abstract |
1. Use of a compound of the formulan nin which:n one of R 1 and R 2 is R 3 -X and the other is hydrogen, nitro, cyano, trifluoromethyl,ncarbo(lower)alkoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, lower alkyl,nalkylamino, lower alkoxy, halo, HF 2 CO, F 3 CO or R 3 -X-; R 3 is monocycloalkyl, bicycloalkyl or benzocycloalkyl of up to 18 carbon atoms,ntetrahydropyran or tetrahydrofuran; X is a carbon-carbon bond, -CH 2 -, -O- or -N=; R 5 is (i) o-phenylene, unsubstituted or substituted with 1 or more substituents eachnselected independently from nitro, cyano, halo, trifluoromethyl, carbo(lower)alkoxy,nacetyl, or carbamoyl, unsubstituted or substituted with lower alkyl, acetoxy, carboxy,nhydroxy, amino, lower alkylamino, lower acylamino, aminoalkyl, or lower alkoxy; (ii)nthe vicinally divalent residue of pyridine, pyrrolidine, imidizole, naphthalene, ornthiophene, wherein the divalent bonds are on vicinal ring carbon atoms; (iii) a vicinallyndivalent cycloalkyl or cycloalkenyl of 4-10 carbon atoms, unsubstituted or substitutednwith one or more substituents each selected independently from the group consisting ofnnitro, cyano, halo, trifluoromethyl, carbo(lower)alkoxy, acetyl, carbamoyl, acetoxy,ncarboxy, hydroxy, amino, lower alkylamino, lower alkyl, lower alkoxy, or phenyl; (iv)nvinylene di-substituted with lower alkyl; or (v) ethylene, unsubstituted ornmonosubstituted or disubstituted with lower alkyl; R 6 is -CO-, -CH 2 - or -CH 2 CO-; Y is -COZ, -CN, -OR 8 , lower alkyl or aryl, Z is -NH 2 , -OH, -NHR, -R 9 , or -OR 9 ; R 8 is hydrogen or lower alkyl; R 9 is lower alkyl or benzyl, and n has a value of 0, 1, 2, or 3, nwherein the term "lower" denotes from 1 to 6 carbon atoms,nfor the manufacture of a medicament for treating cancer. |