YU21595A

YU21595A - Substituted morpholine derivatives, pharmaceutical compositions containing them and methods for their obtaining

Info

Publication number: YU21595A
Application number: YU21595A
Authority: YU
Inventors: Raymond Baker; Timothy Harrison; Angus Murray Masleod; Andrew Pate Owens; Eillen Mary Seward; Christopher John Swain; Richard Martin Teall
Original assignee: Merck Sharp & Dohme Limited
Priority date: 1994-04-12
Filing date: 1995-04-05
Publication date: 1999-03-04
Also published as: CO4370100A1

Abstract

Ovaj pronalazak se odnosi na jedinjenja formule (I): gde je R1 vodonik, halogen, C1-6 alkil, C1-6 alkoksi, CF3, NO2, CN, SRa, SORa, SO2Ra, CO2Ra, CONRaRb, C2-6 alkenil, C2-6 alkinil ili C1-4 alkil supstituisan sa C1-4 alkoksi, gde su Ra i Rb vodonik ili C1-4 alkil; R2 je vodonik, halogen, C1-6 alkil, C1-6 alkoksi supstituisan sa C1-4 alkoksi ili CF3; R3 je vodonik, halogen ili CF3; R4 je odabrano iz definicija za R1; R5 je odabrano iz definicija za R2; R6 je 5-to člani ili 6-to člani heterociklični prsten koji sadrži 2 ili 3 atoma azota opciono supstituisan sa =O, =S ili C1-4 alkil grupa, i opiciono supstituisan sa aminoalkil grupom;: R9a i R9b su vodonik ili C1-4 alkil, ili R9a i R9b su spojeni tako da obrazuju C5-7 prsten; X je C1-4 alkilen opciono supstituisan sa okso; i Y je C1-4 alkil grupa opciono supstituisana sa hidroksilom; pod uslovom da ako je Y C1-4 alkil, R6 je supstituisan bar sa aminoalkil grupom;i njihove faramceutski prihvatljive soli i njihovi pro-lekovi. Jedinjenja su od posebne koristi u tretiranju bola, inflamacije, migrene i povraćanja.The present invention relates to compounds of formula (I): wherein R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, CF3, NO2, CN, SRa, SORa, SO2Ra, CO2Ra, CONRaRb, C2-6 alkenyl, C2 -6 alkynyl or C1-4 alkyl substituted with C1-4 alkoxy, wherein Ra and Rb are hydrogen or C1-4 alkyl; R2 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy substituted with C1-4 alkoxy or CF3; R3 is hydrogen, halogen or CF3; R4 is selected from the definitions for R1; R5 is selected from the definitions for R2; R 6 is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by a = O, = S or C 1-4 alkyl group, and optionally substituted by an aminoalkyl group; R9a and R9b are hydrogen or C1 -4alkyl, or R9a and R9b are joined to form a C5-7 ring; X is C1-4 alkylene optionally substituted by oxo; and Y is a C1-4 alkyl group optionally substituted by hydroxyl; provided that if Y is C1-4 alkyl, R6 is substituted at least with an aminoalkyl group; and their pharmaceutically acceptable salts and their prodrugs. The compounds are of particular benefit in the treatment of pain, inflammation, migraines and vomiting.