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US4761405A
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Antagonists of specific excitatory amino acid neurotransmitter receptors having increased potency
Assignee: Eisai Corp of North America
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Filing: 1987-03-04
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Granted: 1988-08-02
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Expires: 2007-03-04
Abstract
Abstract The invention pertains to novel, potent anticonvulsants, analgesics, cognition enhancers and neuroprotectants achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to ω-[2-(phosphonoalkylenyl)-cycloalkyl]-2-aminoalkanoic acids having general formula: ##STR1## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C 1 to C 6 ), alkyl (C 7 to C 12 ), fatty acid chain (C 13 to C 24 ), aryl, aralkyl, hydroxyl; the stereoisomers being in their resolved or racemic form; n and m=0,1,2 or 3; z=0,1 or 2; the cycloalkyl ring being replaced with the cycloalkenyl ring; and the pharmaceutically acceptable salts and derivatives thereof.
Inventors
- 👤 Waclaw J. Rzeszotarski
- 👤 Donald J. Kyle
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 20:35
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/383; C07F9/40; C07F9/4003; C07F9/4018
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
96 words
A potent selective excitatory amino acid neurotransmitter receptor antagonist having the general formula: ##STR4## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C 1 to C 6 ), alkyl (C 7 to C 12 ), fatty acid chain (C 13 to C 24 ), aryl, aralkyl, hydroxyl, the stereoisomers being in their resolved or racemic form; n and m=1, 2, or 3 and z=0, 1 or 2; the cycloalkyl ring being replaced with the cycloalkenyl ring; and the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
96 words
A potent selective excitatory amino acid neurotransmitter receptor antagonist having the general formula: ##STR4## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C 1 to C 6 ), alkyl (C 7 to C 12 ), fatty acid chain (C 13 to C 24 ), aryl, aralkyl, hydroxyl, the stereoisomers being in their resolved or racemic form; n and m=1, 2, or 3 and z=0, 1 or 2; the cycloalkyl ring being replaced with the cycloalkenyl ring; and the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
26 words
The potent selective excitatory amino acid neurotransmitter receptor antagonist of claim 1 where R 1 and R 2 are both hydrogen and n=1, m=2 and z=1.
Claim 4
Dependent Claim
10 words
The compound according to claim 1 that is 3-{2-phosphonoethylcyclohexyl}-2-aminopropanoic acid.
Claim 5
Dependent Claim
10 words
The compound according to claim 1 that is 4-[2-phosphonomethylcyclohexyl]-2-aminobutanoic acid.
Claim 6
Dependent Claim
28 words
A pharmaceutical composition for relieving pain which comprises a pain relieving effective amount of one or more compounds of claim 1 with a pharmaceutically acceptable carrier and/or diluent.
Claim 7
Dependent Claim
35 words
A process of relieving pain in an animal in need thereof which comprises administering said compound of claim 1 or 5 parenterally, nasally, orally, rectally or a combination thereof to said animal in need thereof.
Claim 8
Dependent Claim
29 words
A pharmaceutical composition for treatment of convulsions or epilepsy which comprises an effective amount of one or more compounds of claim 1 with a pharmaceutically acceptable carrier and/or diluent.
Claim 9
Dependent Claim
31 words
A process for treating convulsions or epilepsy which comprises administering said compound of claim 1 or 7 parenterally, orally, nasally, rectally or a combination thereof to said animal in need thereof.
Claim 10
Dependent Claim
27 words
A pharmaceutical composition of enhancing cognition which comprises a cognition enhancing amount of one or more compounds of claim 1 with a pharmaceutically acceptable carrier and/or diluent.
Claim 11
Dependent Claim
29 words
A process of enhancing cognition which comprises administering said compound of claim 1 or 9 parenterally, orally, nasally, rectally or a combination thereof to said animal in need thereof.
Claim 12
Dependent Claim
88 words
A potent, selective excitatory amino acid neurotransmitter receptor antagonist having the general formula: ##STR5## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C 1 to C 6 ), alkyl (C 7 to C 12 ), fatty acid chain (C 13 to C 24 ), aryl, aralkyl and hydroxyl; the stereoisomers being in their resolved or racemic form; n=1 and m=0, 1, 2 or 3; z=0, 1 or 2; and the pharmaceutically acceptable salts thereof.
Claim 13
Dependent Claim
88 words
A potent, selective excitatory amino acid neurotransmitter receptor antagonist having the general formula: ##STR5## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C 1 to C 6 ), alkyl (C 7 to C 12 ), fatty acid chain (C 13 to C 24 ), aryl, aralkyl and hydroxyl; the stereoisomers being in their resolved or racemic form; n=1 and m=0, 1, 2 or 3; z=0, 1 or 2; and the pharmaceutically acceptable salts thereof.
Claim 14
Dependent Claim
29 words
The potent, selective excitatory amino acid neurotransmitter receptor antagonist of claim 11 wherein m=1, 2 or 3 and the sum of n+m is a number from 2 to 5.
Claim 15
Dependent Claim
19 words
The potent, selective excitatory amino acid neurotransmitter receptor antagonist of claim 12 wherein the sum of n+m is 3.
Claim 16
Dependent Claim
89 words
A potent, selective excitatory amino acid neurotransmitter receptor antagonist having the general formula: ##STR6## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C 1 to C 6 ), alkyl (C 7 to C 12 ), fatty acid chain (C 13 to C 24 ), aryl, aralkyl, hydroxyl; the stereoisomers being in their resolved or racemic form; z=0, 1 or 2; the cycloalkyl ring being replaced with the cycloalkenyl ring; and the pharmaceutically acceptable salts thereof.
Claim 17
Dependent Claim
89 words
A potent, selective excitatory amino acid neurotransmitter receptor antagonist having the general formula: ##STR6## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C 1 to C 6 ), alkyl (C 7 to C 12 ), fatty acid chain (C 13 to C 24 ), aryl, aralkyl, hydroxyl; the stereoisomers being in their resolved or racemic form; z=0, 1 or 2; the cycloalkyl ring being replaced with the cycloalkenyl ring; and the pharmaceutically acceptable salts thereof.
Claim 18
Dependent Claim
98 words
A potent selective excitatory amino acid neurotransmitter receptor antagonist having the general formula: ##STR7## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C 1 to C 6 ), alkyl (C 7 to C 12 ), fatty acid chain (C 13 to C 24 ), aryl, aralkyl, hydroxyl, the stereoisomers being in their resolved or racemic form; n and m=1, 2, or 3 and z=0, 1 or 2; the cyclic ring is either a cycloalkanyl or a cycloalkenyl ring and the pharmaceutically acceptable salts thereof.
Claim 19
Dependent Claim
98 words
A potent selective excitatory amino acid neurotransmitter receptor antagonist having the general formula: ##STR7## wherein R 1 and R 2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C 1 to C 6 ), alkyl (C 7 to C 12 ), fatty acid chain (C 13 to C 24 ), aryl, aralkyl, hydroxyl, the stereoisomers being in their resolved or racemic form; n and m=1, 2, or 3 and z=0, 1 or 2; the cyclic ring is either a cycloalkanyl or a cycloalkenyl ring and the pharmaceutically acceptable salts thereof.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-08-02 | 1992-02-01 | 1992-08-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-08-02 | 1996-02-01 | 1996-08-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-08-02 | 2000-02-01 | 2000-08-02 | $7700.00 | Window Closed / Lapsed |