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US 2003/0119871 A1Published application
Amidine derivatives as selective antagonists of ndma receptors
OwnerNeil Roy Curtis, Janusz Jozef Kulagowski +2inventors
InventorsNeil Roy Curtis, Janusz Jozef Kulagowski, Steve Thomas, Alan Paul Watt
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Abstract
A class of styryl amidine derivatives which are antagonists of the hum NMDA receptor, being selective for those containing the NR2B subunit, are active in the treatment and/or prevention of neurological and neurodegenerative disorders, in particular neuropathic pain and headache, specifically migraine, whils displaying fewer ataxic and related side-effects associated with other classes of NMDA receptor antagonists.
Claims11
A compound of formula I, or a pharmaceutically acceptable salt, hydrate or prodrug thereof:
- 13
- wherein:
- R1 represents C1-6 alkyl, C3-7 cycloalkyl, C3-7 Cycloalkyl(C1-6)alkyl, aryl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted;
- R2 represents C3-7 cycloalkyl, aryl or heteroaryl, any of which groups may be optionally substituted;
- and
- R3 represents hydrogen or C1-6 alkyl;
- or
- R1 and R3 are taken together with the intervening nitrogen atom to form an optionally substituted isoquinoline ring.
5 more elements
A compound selected from:
- (E)-N-(3-iodobenzyl)cinnamamidine;
- (E)-N-(benzyl)cinnamamidine;
- (E)-N-(4-chlorobenzyl)cinnamamidine;
- (E)-N-(2-chlorobenzyl)cinnamamidine;
- (E)-N-(3-chlorobenzyl)cinnamamidine;
- (E)-N-(4-fluorobenzyl)cinnamamidine;
- (E)-N-(4-trifluoromethylbenzyl)cinnamamidine;
- (E)-N-(4-methoxybenzyl)cinnamamidine;
- (E)-N-(4-methylbenzyl)cinnamamidine;
- (E)-N-(3-methylbenzyl)cinnamamidine;
- (E)-N-(2-methylbenzyl)cinnamamidine;
- (E)-N-(3,4-dichlorobenzyl)cinnamamidine;
- (E)-N-(2-phenylethyl)cinnamamidine;
- (E)-N-(R)-α-methylbenzylcinnamamidine;
- (E)-N-(S)-α-methylbenzylcinnamamidine;
- (E)-N-(3-trifluoromethylbenzyl)cinnamamidine;
- (E)-N-(3,5-dichlorobenzyl)cinnamamidine;
- (E)-N-(2-methoxybenzyl)cinnamamidine;
- (E)-N-(3-methoxybenzyl)cinnamamidine;
- (E)-N-(2-trifluoromethylbenzyl)cinnamamidine;
- (E)-N-(2,5-dichlorobenzyl)cinnamamidine;
- (E)-N-(3-bromobenzyl)cinnamamidine;
- (E)-N-(4-pyridylmethyl)cinnamamidine;
- (E)-N-methyl-N-benzylcinnamamidine;
- (E)-N-(2,3-dicblorobenzyl)cinnamamidine;
- (E)-N-(cyclohexylmethyl)cinnamamidine;
- (E)-N-(isobutyl)cinnamamidine;
- (E)-N-(n-butyl)cinnamamidine;
- (E)-N-(2-trifluoromethoxybenzyl)cinnamamidine;
- (E)-N-(3-thienylmethyl)cinnamamidine;
- (E)-N-(2-bromobenzyl)cinnamamidine;
- (E)-N-(2-ethoxybenzyl)cinnamamidine;
- (E)-N-(2-phenylbenzyl)cinnamamidine;
- (E)-N-(2-furylmethyl)cinnamamidine;
- (E)-N-(cyclohcxyl)cinnamamidine;
- (E)-N-(3-methyl-1-butyl)cinnamamidine;
- (E)-2-(3-phenyl-1-imino-2-propenyl)-1,2,3,4-tetrahydroisoquinoline;
- (E)-N-(n-pentyl)cinnamamidine;
- (E)-N-(3-phenyl-1-propyl)cinnamamidine;
- (E)-N-(2-hydroxybenzyl)cinnamamidine;
- (E)-N-phenylcinnamanidine;
- (E)-N-benzyl-2-chlorocinnamamidine;
- (E)-N-benzyl-3-chlorocinnamamidine;
- (E)-N-benzyl-4-chlorocinnamamidine;
- (E)-N-benzyl-4-fluorocinnamamidine;
- (E)-N-benzyl-4-methoxycinnamamidine;
- (E)-N-benzyl-3-methoxycinnamamidine;
- (E)-N-benzyl-2-methoxycinnamamidine;
- (E)-N-benzyl-3,4-difluorocinnamamidine;
- (E)-N-benzyl-3-cyclohexaneacrylamidine;
- and pharmaceutically acceptable salts, hydrates and prodrugs thereof.
48 more elements
Dependencies are inferred from the claim text.