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US 6,720,452 B2Granted
Adamantane derivatives
AssigneeAstraZeneca AB
InventorsLilian Alcaraz, Mark Furber, Timothy Luker, Michael Mortimore, Philip Thorne
Life of this patent
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Abstract
The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
Claims15
A compound of general formula
- wherein D represents CH2 or CH2CH2;
- E represents C(O)NH or NHC(O);
- R1 and R2 each independently represent a hydrogen or halogen atom, or an amino, nitro, C1-C6
- alkyl or trifluoromethyl group;
- R3 represents a group of formula
- X represents an oxygen or sulphur atom or a group NH, SO or SO2;
- Y represents an oxygen or sulphur atom or a group NR11, SO or SO2;
- Z represents a group —OH, —SH, —CO2H, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6-alkylsulphinyl, C1-C6-alkylsulphonyl, —NR6R7, —C(O)NR8R9, imidazolyl, 1-methylimidazolyl, —N(R10)C(O)—C1-C6 alkyl, C1-C6 alkylcarbonyloxy, C1-C6 alkoxycarbonyloxy, —OC(O)NR12 R13, —OCH2OC(O)R14, —OCH2OC(O)OR15 or —OC(O)OCH2OR6;
- R4 represents a linear or branched C2-C6 alkylene group;
- R5 represents a linear or branched C1-C6 alkylene group;
- R6, R7, R8, R9, R10, R12 and R13 each independently represent a hydrogen atom, or a C1-C6 alkyl group optionally substituted by at least one hydroxyl group;
- R11 represents a hydrogen atom, or a C1-C6 alkyl group optionally substituted by at least one substituent independently selected from hydroxyl and C1-C6 alkoxy;
- and
- R14, R15 and R16 each independently represent a C1-C6 alkyl group;
- with the provisos that (i) when E represents NHC(O), X represents O, S or NH and Y represents O, then Z represents —NR6R7 where R6 represents a hydrogen atom and R7 represents either a hydrogen atom or a C1-C6 alkyl group substituted by at least one hydroxyl group, and (ii) when E represents NHC(O), X represents O, S or NH, Y represents NH and
- R5 represents CH2CH2, then Z is not —OH or imidazolyl;
- or a pharmaceutically acceptable salt or solvate thereof.
14 more elements
Dependencies are inferred from the claim text.