Back to results
US 2007/0191603 A1Published application
Novel bicyclic sulfonamide derivatives which are L-CPT1 inhibitors
AssigneeHoffmann-La Roche Inc.
InventorsJean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
Life of this patent
Estimating the term…
Abstract
The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
Claims33
A compound of formula (I):
- wherein:
- V is N or —C(R7)—;
- W is a single bond or —C(R8R9)—;
- X is O, S, SO, SO2 or N(R10);
- Y is —C(R11R12)—, —C(R11R12)C(R13R14)—, —C(R11R12)C(R13R14)C(R15R16)—, —C(R11R12)C(R13R14)C(R15R16)C(R17R18)— or —C(R11)═C(R12)—;
- R1, R2, R3, R4 and R5 independently from each other are hydrogen, halogen, cyano, hydroxy, lower-alkyl, fluoro-lower-alkyl, lower-alkoxy, fluoro-lower-alkoxy, lower-alkyl-C(O), lower-alkyl-C(O)—NH, lower-alkyl-C(O)—N(lower-alkyl), lower-alkyl-S(O)2, NH2—S(O)2, N(H,lower-alkyl)-S(O)2 or N(lower-alkyl)2-S(O)2, NH2—C(O), N(H,lower-alkyl)-C(O), N(lower-alkyl)2-C(O), COOH or lower-alkoxy-C(O), wherein lower-alkyl is optionally substituted with hydroxy, NH2, N(H,lower-alkyl) or N(lower-alkyl)2;
- R6 is an aryl or heteroaryl group, which aryl or heteroaryl group is optionally substituted by 1 to 4 substituents selected from the group consisting of halogen, hydroxy, cyano, lower-alkyl, fluoro-lower-alkyl, lower-alkoxy, fluoro-lower-alkoxy, lower-alkyl-C(O), lower-alkyl-C(O)—NH, lower-alkyl-C(O)—N(lower-alkyl), lower-alkyl-S(O)2, NH2—S(O)2, N(H,lower-alkyl)-S(O)2, N(lower-alkyl)2-S(O)2, NH2—C(O), N(H,lower-alkyl)-C(O), N(lower-alkyl)2-C(O), lower-alkoxy-C(O), COOH, 1H-tetrazol-5-yl, 5-oxo-4H-[1,2,4]oxadiazol-3-yl, 5-oxo-4H-[1,2,4]thiadiazol-3-yl, 5-thioxo-4H-[1,2,4]oxadiazol-3-yl, 2-oxo-3H-[1,2,3,5]oxathiadiazol-4-yl, SO3H, 3-hydroxy-isooxazol-5-yl, 6-oxo-6H-pyran-3-yl, 6-oxo-6H-pyran-2-yl, 2-oxo-2H-pyran-3-yl, 2-oxo-2H-pyran-4-yl and P(O)(OCH2CH3)OH, wherein lower-alkyl is optionally substituted with COOH, hydroxy, NH2, N(H,lower-alkyl) or N(lower-alkyl)2, and wherein fluoro-lower-alkyl is optionally substituted with hydroxy;
- R7 is hydrogen, halogen, lower-alkyl, lower-alkoxy, fluoro-lower-alkyl, fluoro-lower-alkoxy, hydroxy or hydroxy-lower-alkyl;
- R8 and R9 independently from each other are hydrogen or lower-alkyl;
- R10 is hydrogen, lower-alkyl, cycloalkyl, lower-alkyl-C(O), lower-alkyl-S(O)2, lower-alkoxy-C(O), (lower-alkyl)NH—C(O), or (lower-alkyl)2N—C(O);
- R11, R12, R13, R14, R15, R16, R17 and R18 independently from each other are hydrogen, halogen, hydroxy, lower alkyl, lower-alkoxy, fluoro-lower-alkyl, fluoro-lower-alkoxy, hydroxy-lower-alkyl, aryl, COOH, C(O)O-lower-alkyl or cyano;
- and pharmaceutically acceptable salts and esters thereof.
9 more elements
Dependencies are inferred from the claim text.