Back to results
US 2012/0232104 A1Published application
Novel sulfonamides as l-cpt1 inhibitors
OwnerKonrad Bleicher, Simona Maria Ceccarelli +4inventors
InventorsKonrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
Life of this patent
Estimating the term…
Abstract
The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 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.
Claims29
A compound of formula (I):
- wherein
- A is —C(O)OR1 or selected from the group consisting of tetrazol-5-yl, 5-thioxo-4,5-dihydro-[1,2,4]oxadiazol-3-yl, 2-oxo-2,3-dihydro-[1,2,3,5]oxathiadiazol-4-yl and 5-oxo-4,5-dihydro-[1,2,4]oxadiazol-3-yl;
- X is —N(R5)C(O)— or —C(O)N(R5)—;
- V is N or C(R6);
- Y2 is N or C(R7);
- Y3 is N or C(H);
- Y4 is N or C(R8);
- Z1 is N or C(R9);
- R1 is hydrogen or lower-alkyl;
- R2 is hydrogen, halogen, hydroxy, cyano, lower-alkyl, fluoro-lower-alkyl, lower-alkoxy, fluoro-lower-alkoxy;
- NH2, N(H,lower-alkyl), N(lower-alkyl)2, or lower-alkyl-C(O)—O—, wherein lower-alkyl is optionally substituted with hydroxy, halogen, NH2, N(H,lower-alkyl), N(lower-alkyl)2 or lower-alkoxy;
- R3 is hydrogen, lower-alkyl or lower-alkoxy-lower-alkyl;
- R4 is aryl or heteroaryl, which aryl or heteroaryl is optionally substituted with 1 to 3 substituents independently selected from the group consisting of halogen, 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 or 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) or heteroaryl which is optionally substituted with lower-alkyl, halogen, thio-lower-alkoxy, or fluoro-lower-alkyl,
- wherein lower-alkyl is optionally substituted with hydroxy, NH2, N(H,lower-alkyl) or N(lower-alkyl)2;
- R5 is hydrogen, lower-alkyl or lower-alkoxy-lower-alkyl;
- R6, R7 and R8 independently from each other are selected from the group consisting of hydrogen, halogen, hydroxy, cyano, lower-alkyl, fluoro-lower-alkyl, lower-alkoxy, fluoro-lower-alkoxy;
- NH2, N(H,lower-alkyl), N(lower-alkyl)2, or lower-alkyl-C(O)—O—, wherein lower-alkyl is optionally substituted with hydroxy, halogen, NH2, N(H,lower-alkyl), N(lower-alkyl)2 and lower-alkoxy;
- R9 is hydrogen, halogen, hydroxy, cyano, lower-alkyl, fluoro-lower-alkyl, lower-alkoxy, fluoro-lower-alkoxy;
- NH2, N(H,lower-alkyl), N(lower-alkyl)2, or lower-alkyl-C(O)—O—, wherein lower-alkyl is optionally substituted with hydroxy, halogen, NH2, N(H,lower-alkyl), N(lower-alkyl)2 or lower-alkoxy;
- and pharmaceutically acceptable salts and esters thereof.
17 more elements
Dependencies are inferred from the claim text.