Patent ID: 6191164
Filing Date: 2001-02-20
Classification: A61K

Abstract:
A chroman of formula I: ##STR254##wherein:R(1) and R(2) each independently of one another is hydrogen C.sub.p F.sub.2p+1, having 1, 2, 3, 4, 5 or 6 carbon atoms, or phenyl, which is unsubstituted or substituted by 1 or 2 substituents selected from F, Cl, Br, I, --CF.sub.3, methyl, methoxy, sulfamoyl, methylsulfonylamino or methylsulfonyl;p is 1, 2, or 3; orR(1) and R(2) together are an alkylene chain having 2, 3, 4, 5, 6, 7, 8, 9, or 10 carbon atoms;R(3) is R(9)--C.sub.n H.sub.2n [NR(11)].sub.m --;R(9) is hydrogen or cycloalkyl having 3, 4, 5, 6, 7, or 8 carbon atoms;n is zero, 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10;m is zero or 1;R(11) is hydrogen or alkyl having 1, 2, 3, 4, 5, or 6 carbon atoms; orR(11), together with R(9), is an alkylene group having 1, 2, 3, 4, 5, 6, 7, or 8 carbon atoms;where one CH.sub.2 group of the group C.sub.n H.sub.2n is optionally replaced by --O--, --SO.sub.q --, or --NR(10)--;q is zero, 1, or 2;R(10) is hydrogen, methyl, or ethyl;R(4) is R(12)--C.sub.r H.sub.2r --;R(12) is hydrogen, cycloalkyl having 3, 4, 5, 6, 7, or 8 carbon atoms, piperidyl, 1-pyrrolidinyl, N-morpholino, N-methylpiperazino, --C.sub.p F.sub.2p+1 pyridyl, thienyl, imidazolyl, or phenyl, which is unsubstituted or substituted by 1 or 2 substituents selected from F, Cl, Br, I, --CF.sub.3 m methyl, methoxy, sulfamoyl, methylsulfonyl or methylsulfonylamino;r is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16 ,17, 18, 19, or 20;where once CH.sub.2 group of the group C.sub.2 H.sub.2r can be replaced by --O--, --C.dbd.C--, --C.tbd.C--, --CO--, --CO--O--, --SO.sub.q -- or --NR(10)--;q is zero, 1 or 2;R(10) is hydrogen, methyl, or ethyl;R(5), R(6), R(7), and R(8) each independently of one another is hydrogen, F, Cl, Br, I, alkyl having 1, 2, 3, or 4 carbon atoms, cycloalkyl having 3, 4, 5, 6, 7, or 8 carbon atoms, --CN, --CF.sub.3, --C.sub.2 F.sub.5, --C.sub.3 F.sub.7, --N.sub.3, --NO.sub.2, --CONR(13)R(14), --COOR(15), R(16)--C.sub.s H.sub.2s --Y--, or phenyl, which is unsubstituted or substituted by 1 or 2 substituents selected from F, Cl, Br, I, --CF.sub.3, methyl, methoxy, sulfamoyl or methylsulfonyl;R(13) and R(14) each independently of one another is hydrogen or alkyl having 1, 2 or 3 carbon atoms;R(15) is hydrogen, methyl, ethyl, phenyl, or --C.sub.u H.sub.2u --NR(13)R(14);u is 2 or 3;R(16) is hydrogen, cycloalkyl having 3, 4, 5, 6, 7, or 8 carbon atoms, --COOR(15), thienyl, imidazolyl, pyridyl, quinolyl, isoquinolyl, piperidyl, 1-pyrrolidinyl, N-morpholino, N-methylpiperazino, --C.sub.t F.sub.2t+1, or phenyl, which is unsubstituted or substituted by 1 or 2 substituents selected from F, Cl, Br, I, --CH.sub.3, methyl, methoxy, sulfamoyl or methylsulfonyl;s is zero, 1, 2, 3, 4, 5 or 6;t is 1, 2 or 3;Y is --SO.sub.q --, --CO--, --SO.sub.2 --NR(10)--, --O--, NR(10)--, or --CO--NR(10);wherein R(6) is other than --OCF.sub.3 or --OC.sub.2 F.sub.5 ; or a physiologically tolerable salt thereof.