Patent US725630A successfully refreshed from Google Patents.
US5124319A
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Benzimidazole phosphono-amino acids
Assignee: Wyeth LLC
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Filing: 1991-10-11
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Granted: 1992-06-23
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Expires: 2011-10-11
Abstract
Abstract The compounds of the formula ##STR1## wherein R is hydrogen, lower alkyl, benzyl or pivaloyloxymethyl; R 1 and R 2 are, independently, hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonylamino, acetylamino, or halo, or when taken together R 1 and R 2 represent a methylenedioxy grouping; and the pharmacologically acceptable salts thereof are NMDA antagonists useful in the treatment and prevention of central nervous system related pathological conditions resulting from overstimulation by excitatory amino acids.
Inventors
- 👤 Reinhardt B. Baudy
- 👤 Horace Fletcher, III
- 👤 John P. Yardley
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 18:45
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/547; C07F9/645; C07F9/6503; C07F9/6506; C07F9/65068; A; A61; A61P; A61P25/00; A61P9/00; A61P9/10
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
52 words
A compound having the formula ##STR6## wherein R is hydrogen, lower alkyl, benzyl or pivaloyloxymethyl; R 1 and R 2 are, independently, hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonylamino, acetylamino, or halo, or when taken together R 1 and R 2 represent a methylenedioxy grouping; and the pharmacologically acceptable salts thereof.
Claim 2
Dependent Claim
52 words
A compound having the formula ##STR6## wherein R is hydrogen, lower alkyl, benzyl or pivaloyloxymethyl; R 1 and R 2 are, independently, hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonylamino, acetylamino, or halo, or when taken together R 1 and R 2 represent a methylenedioxy grouping; and the pharmacologically acceptable salts thereof.
Claim 3
Dependent Claim
10 words
The compound of claim 1, having the name R-α-amino-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid.
Claim 4
Dependent Claim
10 words
The compound of claim 1, having the name R-α-amino-5,6-dichloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid.
Claim 5
Dependent Claim
10 words
The compound of claim 1, having the name R-α-amino-5,6-dimethyl-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid.
Claim 6
Dependent Claim
10 words
The compound of claim 1, having the name R-α-amino-6-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid.
Claim 7
Dependent Claim
10 words
The compound of claim 1, having the name R-α-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid.
Claim 8
Independent Claim
83 words
A method for the treatment of neuropathological disorders induced by overstimulation of excitatory amino acid receptors which comprises administering to a mammal suffering from such disorders a neuroprotective amount of an NMDA antagonist of the formula: ##STR7## wherein R is hydrogen, lower alkyl, benzyl or pivaloyloxymethyl; R 1 and R 2 are, independently, hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonylamino, acetylamino, or halo, or when taken together R 1 and R 2 represent a methylenedioxy grouping; and the pharmacologically acceptable salts thereof.
Claim 9
Independent Claim
83 words
A method for the treatment of neuropathological disorders induced by overstimulation of excitatory amino acid receptors which comprises administering to a mammal suffering from such disorders a neuroprotective amount of an NMDA antagonist of the formula: ##STR7## wherein R is hydrogen, lower alkyl, benzyl or pivaloyloxymethyl; R 1 and R 2 are, independently, hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonylamino, acetylamino, or halo, or when taken together R 1 and R 2 represent a methylenedioxy grouping; and the pharmacologically acceptable salts thereof.
References Cited (Backward Citations)
SU959724A1
Cited
US4746653A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-06-23 | 1995-12-23 | 1996-06-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-06-23 | 1999-12-23 | 2000-06-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-06-23 | 2003-12-23 | 2004-06-23 | $7700.00 | Window Closed / Lapsed |