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US 2003/0158235 A1Published application
Pyridine amido derivatives
AssigneeHoffmann-La Roche Inc.
InventorsAndrea Cesura, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Abstract
Disclosed are pyridine amido derivatives of the formula 1 wherein X, Y, and R1 to R6 are as defined herein. These compounds are selective MAO-B inhibitors and are useful in treating diseases such as, for example, Alzheimer's and senile dementia. Also disclosed are pharmaceutical compositions containing such compounds and a method of preparing such compounds.
Claims16
A compound of formula
- 10
- wherein
- one of X or Y is —N═ and the other one is —CR7═;
- R1 is hydrogen or C1-C6-alkyl;
- R2 is hydrogen or C1-C6-alkyl;
- R3 is hydrogen or C1-C6-alkyl;
- R4 is selected from the group halogen-(C1-C6)-alkyl, unsubstituted aryl, and aryl substituted by one or more substituents selected from the group C1-C6-alkyl, halogen, halogen-(C1-C6)-alkyl, (C1-C6)-alkoxy and cyano;
- R5 is hydrogen or C1-C6-alkyl;
- R6 is hydrogen or C1-C6-alkyl;
- and
- R7 is hydrogen or C1-C6-alkyl;
- or a pharmaceutically acceptable salt thereof.
9 more elements
A process for the preparation of a compound of formula I comprising:
- reacting a compound of formula
- 11
- with a compound of formula
- 12
- to obtain a compound of formula
- 13
- wherein
- one of X or Y is —N═ and the other one is —CR7═;
- R1 is hydrogen or C1-C6-alkyl;
- R2 is hydrogen or C1-C6-alkyl;
- R3 is hydrogen or C1-C6-alkyl;
- R4 is selected from the group halogen-(C1-C6)-alkyl, unsubstituted aryl, and aryl substituted by one or more substituents selected from the group C1-C6-alkyl, halogen, halogen-(C1-C6)-alkyl, (C1-C6)-alkoxy and cyano;
- R5 is hydrogen or C1-C6-alkyl;
- R6 is hydrogen or C1-C6-alkyl;
- and
- R7 is hydrogen or C1-C6-alkyl.
13 more elements
Dependencies are inferred from the claim text.