	US 7,544,700 B2
	Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein JunKinases
Serge Halazy, Vetraz-Monthoux (France); Dennis Church, Commugny (Switzerland); Stephen J. Arkinstall, Belmont, Mass. (US); Marco Biamonte, San Diego, Calif. (US); Montserrat Camps, Versoix (Switzerland); Jean-Pierre Gotteland, Beaumont (France); and Thomas Rueckle, Plan-les-Ouates (Switzerland)
Assigned to Laboratoires Serono SA, Coinsins (Switzerland)
Appl. No. 10/381,665 PCT Filed Sep. 27, 2001, PCT No. PCT/IB01/01772 § 371(c)(1), (2), (4) Date Oct. 10, 2003, PCT Pub. No. WO02/26733, PCT Pub. Date Apr. 04, 2002.
Claims priority of application No. 00810887 (EP), filed on Sep. 27, 2000.
Prior Publication US 2004/0077854 A1, Apr. 22, 2004
This patent is subject to a terminal disclaimer.
Int. Cl. A61P 25/00 (2006.01); A61P 25/16 (2006.01); A61K 31/4535 (2006.01); A61K 31/55 (2006.01); A61K 31/4025 (2006.01); C07D 333/34 (2006.01); C07D 409/12 (2006.01); C07D 409/14 (2006.01); C07D 413/14 (2006.01)

U.S. Cl. 514—322 [514/323; 514/326; 546/199; 546/201; 546/212]

21 Claims

1. A sulfonamide according to formula I:

wherein

Ar¹and Ar²are independently from each other aryl or heteroaryl,

X is O or S;

R¹is hydrogen or a C₁-C₆-alkyl group, or R¹forms a 5-6-membered saturated or unsaturated ring with Ar¹;

n is an integer from 0 to 5;

Y is piperidine substituted with —NR^3′R³, wherein R^3′ and R³are selected from the group consisting of hydrogen, C₄-C₁₈alkyl, aryl-C₁-C₁₈-alkyl, heteroaryl-C₂-C₁₈-alkyl, C₁-C₁₄alkyl substituted with C₃-C₁₂cyclo-, bicyclo-, or tricyclo-alkyl, wherein said alkyl chains may contain 1-3 oxygen or sulfur atoms; and wherein at least one of R³′ or R³is not hydrogen;

where Y forms a bond with the sulfonyl group in formula I;

wherein said sulfonamide includes its geometrical isomers, in an optically active form as enantiomers, diastereomers, as well as in the form of racemates, as well as pharmaceutically acceptable salts thereof.