US4888347A
Expired / Lapsed
US
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Use of specific N-methyl-D-aspartate receptor antagonists in the prevention and treatment of neurodegeneration
Assignee: Organon Pharma UK Ltd
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Filing: 1986-12-24
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Granted: 1989-12-19
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Expires: 2006-12-24
Abstract
Abstract Specific N-methyl-D-aspartate receptor antagonists are useful in the prevention and treatment of neurodegeneration in various pathological states.
Inventors
- 👤 Geoffrey N. Woodruff
- 👤 Erik H. F. Wong
- 👤 John A. Kemp
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 06:07
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/40; A61K31/435; A61K31/46; A61P; A61P25/00; A61P43/00
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
162 words
A method of producing a neuroprotective effect by selectively antagonizing N-methyl-D-aspartate receptors which comprises the administration to a patient in need of such treatment, of an effective amount of a compound of structural formula: ##STR6## or a pharmaceutically acceptable salt thereof, wherein R is (1) hydrogen, (2) C 1-5 alkyl, (3) C 2-5 alkenyl, (4) (optionally substituted phenyl)-(C 1-3 alkyl), (5) C 3-6 cycloalkyl, (6) (C 3-6 cycloalkyl)-(C 1-3 alkyl), or (7) di(C 1-5 alkyl)amino-(C 1-3 alkyl); R 1 is (1) hydrogen, (2) C 1-5 alkyl, (3) C 2-5 alkenyl, (4) phenyl-(C 1-3 alkyl), (5) C 3-6 cycloalkyl, or (6) (C 3-6 cycloalkyl)-(C 1-3 alkyl); R 2 is (1) C 1-5 alkyl, (2) C 1-5 alkenyl, (3) phenyl-(C 1-3 alkyl), (4) (C 3-6 cycloalkyl)-C 1-3 alkyl), (5) di(C 1-5 alkyl)amino-C 1-5 alkyl), or (6) (C 2-3 hydroxyalkyl); and R 3 and R 4 are independently, (1) hydrogen (2) halogen, (3) C 1-5 alkoxy, (4) trifluoromethylthio, (5) cyano, (6) carboxy, or (7) hydroxy.
Claim 2
Independent Claim
162 words
A method of producing a neuroprotective effect by selectively antagonizing N-methyl-D-aspartate receptors which comprises the administration to a patient in need of such treatment, of an effective amount of a compound of structural formula: ##STR6## or a pharmaceutically acceptable salt thereof, wherein R is (1) hydrogen, (2) C 1-5 alkyl, (3) C 2-5 alkenyl, (4) (optionally substituted phenyl)-(C 1-3 alkyl), (5) C 3-6 cycloalkyl, (6) (C 3-6 cycloalkyl)-(C 1-3 alkyl), or (7) di(C 1-5 alkyl)amino-(C 1-3 alkyl); R 1 is (1) hydrogen, (2) C 1-5 alkyl, (3) C 2-5 alkenyl, (4) phenyl-(C 1-3 alkyl), (5) C 3-6 cycloalkyl, or (6) (C 3-6 cycloalkyl)-(C 1-3 alkyl); R 2 is (1) C 1-5 alkyl, (2) C 1-5 alkenyl, (3) phenyl-(C 1-3 alkyl), (4) (C 3-6 cycloalkyl)-C 1-3 alkyl), (5) di(C 1-5 alkyl)amino-C 1-5 alkyl), or (6) (C 2-3 hydroxyalkyl); and R 3 and R 4 are independently, (1) hydrogen (2) halogen, (3) C 1-5 alkoxy, (4) trifluoromethylthio, (5) cyano, (6) carboxy, or (7) hydroxy.
Claim 3
Independent Claim
36 words
A method of producing a neuroprotective effect by selectively antagonizing N-methyl-D-aspartate receptors which comprises the administration to a patient in need of such treatment, of an effective amount of 5-methyl-10,11-dihydro-5H-dibenzo[a,d]-cyclohepten-5-10-imine or a pharmaceutically acceptable salt thereof.
Claim 4
Independent Claim
36 words
A method of producing a neuroprotective effect by selectively antagonizing N-methyl-D-aspartate receptors which comprises the administration to a patient in need of such treatment, of an effective amount of 5-methyl-10,11-dihydro-5H-dibenzo[a,d]-cyclohepten-5-10-imine or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
11 words
The method according to claim 1, wherein R 1 is hydrogen.
Claim 6
Dependent Claim
41 words
The method according to claim 1, wherein R 1 , R 3 and R 4 are hydrogen, R is hydrogen, C 1-5 alkyl, phenyl-C 1-3 alkyl or chlorophenyl-C 1-3 alkyl, and R 2 is C 1-5 alkyl or hydroxy-C 2-3 alkyl.
Claim 7
Independent Claim
12 words
The method as described in claims 1, wherein the compounds are dextrorotatory.
Claim 8
Dependent Claim
12 words
The method as described in claim 3, wherein the compounds are dextrorotatory.
Claim 9
Dependent Claim
12 words
The method as described in claim 4, wherein the compounds are dextrorotatory.
Claim 10
Dependent Claim
12 words
The method as described in claim 2, wherein the compound is dextrorotatory.
References Cited (Backward Citations)
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