,3-dihydroxybenzo(f)quinoxaline 6-cyano-7,8,9,10-tetrahydro-2,3-dihydroxybenzo(f)quinoxaline 7,8,9,10-tetrahydro-2,3-dihydroxy-5,6-dinitrobenzo(f)quinoxaline 5-carbamoyl-7,8,9,10-tetrahydro-2,3-dihydroxybenzo(f)quinoxaline 2,3-dihydroxy-7-cyano-benzo(f)quinoxaline 2,3-dihydroxy-7-sulphamoyl-benzo(f)quinoxaline 2,3-dihydroxy-6-nitro-7-sulphamoyl-benzo(f)quinoxaline and 6-amino-2,3-dihydroxy-7-sulphamoyl-benzo(f)quinoxaline.
Claim 7
Dependent Claim
24 words
A heterocyclic compound selected from the group consisting of: 7-bromo-2,3-dihydroxybenzo(f)quinoxaline 6-bromo-2,3-dihydroxybenzo(f)quinoxaline 6-amino-2,3-dihydroxybenzo(f)quinoxaline 6-cyano-2,3-dihydroxybenzo(f)quinoxaline 10-amino-2,3-dihydroxybenzo(f)quinoxaline 10-cyano-2,3-dihydroxybenzo(f)quinoxaline 6-amino-7,8,9,10-tetrahydro-2,3-dihydroxybenzo(f)quinoxaline 6-cyano-7,8,9,10-tetrahydro-2,3-dihydroxybenzo(f)quinoxaline 7,8,9,10-tetrahydro-2,3-dihydroxy-5,6-dinitrobenzo(f)quinoxaline 5-carbamoyl-7,8,9,10-tetrahydro-2,3-dihydroxybenzo(f)quinoxaline 2,3-dihydroxy-7-cyano-benzo(f)quinoxaline 2,3-dihydroxy-7-sulphamoyl-benzo(f)quinoxaline 2,3-dihydroxy-6-nitro-7-sulphamoyl-benzo(f)quinoxaline and 6-amino-2,3-dihydroxy-7-sulphamoyl-benzo(f)quinoxaline.
Claim 8
Dependent Claim
89 words
A pharmaceutical composition comprising as active glutamate antagonistic component an effective amount of a heterocyclic compound having the formula I ##STR23## wherein --A-- together with the two carbon atoms denoted as 1 and 2 is selected from ##STR24## 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 solid, sugar, suspending agent, emulsifier, or alcohol pharmaceutically-acceptable carrier or auxiliary agent.
Claim 9
Dependent Claim
89 words
A pharmaceutical composition comprising as active glutamate antagonistic component an effective amount of a heterocyclic compound having the formula I ##STR23## wherein --A-- together with the two carbon atoms denoted as 1 and 2 is selected from ##STR24## 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 solid, sugar, suspending agent, emulsifier, or alcohol pharmaceutically-acceptable carrier or auxiliary agent.
Claim 10
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 11
Dependent Claim
13 words
A heterocyclic compound selected from the group consisting of: 2,3-dihydroxy-6,7-dinitrobenzo(f)quinoxaline, 2,3-dihydroxy-6,10-dinitrobenzo(f)quinoxaline, and 6-bromo-2,3-dihydroxy-10-nitrobenzo(f)quinoxaline.
Claim 12
Dependent Claim
13 words
A heterocyclic compound selected from the group consisting of: 2,3-dihydroxy-6,7-dinitrobenzo(f)quinoxaline, 2,3-dihydroxy-6,10-dinitrobenzo(f)quinoxaline, and 6-bromo-2,3-dihydroxy-10-nitrobenzo(f)quinoxaline.
Claim 13
Dependent Claim
12 words
A pharmaceutical composition of claim 6 wherein the heterocyclic compound is 6-bromo-2,3-dihydroxy-10-nitrobenzo(f)quinoxaline.
Claim 14
Dependent Claim
30 words
The method of claim 1 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 15
Dependent Claim
12 words
A pharmaceutical composition of claim 6 wherein the heterocyclic compound is 2,3-dihydroxy-6,7-dinitrobenzo(f)quinoxaline.
Claim 16
Dependent Claim
12 words
A pharmaceutical composition of claim 6 wherein the heterocyclic compound is 2,3-dihydroxy-6,10-dinitrobenzo(f)quinoxaline.
References Cited (Backward Citations)
US3431111A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-12-25 | 1993-06-26 | 1993-12-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-12-25 | 1997-06-26 | 1997-12-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-12-25 | 2001-06-26 | 2001-12-26 | $7700.00 | Window Closed / Lapsed |