PHARMACEUTICALLY ACTIVE SULPONAMIDE DERIVATIVES

• Main Authors: CHURCH DENNIS, HALAZY SERGE, ARKINSTALL STEPHEN, BIAMONTE MARCO, CAMPS MONTSERRAT, GOTTELAND JEAN-PIERRE, RUECKLE THOMAS
• Format: Patent
• Language: Bulgarian; English
• Published: 31.12.2009
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Сулфонамидните производни имат формула@@Изобретението се отнася също до приложението им като фармацевтично активни съединения, до фармацевтични състави, съдържащи тези сулфонамидни производни, и до методи за получаването им. Те са мощни модулатори на проводящия път на JNK (Jun-киназа) и са изключително ефективни и селективни инхибитори на JNK2 и 3. Във формулата Ar1 и Ar2 независимо един от друг означават заместен или незаместен арил или хетероарил, Х е О или S, за предпочитане О The present invention is related to sulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula I according to the present invention being suitable pharmaceutical agents are those wherein Ar and Ar are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R is hydrogen or a C1-C6-alkyl group, preferably H, or R forms a substituted or unsubstituted 5-6-membered saturated or non-saturated ring with Ar ; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1. Y within formula I is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula I thus providing the sulfonamide.