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US 6,762,320 B2Granted
N-acylamino benzyl ether derivatives
AssigneeHoffman-La Roche Inc.
InventorsSynese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Abstract
This invention relates to N-acylamino aryl derivatives of the formula where R1, R21, R22, R23, R24, R3, R4, R5 R6, R7, R8, R, and n are as defined herein and where X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH═CH— or —C≡C—. The compounds of the invention are selective monoamine oxidase B inhibitors, and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B, for example, for the treatment of Alzheimer's disease or senile dementia.
Claims24
A compound of the formula
- wherein
- R1 is halogen, halogen-(C1-C6)-alkyl, cyano, (C1-C6)-alkoxy or halogen-(C1-C6)-alkoxy;
- R21, R22, R23 and R24 are each independently selected from the group consisting of hydrogen, (C1-C6)-alkyl, halogen, halogen-(C1-C6)-alkyl, hydroxy, (C1-C6)-alkoxy or —CHO;
- R3 is hydrogen or (C1-C3)-alkyl;
- R4, R5 are each independently selected from the group consisting of hydrogen, (C1-C6)-alkyl, (C1-C6)-alkoxy or —COO(C1-C6)alkyl, or, alternatively, R4 and R5, together with the C-atom to which they are attached, for
- a (C3-C7)-cycloalkyl ring;
- R6 is —CO—NR7R8, —COO(C1-C6)-alkyl, —CN, —N(R)2 or —NHC(O)R;
- R7 and R8 are each independently selected from the group consisting of hydrogen, (C1-C6)-alkyl, NH2 or hydroxy;
- R is hydrogen or (C1-C6)-alkyl;
- n is 0, 1, 2 or 3;
- X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH═CH— or —C≡C—;
- or a pharmaceutically acceptable salt thereof.
9 more elements
A composition comprising one or more compounds of the formula
- wherein
- R1 is halogen, halogen-(C1-C6)-alkyl, cyano, (C1-C6)-alkoxy or halogen-(C1-C6)-alkoxy;
- R21, R22, R23 and R24 are each independently selected from the group consisting of hydrogen, (C1-C6)-alkyl, halogen, halogen-(C1-C6)-alkyl, hydroxy, (C1-C6)-alkoxy or —CHO;
- R3 is hydrogen or (C1-C3)-alkyl;
- R4, R5 are each independently selected from the group consisting of hydrogen, (C1-C6)-alkyl, (C1-C6)-alkoxy or —COO(C1-C6)alkyl;
- Or, alternatively, R4 and R5, together with the carbon atom to which they are attached, form a (C3-C7)-cycloalkyl ring;
- R6 is —CO—NR7R8, —COO(C1-C6)-alkyl, —CN, —NR2 or —NHC(O)R;
- R7 and R8 are each independently selected from the group consisting of hydrogen, (C1-C6)-alkyl, NH2 or hydroxy;
- R is hydrogen or (C1-C6)-alkyl;
- n is 0, 1, 2 or 3;
- X is —CHRO, —OCHR—, —CH2S—, —SCH2—, —CH2CH2—, —CH═CH— or —C≡C—;
- or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
9 more elements
Dependencies are inferred from the claim text.