US2003130354A1PendingUtilityA1
1-(Adamantyl) amidines and their use in the treatment of conditions generally associated with abnormalities in glutamatergic transmission
Est. expiryDec 12, 2017(expired)· nominal 20-yr term from priority
A61P 43/00C07C 257/16A61P 25/28C07C 2603/74C07C 257/14A61P 25/00
47
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Claims
Abstract
Use of a compound of the formula (1), wherein X is an alkylene chain comprising 0, 1, 2, 3 or 4 carbon atoms; R 1 , R 2 and R 3 are independently selected from hydrogen, alkyl and aryl; R 4 , R 5 and R 6 are independently selected from hydrogen, alkyl, aryl, halogen and alkoxy; and prodrugs thereof and pharmaceutically acceptable salts thereof; in the manufacture of a medicament for use in the treatment of a condition generally associated with abnormalities in glutamatergic transmission.
Claims
exact text as granted — not AI-modified1 . Use of a compound of the formula (1):
Wherein X is an alkylene chain comprising 0, 1, 2, 3 or 4 carbon atoms;
R 1 , R 2 and R 3 are independently selected from hydrogen, alkyl and aryl;
R 4 , R 5 and R 6 are independently selected from hydrogen, alkyl, aryl, halogen and alkoxy;
and prodrugs thereof and pharmaceutically acceptable salts thereof;
in the manufacture of a medicament for use in the treatment of a condition generally associated with abnormalities in glutamatergic transmission
2 . Use of a compound according to claim 1 wherein X is an alkylene chain comprising 1, 2, 3 or 4 carbon atoms and one or more carbon atom(s) of the chain X is/are independently substituted by substituent group(s) selected from allyl and aryl.
3 . Use of a compound according to claim 2 wherein a substituted carbon atom is substituted by one substituent group selected from alkyl and aryl.
4 . Use of a compound according to claim 2 wherein a substituted carbon atom is substituted by two substituent groups independently selected from allyl and aryl.
5 . Use of a compound according to claim 2 , 3 or 4 wherein the substituent group(s) are selected from methyl, ethyl, phenyl and benzyl.
6 . Use of a compound according to claim 2 , 3 , 4 or 5 wherein one carbon atom of the chain X is substituted.
7 . Use of a compound according to claim 1 wherein X is (CH 2 ) n where n=0 to 4.
8 . Use of a compound according to any one of claims 1 to 7 wherein X is an alkylene chain comprising 1 or 2 carbon atoms in the chain.
9 . Use of a compound according to claim 7 wherein n=0.
10 . Use of a compound according to any preceding claim wherein R 1 and R 2 are hydrogen and R 3 is selected from hydrogen, alkyl and aryl.
11 . Use of a compound according to any preceding claim wherein R 1 , R 2 and R 3 are hydrogen.
12 . Use of a compound according to any one of claims 1 to 11 wherein at least one of R 4 , R 5 and R 6 is alkyl, aryl halogen or alkoxy.
13 . Use of a compound according to any one of claims 1 to 12 wherein R 4 is selected from hydrogen, allyl and halogen.
14 . Use of a compound according to any one of claims 1 to 13 wherein R 5 is selected from hydrogen and alkyl.
15 . Use of a compound according to any one of claims 1 to 14 wherein R 6 is selected from hydrogen and alkyl.
16 . Use of a compound according to claim 1 wherein X has 0 carbon atoms; R 1 , R 2 and R 3 are hydrogen; R 4 and R 5 are CH 3 ; and R 6 is hydrogen.
17 . Use of a compound according to claim 1 wherein X has 0 carbon atoms; R 1 , R 2 and R 3 are hydrogen; R 4 is methyl; and R 5 =R 6 =hydrogen or methyl
18 . Use of a compound according to claim 2 wherein X has one carbon atom and is substituted by an ethyl or benzyl group; and R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are hydrogen.
19 . Use of a compound according to claim 1 wherein X has one carbon atom and is unsubstituted; R 1 , R 2 and R 3 are hydrogen; R 4 and R 5 are methyl and R 6 is hydrogen.
20 . A compound of formula (1) as defined in any of claims 1 to 19 wherein at least one of R 4 , R 5 and R 6 is alkyl, aryl, halogen or alkoxy, with the proviso that if R 1 , R 2 and R 3 are hydrogen and R 4 , R 5 and R 6 are independently selected from hydrogen and C 1-4 alkyl, then either X is an alkylene chain comprising 2, 3 or 4 carbon atoms, substituted or unsubstituted, or X is an alkylene chain of one carbon atom substituted with one or two substituent group(s) independently selected from alkyl and aryl and prodrugs and pharmaceutically acceptable salts thereof.
21 . A compound of formula (1) as defined in any of claims 1 to 19 wherein R 4 , R 5 and R 6 are hydrogen and either X is an alkylene chain of 2, 3, or 4 carbon atoms, substituted or unsubstituted, or X is an alkylene chain of 1 carbon atom substituted with one or two substituent group(s) independently selected from alkyl and aryl, or X is a CH 2 group, with the proviso that where X is a CH 2 group then at least one of R 1 , R 2 and R 3 are selected from alkyl and aryl, and prodrugs and pharmaceutically acceptable salts thereof.
22 . A compound of formula (2), (3), (4) or (5):
and prodrugs and pharmaceutically acceptable salts thereof
23 . A compound according to any one of claims 20 to 22 for use in therapy.
24 . A pharmaceutical composition comprising a compound according to any one of claims 20 to 22 in combination with a pharmaceutically acceptable excipient
25 . A method of treatment of a condition generally associated with abnormalities in glutamatergic transmission comprising administration to a patient in need of such treatment of a pharmaceutically effective dose of a compound of formula (1) as defined in any one of claims 1 to 19 .Join the waitlist — get patent alerts
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