The invention provides the compounds of formula (I) and pharmaceutically
acceptable derivatives thereof in which: R.sup.0 is halogen, C.sub.1-6
alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy substituted by one or more
fluorine atoms, or O(CH.sub.2).sub.n NR.sup.4 R.sup.5 ; R.sup.1 and
R.sup.2 are independently selected from H, C.sub.1-6 alkyl, C.sub.1-6
alkyl, substituted by one or more fluorine atoms, C.sub.1-6 alkoxy,
C.sub.1-6 hydroxyalkyl, SC.sub.1-6 alkyl, C(O)H, C(O)C.sub.1-6 alkyl,
C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxy substituted by one or more
fluorine atoms, O(CH.sub.2).sub.n CO.sub.2 C.sub.1-6 alkyl,
O(CH.sub.2).sub.n SC.sub.1-6 alkyl, (CH.sub.2).sub.n NR.sup.4 R.sup.5,
(CH.sub.2).sub.n SC.sub.1-6 alkyl or C(O)NR.sup.4 R.sup.5 ; with the
proviso that when R.sup.0 is at the 4-position and is halogen, at least
one of R.sup.1 and R.sup.2 is C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxy
substituted by one or more fluorine atoms, O(CH.sub.2).sub.n CO.sub.2
C.sub.1-6 alkyl, O(CH.sub.2).sub.n SC.sub.1-6 alkyl, (CH.sub.2).sub.n
NR.sup.4 R.sup.5 or (CH.sub.2).sub.n SC.sub.1-6 alkyl, C(O)NR.sup.4
R.sup.5 ; R.sup.3 is C.sub.1-6 alkyl or NH.sup.2 ; R.sup.4 and R.sup.5 are
independently selected from H, or C.sub.1-6 alkyl or, together with the
nitrogen atom to which they are attached, form a 4-8 membered saturated
ring; and n is 1-4. Compounds of formula (I) are potent and selective
inhibitors of COX-2 and are of use in the treatment of the pain, fever,
inflammation of a variety of conditions and diseases.
##STR1##
De uitvinding verstrekt de samenstellingen van formule (I) en farmaceutisch aanvaardbare derivaten daarvan waarin: R.sup.0 is halogeen, c.sub.1-6 alkyl, alkoxy c.sub.1-6, c.sub.1-6 alkoxy die door één of meerdere fluoratomen wordt gesubstitueerd, of O(CH.sub.2).sub.n NR.sup.4 R.sup.5; R.sup.1 en R.sup.2 worden onafhankelijk geselecteerd uit H, c.sub.1-6 alkyl, alkyl c.sub.1-6, die door één of meerdere fluoratomen wordt gesubstitueerd, alkoxy c.sub.1-6, hydroxyalkyl c.sub.1-6, sC.sub.1-6 alkyl, C(O)H, c(O)C.sub.1-6 alkyl, c.sub.1-6 alkylsulphonyl, c.sub.1-6 alkoxy gesubstitueerd door één of meerdere fluoratomen, O(CH.sub.2).sub.n CO.sub.2 c.sub.1-6 alkyl, alkyl O(CH.sub.2).sub.n sC.sub.1-6, (CH.sub.2).sub.n NR.sup.4 R.sup.5, (alkyl CH.sub.2).sub.n sC.sub.1-6 of C(O)NR.sup.4 R.sup.5; op voorwaarde dat wanneer R.sup.0 bij de 4-positie is en halogeen is, minstens één van R.sup.1 en R.sup.2 alkylsulphonyl c.sub.1-6 is, c.sub.1-6 alkoxy gesubstitueerd door één of meerdere fluoratomen, O(CH.sub.2).sub.n CO.sub.2 c.sub.1-6 alkyl, alkyl O(CH.sub.2).sub.n sC.sub.1-6, (CH.sub.2).sub.n NR.sup.4 R.sup.5 of H, of c.sub.1-6 alkyl of, samen met het stikstofatoom waaraan zij in bijlage zijn, vormt een membered verzadigde ring 4-8; en n is 1-4, Samenstellingen van formule (I) is machtige en selectieve inhibitors van Cox-2 en is van gebruik in de behandeling van de pijn, koorts, ontsteking van een verscheidenheid van voorwaarden en ziekten. ## STR1 ##