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US 6,242,470 B1Granted
Adamantane derivatives
AssigneeAstraZeneca AB
InventorsAndrew Baxter, Stephen Brough, Thomas McInally, Michael Mortimore
Life of this patent
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Abstract
The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.
Claims11
A compound of general formula
- wherein A represents a CH2 group;
- B represents a hydrogen or halogen atom;
- D represents a group CH2, OCH2, NHCH2 or CH2CH2;
- R represents a phenyl group, which may be optionally substituted by one or more substituents independently selected from a halogen atom or a cyano, carboxyl, hydroxyl, nitro, halo-C1-C6-alkyl, —N(R1)—C(═O)—R2, —C(O)NR3R4, —NR5R6, C3-C8-cycloalkyl, 3- to 8-membered heterocyclyl, C3-C8-cycloalkyloxy, C1-C6-alkylcarbonyl, phenoxy, benzyl, C1-C6-alkylthio, phenylthio, C1-C6-alkoxycarbonyl, C1-C6-alkylsulphinyl or C1-C6-alkylsulphonyl group, or a C1-C6-alkyl or C1-C6-alkoxy group optionally substituted by one or more substituents independently selected from a halogen atom or an amino, carboxyl, hydroxyl, C1-C6-alkoxy, (di)C1-C6-alkylamino, C1-C6-alkoxycarbonyl, imidazolyl, morpholinyl, piperldinyl or pyrrolidinyl group;
- R1 represents a hydrogen atom or a C1-C6-alkyl or C3-C8-cycloalkyl group;
- R2 represents a C1-C6-alkyl or C3-C8-cycloalkyl group;
- and
- R3, R4, R5 and R6 each independently represent a hydrogen atom or a C1-C6-alkyl or C3-C8-cycloalkyl group;
- with the provisos that (i) when A is CH2, B is H and D is CH2, then R does not represent a phenyl, ortho-carboxyphenyl, ortho-nitrophenyl, ortho-aminophenyl, ortho-(dimethylaminoethyl)phenyl, methylphenyl or para-phenoxyphenyl group, and (ii) when A is CH2, B is Br and D is CH2, then R does not represent an orthocarboxyphenyl group, and (iii) when A is CH2, B is H and D is CH2CH2, then R does not represent a phenyl group, and (iv) when A is CH2 D is CH2 or CH2CH2 and R represents a substituted phenyl group, the substituent or substituents present do not comprise, in an ortho position, a C1-C6-alkoxy group substituted by an amino, (di)C1-C6-alkylamino, imidazolyl, morpholinyl, piperidinyl or pyrrolidinyl group;
- or a pharmaceutically acceptable salt or solvate thereof.
7 more elements
Dependencies are inferred from the claim text.