| US 7,468,369 B2 | ||
| Sulfonyl pyrrolidines, method for producing the same and their use as drugs | ||
| Stefanie Keil, Hofheim (Germany); Hans-Ludwig Schaefer, Hochheim (Germany); Maike Glien, Wiesbaden (Germany); Stefan Guessregen, Wiesbadan (Germany); Wolfgang Wendler, Selters (Germany); and Marion Schneider, Hofheim (Germany) | ||
| Assigned to Sanofi-Aventis, Paris (France) | ||
| Filed on Jun. 20, 2007, as Appl. No. 11/765,705. | ||
| Application 11/765705 is a continuation of application No. PCT/EP2005/013772, filed on Dec. 21, 2005. | ||
| Claims priority of application No. 10 2005 000 666 (DE), filed on Jan. 04, 2005. | ||
| Prior Publication US 2008/0045540 A1, Feb. 21, 2008 | ||
| Int. Cl. A61K 31/496 (2006.01); C07D 401/04 (2006.01); C07D 401/14 (2006.01); C07D 413/12 (2006.01); C07D 413/14 (2006.01); C07D 409/04 (2006.01); C07D 207/48 (2006.01) | ||
| U.S. Cl. 514—252.13 [514/253.07; 514/253.09; 514/254.03; 514/254.04; 544/363; 544/367; 544/372; 544/105] | 7 Claims |
1. A compound of the formula Ia:
 R1 is selected from (C1-C6)-alkyl, where one or more hydrogens in the alkyl radical may be replaced by fluorine; phenyl, (C1-C8)-alkylene-phenyl, heterocyclyl, (C1-C8)-alkylene-heterocyclyl, where the phenyl or heterocycle radical may be substituted one or more times by a substituent selected
from F, Cl, Br, NO2, COO—(C1-C6)-alkyl, (C1-C6)-alkylene-O—(C1-C6)-alkyl, OCF3, (C1-C6)-alkyl, CO—(C1-C6)-alkyl, phenyl, SCF3, and SF5;
and the heterocycle is selected from the group consisting of thiophene, quinoline, oxadiazole, isoxazole and pyridine and
may be fused to a benzene ring;
R2 is selected from phenyl and heterocycle, where the phenyl or heterocycle radical may be substituted one or more times by
a substituent selected from F, Cl, Br, NO2, COO—(C1-C6)-alkyl, (C1-C6)-alkylene-O—(C1-C6)-alkyl, OCF3, (C1-C6)-alkyl, CO—(C1-C6)-alkyl, phenyl, SCF3, and SF5 and the heterocycle is selected from the group consisting of dioxole, tetrahydrofuran, isoxazole, oxazine, thiophene and pyridine
and may be fused to a benzene ring; and
R3 and R4 are, independently of one another, selected from H, F, Cl, Br, NO2, COO—(C1-C6)-alkyl, (C1-C6)-alkylene-O—(C1-C6)-alkyl, OCF3, (C1-C6)-alkyl, CO—(C1-C6)-alkyl, phenyl, SCF3, and SF5;
where the compound of the following formula is excluded
 |