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US 2004/0110807 A1Published application
Thiazole derivatives
AssigneeHoffmann-La Roche Inc.
InventorsAlfred Binggeli, Uwe Grether, Hans Hilpert, Georges Hirth, Hans-Peter Maerki, Markus Meyer, Peter Mohr
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Abstract
The present invention provides compounds of formula (I) 1 wherein R1 to R10, X, Y and n are indicated in the specification, and pharmaceutically acceptable salts and esters thereof. The compounds are useful for the treatment of non-insulin dependent diabetes mellitus.
Claims27
A compound of formula (I)
- 21
- wherein
- X is N and Y is S;
- or
- X is S and Y is N;
- R1 is aryl or heteroaryl;
- R2 is hydrogen, lower-alkyl or fluoro-lower-alkyl;
- R3, R4, R5 and R6 independently from each other are selected from hydrogen, hydroxy, lower-alkenyl, halogen, lower-alkyl, fluoro-lower-alkyl, hydroxy-lower-alkyl, lower-alkoxy-lower-alkyl, lower-alkoxy, fluoro-lower-alkoxy, hydroxy-lower-alkoxy, and lower-alkoxy-lower-alkoxy, wherein at least one of R3, R4, R5 and R6 is not hydrogen, or
- R3 and R4 are bonded to each other to form a ring together with the carbon atoms to which they are attached, and R3 and R4 together are —CH═CH—S—, —S—CH═CH—, —CH═CH—O—, —O—CH═CH—, —CH═CH—CH═CH—, —(CH2)3-5—, —O—(CH2)2-3— or —(CH2)2-3—O—, and R5 and R6 are as defined above;
- R7 is lower-alkyl, lower-alkoxy, lower-alkenyloxy, aryloxy or aryl-lower-alkoxy;
- R8 is hydrogen or lower-alkyl;
- R9 and R10 independently from each other are hydrogen, lower-alkyl, lower-alkenyl, cycloalkyl, phenyl or [1,3]dioxan-2-ethyl;
- n is 1, 2 or 3;
- or a pharmaceutically acceptable salt or a pharmaceutically acceptable ester thereof.
11 more elements
A compound of formula (Ia)
- 22
- wherein
- X is N and Y is S;
- or
- X is S and Y is N;
- R1 is aryl or heteroaryl;
- R2 is hydrogen, lower-alkyl or fluoro-lower-alkyl;
- R3, R4, R5 and R6 independently from each other are selected from hydrogen, hydroxy, lower-alkenyl, halogen, lower-alkyl, fluoro-lower-alkyl, hydroxy-lower-alkyl, lower-alkoxy-lower-alkyl, lower-alkoxy, fluoro-lower-alkoxy, hydroxy-lower-alkoxy, and lower-alkoxy-lower-alkoxy, wherein at least one of R3, R4, R5 and R6 is not hydrogen, or
- R3 and R4 are bonded to each other to form a ring together with the carbon atoms to which they are attached, and R3 and R4 together are —CH═CH—S—, —S—CH═CH—, —CH═CH—O—, —O—CH═CH—, —CH═CH—CH═CH—, —(CH2)3-5—, —O—(CH2)2-3— or —(CH2)2-3—O—, and R5 and R6 are as defined above;
- R7 is lower-alkoxy, lower-alkenyloxy, aryloxy or aryl-lower-alkoxy;
- R8 is hydrogen or lower-alkyl;
- n is 1, 2 or 3;
- or a pharmaceutically acceptable salt or a pharmaceutically acceptable ester thereof.
10 more elements
Dependencies are inferred from the claim text.