Forbindelser med medisinske effekter grunnet interaksjonen med glukokortikoidreseptor

• Main Authors: HO KOC-KAN, HAMILTON NIALL MORTON, KULTGEN STEVEN G, OHLMEYER MICHAEL, KINGSBURY CELIA, LITTLEWOOD PETER THOMAS ALBERT, KICZUN MICHAEL JOHN, SHERBORNE BRAD, MORPHY JOHN RICHARD, BROWN ANGUS RICHARD, GROVE SIMON JAMES ANTHONY
• Format: Patent
• Language: Norwegian
• Published: 08.09.2008
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

Oppfinnelsen tilveiebringer forbindelser som har strukturen i henhold til formelen I Formel I hvor: X er et karbon eller nitrogenatom; Ar er fenyl eller heteroaromatisk ring; R1 er hydrogen, halogen, CN eller (1C-4C)alkyl; R2 er hydrogen, halogen eller eventuelt fluorert (1C-3C)alkoksy; R3 og R5 er uavhengig hydrogen, eventuelt halogenert (1C-4C)alkyl, eventuelt halogenert (1C-4C)alkoksy, eventuelt halogenert aryl(1C-4C)alkoksy, eventuelt halogenert (1C-4C)alkenyl eller hydroksylmetyl; R4 er hydrogen, halogen, eventuelt halogenert (1C-4C)alkoksy eller eventuelt halogenert aryl(1C-4C)alkoksy; R6 er hydrogen, benzyl, eventuelt substituert med ett eller flere halogenatomer eller (1C-4C)alkyl eller R6 er eventuelt halogenert (1C-4C)alkyl; hver R7 er uavhengig hydrogen, halogen, eventuelt halogenert (1C-4C)alkyl eller eventuelt halogenert (1C-4C)alkoksy og farmasøytisk egnede syreaddisjonssalter derav for anvendelse som glukokortikoid reseptor-modulatorer, spesielt for behandling av sentralnervesystemlidelser. The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R1 is hydrogen, halogen, CN or (1C-4C)alkyl; R2 is hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; R3 and R5 are independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; R4 is hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; R6 is hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or R6 is optionally halogenated (1C-4C)alkyl; each R7 independently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.