US4918064A
Expired / Lapsed
US
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Phenyl glycines for use in reducing neurotoxic injury
Assignee: GD Searle LLC
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Filing: 1987-10-21
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Granted: 1990-04-17
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Expires: 2007-10-21
Abstract
Abstract A class of phenyl glycine compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phenyl glycine compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites.
Inventors
- 👤 Alex A. Cordi
- 👤 Michael L. Vazquez
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 17:17
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/38; C07F9/3804; C07F9/3882; A; A61; A61P; A61P25/00; A61P25/04; A61P25/08; A61P25/28; A61P39/00; A61P39/02; A61P43/00; A61P9/00; A61P9/10; C07F9/40; C07F9/4003; C07F9/4056
Claims Analysis
Total Claims: 45
Claim 1
Independent Claim
160 words
A method to control neuropathological processes and the neurodegenerative consequences thereof in mammals, which method comprises treating a mammal susceptible to neurologic injury with an effective amount of a compound of the formula ##STR16## wherein each of R 1 through R 4 is independently selected from hydrido, alkyl, cycloalkyl, aralkyl, aryl, haloalkyl, halo, cyano, nitro, and groups represented by --OR 5 , --SR 5 , ##STR17## wherein each R 5 is independently selected from hydrido, alkyl, aryl, and aralkyl; and wherein each of R 6 and R 7 is independently selected from hydrido, alkyl, acyl, aryl, aralkyl and ##STR18## and wherein Z is selected from --OR 5 , --SR 5 , ##STR19## and ##STR20## wherein each of R 5 , R 6 and R 7 defined as before; with the proviso that R 6 and R 7 are not at the same time carbonyl-containing groups; and wherein R 8 is selected from hydrido and alkyl; or a pharmaceutically-acceptable salt thereof.
Claim 2
Independent Claim
160 words
A method to control neuropathological processes and the neurodegenerative consequences thereof in mammals, which method comprises treating a mammal susceptible to neurologic injury with an effective amount of a compound of the formula ##STR16## wherein each of R 1 through R 4 is independently selected from hydrido, alkyl, cycloalkyl, aralkyl, aryl, haloalkyl, halo, cyano, nitro, and groups represented by --OR 5 , --SR 5 , ##STR17## wherein each R 5 is independently selected from hydrido, alkyl, aryl, and aralkyl; and wherein each of R 6 and R 7 is independently selected from hydrido, alkyl, acyl, aryl, aralkyl and ##STR18## and wherein Z is selected from --OR 5 , --SR 5 , ##STR19## and ##STR20## wherein each of R 5 , R 6 and R 7 defined as before; with the proviso that R 6 and R 7 are not at the same time carbonyl-containing groups; and wherein R 8 is selected from hydrido and alkyl; or a pharmaceutically-acceptable salt thereof.
Claim 3
Dependent Claim
9 words
The method of claim 1 wherein Z is hydroxyl.
Claim 4
Dependent Claim
10 words
The method of claim 2 wherein R 6 is hydrido.
Claim 5
Dependent Claim
25 words
The method of claim 3 wherein at least one of the substituents R 1 , R 2 , R 3 and R 4 are hydrido.
Claim 6
Dependent Claim
25 words
The method of claim 4 wherein two or more of the substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 7
Dependent Claim
23 words
The method of claim 5 wherein three or more substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 8
Dependent Claim
26 words
The method of claim 6 wherein each of the substituents R 1 , R 2 , R 3 , R 4 and R 5 is hydrido.
Claim 9
Dependent Claim
31 words
The method of claim 1 wherein each of the substituents R 1 , R 2 , R 3 or R 4 is independently selected from hydrido, halo, alkyl, alkoxy and thioalkoxy.
Claim 10
Dependent Claim
25 words
The method of claim 8 wherein two or more of the substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 11
Dependent Claim
27 words
The method of claim 8 wherein three or more of there of the substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 12
Dependent Claim
23 words
The method of claim 36 wherein each of the substituents R 1 , R 2 , R 3 and R 4 are hydrido.
Claim 13
Dependent Claim
10 words
The method of claim 8 wherein said compound is 4-(phosphonomethyl)phenylglycine.
Claim 14
Dependent Claim
11 words
The method of claim 8 wherein said compound is 4-(Ethyl phosphonomethyl)phenylglycine.
Claim 15
Dependent Claim
11 words
The method of claim 8 wherein said compound is 2,5-dimethyl-4-(phosphonomethyl)phenylglycine hydrochloride.
Claim 16
Dependent Claim
132 words
A compound of the formula ##STR21## wherein each of R 1 through R 4 is independently selected from hydrido, alkyl, cycloalkyl, aralkyl, aryl, haloalkyl, halo, cyano, nitro, and groups represented by --OR 5 , --SR 5 ##STR22## wherein each R 5 is independently selected from hydrido, alkyl, aryl, and aralkyl; and wherein each of R 6 and R 7 is independently selected from hydrido, alkyl, acyl, aryl, aralkyl and ##STR23## and wherein Z is selected from --OR 5 , --SR 5 , ##STR24## and ##STR25## wherein each of R 5 , R 6 and R 7 is defined as before; with the proviso that R 6 and R 7 are not at the same time carbonyl-containing groups; and wherein R 8 is selected from hydrido and alkyl; or a pharmaceutically-acceptable salt thereof.
Claim 17
Dependent Claim
132 words
A compound of the formula ##STR21## wherein each of R 1 through R 4 is independently selected from hydrido, alkyl, cycloalkyl, aralkyl, aryl, haloalkyl, halo, cyano, nitro, and groups represented by --OR 5 , --SR 5 ##STR22## wherein each R 5 is independently selected from hydrido, alkyl, aryl, and aralkyl; and wherein each of R 6 and R 7 is independently selected from hydrido, alkyl, acyl, aryl, aralkyl and ##STR23## and wherein Z is selected from --OR 5 , --SR 5 , ##STR24## and ##STR25## wherein each of R 5 , R 6 and R 7 is defined as before; with the proviso that R 6 and R 7 are not at the same time carbonyl-containing groups; and wherein R 8 is selected from hydrido and alkyl; or a pharmaceutically-acceptable salt thereof.
Claim 18
Dependent Claim
8 words
Compound of claim 15 wherein Z is hydroxyl.
Claim 19
Dependent Claim
9 words
Compound of claim 16 wherein R 6 is hydrido.
Claim 20
Dependent Claim
24 words
Compound of claim 17 wherein at least one of the substituents R 1 , R 2 , R 3 and R 4 is hydrido.
Claim 21
Dependent Claim
22 words
Compound of claim 18 wherein two or more of the substituents R 1 R 2 R 3 or R 4 are hydrido.
Claim 22
Dependent Claim
22 words
Compound of claim 19 wherein three or more substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 23
Dependent Claim
23 words
Compound claim 20 wherein each of the substituents R 1 , R 2 , R 3 R 4 and R 5 is hydrido.
Claim 24
Dependent Claim
30 words
Compound of claim 15 wherein each of the substituents R 1 , R 2 , R 3 or R 4 is independently selected from hydrido, halo, alkyl, alkoxy and thioalkoxy.
Claim 25
Dependent Claim
23 words
Compound of claim 22 wherein two or more of the substituents R 1 , R 2 R 3 or R 4 are hydrido.
Claim 26
Dependent Claim
24 words
Compound of claim 22 wherein three or more of the substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 27
Dependent Claim
22 words
Compound of claim 22 wherein each of the substituents R 1 , R 2 , R 3 and R 4 is hydrido.
Claim 28
Dependent Claim
7 words
Compound of claim 22 which is 4-(phosphonomethyl)phenylglycine.
Claim 29
Dependent Claim
8 words
Compound of claim 22 which is 4-(Ethyl phosphonomethyl)phenylglycine.
Claim 30
Dependent Claim
8 words
Compound of claim 22 which is 2,5-dimethyl-4-(phosphonomethyl)phenylglycine hydrochloride.
Claim 31
Dependent Claim
155 words
A pharmaceutical composition comprising a therapeutically-effective amount of a compound and a pharmaceutically-acceptable carrier or diluent, said compound selected from a family of compounds of the formula ##STR26## wherein each of R 1 through R 4 is independently selected from hydrido, alkyl, cycloalkyl, aralkyl, aryl, haloalkyl, halo, cyano, nitro, and groups represented by --OR 5 , --SR 5 , ##STR27## wherein each R 5 is independently selected from hydrido, alkyl, aryl, and aralkyl; and wherein each of R 6 and R 7 is independently selected from hydrido, alkyl, acyl, aryl, aralkyl and ##STR28## and wherein Z is selected from --OR 5 , --SR 5 , ##STR29## and ##STR30## wherein each of R 5 , R 6 and R 7 is defined as before; with the proviso that R 6 and R 7 are not at the same time carbonyl-containing groups; and wherein R 8 is selected from hydrido and alkyl; or a pharmaceutically-acceptable salt thereof.
Claim 32
Dependent Claim
155 words
A pharmaceutical composition comprising a therapeutically-effective amount of a compound and a pharmaceutically-acceptable carrier or diluent, said compound selected from a family of compounds of the formula ##STR26## wherein each of R 1 through R 4 is independently selected from hydrido, alkyl, cycloalkyl, aralkyl, aryl, haloalkyl, halo, cyano, nitro, and groups represented by --OR 5 , --SR 5 , ##STR27## wherein each R 5 is independently selected from hydrido, alkyl, aryl, and aralkyl; and wherein each of R 6 and R 7 is independently selected from hydrido, alkyl, acyl, aryl, aralkyl and ##STR28## and wherein Z is selected from --OR 5 , --SR 5 , ##STR29## and ##STR30## wherein each of R 5 , R 6 and R 7 is defined as before; with the proviso that R 6 and R 7 are not at the same time carbonyl-containing groups; and wherein R 8 is selected from hydrido and alkyl; or a pharmaceutically-acceptable salt thereof.
Claim 33
Dependent Claim
9 words
The composition of claim 29 wherein Z is hydroxyl.
Claim 34
Dependent Claim
10 words
The composition of claim 30 wherein R 6 is hydrido.
Claim 35
Dependent Claim
25 words
The composition of claim 31 wherein at least one of the substituents R 1 , R 2 , R 3 and R 4 is hydrido.
Claim 36
Dependent Claim
25 words
The composition of claim 32 wherein two or more of the substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 37
Dependent Claim
23 words
The composition of claim 33 wherein three or more substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 38
Dependent Claim
25 words
The composition claim 34 wherein each of the substituents R 1 , R 2 , R 3 , R.sup. 4 and R 5 is hydrido.
Claim 39
Dependent Claim
31 words
The composition of claim 29 wherein each of the substituents R 1 , R 2 , R 3 or R 4 is independently selected from hydrido, halo, alkyl, alkoxy and thioalkoxy.
Claim 40
Dependent Claim
25 words
The composition of claim 36 wherein two or more of the substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 41
Dependent Claim
25 words
The composition of claim 36 wherein three or more of the substituents R 1 , R 2 , R 3 or R 4 are hydrido.
Claim 42
Dependent Claim
23 words
The composition of claim 36 wherein each of the substituents R 1 , R 2 , R 3 and R 4 is hydrido.
Claim 43
Dependent Claim
10 words
The composition of claim 36 wherein said compound is 4-(phosphonomethyl)phenylglycine.
Claim 44
Dependent Claim
11 words
The composition of claim 36 wherein said compound is 4-(ethyl phosphonomethyl)phenylglycine.
Claim 45
Dependent Claim
11 words
The composition of claim 36 wherein said compound is 2,5-dimethyl-4-(phosphonomethyl)phenylglycine hydrochloride.
References Cited (Backward Citations)
US4657899A
Cited
US4761405A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1993-04-16 | 1993-10-16 | 1994-04-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-04-16 | 1997-10-16 | 1998-04-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-04-16 | 2001-10-16 | 2002-04-17 | $7700.00 | Window Closed / Lapsed |