Patent ID: 6071953
Filing Date: 2000-06-06
Classification: A61P,C07D,Y10S

Abstract:
A chroman derivative of formula I: ##STR27## or a physiologically tolerated salt thereof in which: R(1) and R(2)are, independently of one another, hydrogen, CF.sub.3, C.sub.2 F.sub.5, C.sub.3 F.sub.7, alkyl 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, sulfarnoyl or methylsulfonyl;orR(1) and R(2)together are an alkylene chain having 2, 3, 4, 5, 6, 7, 8, 9 or 10 carbon atoms;R(A) is hydroxyl, alkanoyloxy having 1, 2, 3, 4, 5 or 6 carbon atoms or alkylsulfonyloxy having 1, 2, 3, 4, 5 or 6 carbon atoms;R(B) is hydrogen;orR(A) and R(B)together are a bond;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) and R(9)together are an alkylene group having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;wherein one CH.sub.2 group in the C.sub.n H.sub.2n group is optionally replaced by --O--, --SO.sub.zero, 1 or 2 -- or --NR(10);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, CF.sub.3, C.sub.2 F.sub.5, C.sub.3 F.sub.7, pyridyl, thienyl, imidazolyl or phenyl,where pyridyl, thienyl, imidazolyl or phenyl are unsubstituted or substituted by 1 or 2 substituents selected from F, Cl, Br, I, CF.sub.3, methyl, methoxy, sulfamoyl, methylsulfonyl or methylsulfonylamino;r is zero, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 or 20;wherein one CH.sub.2 group in the C.sub.r H.sub.2r group is optionally replaced by --O--, --CH.dbd.CH--, --C.tbd.C--, --CO--, --CO--O--, --SO.sub.zero, 1 or 2 -- or --NR(10)--;R(5), R(6), R(7) and R(8)each independently represent hydrogen, F, Cl, Br, I, alkyl having 1, 2, 3, 4, 5 or 6 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 represent 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, CF.sub.3, C.sub.2 F.sub.5, C.sub.3 F.sub.7 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;s is zero, 1, 2, 3, 4, 5 or 6;Y is --S--, --SO--, --SO.sub.2--, --CO--, --SO.sub.2 --NR(10)--, --O--, --NR(10)-- or --CO--NR(10);but with the condition that two of the substituents R(5), R(6), R(7) and R(8) are not hydrogen.