Patent Number: 6,169,096

Title: Farnesyl protein transferase inhibiting (imidazol-5-yl)methyl-2-quinolinone derivatives

Abstract: This invention comprises the novel compounds of formula (I) ##STR1## wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula --Alk.sup.1 --C(.dbd.O)--R.sup.9, --Alk.sup.1 --S(O)--R.sup.9 or --Alk.sup.1 --S(O).sub.2 --R.sup.9 ; R.sup.2, R.sup.3 and R.sup.16 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxyC.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono-or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy,Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C.sub.2-6 alkenyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, Ar.sup.1, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylS(O)C.sub.1-6 alkyl or C.sub.1-6 alkylS(O).sub.2 C.sub.1-6 alkyl; R.sup.6 and R.sup.7 each independently are hydrogen, halo, cyano, C.sub.1-6 alkyl, 4,4-dimethyl-oxazolyl, C.sub.1-6 alkyloxy or Ar.sup.2 oxy; R.sup.8 is hydrogen, C.sub.1-6 alkyl, cyano, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, C.sub.1-6 alkylcarbonylC.sub.1-6 alkyl, cyanoC.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonylC.sub.1-6 alkyl, carboxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, imidazolyl, haloC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, aminocarbonylC.sub.1-6 alkyl, or a radical of formula --O--R.sup.10, --S--R.sup.10, --N--R.sup.11 R.sup.12 ; R.sup.17 is hydrogen, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, Ar.sup.1 ; R.sup.18 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy or halo; R.sup.19 is hydrogen or C.sub.1-6 alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

Inventors: Venet; Marc Gaston (Le Mesnil Esnard, FR), Angibaud; Patrick Rene (Fontaine-Bellenger, FR), Muller; Philippe (Ande, FR), Sanz; Gerard Charles (Le Mesnil Esnard, FR)

Assignee: Janssen Pharmacaeutic N.V.

International Classification: C07D 405/14 (20060101); C07D 407/14 (20060101); C07D 405/00 (20060101); C07D 407/00 (20060101); C07D 521/00 (20060101); C07D 413/00 (20060101); C07D 401/14 (20060101); C07D 413/14 (20060101); C07D 401/00 (20060101); C07D 401/06 (20060101); A01N 043/42 ()

Expiration Date: 01/02/2018