Five-membered heterocycles having biphenylsulfonyl substitution, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them

A method for the treatment of an illness in which cell proliferation is a primary or secondary cause, which comprises administering to a host in need of such treatment an effective amount of at least one compound of the formula I:

• or a physiologically tolerable salt thereof,
• in which the symbols have the following meaning:
• R1 is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or —CaH2a-phenyl,
• said —CaH2a-phenyl being unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, methyl, methoxy, hydroxyl and NR(8)R(9);
• R(8) and R(9)
• independently of one another are H or (C1-C4)alkyl;
• a is zero, 1 or 2;
• or
• R1 is —CbH2b-(C1-C9)heteroaryl,
• which is unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, CH3, methoxy, hydroxyl and NR(10)R(11);
• R(10) and R(1)
• independently of one another are H or (C1-C4)alkyl;
• b is zero, 1 or 2;
• or
• R1 is —CdH2d-(C3-C7)cycloalkyl;
• d is zero, 1 or 2;
• R2 and R3
• independently of one another are hydrogen, F, Cl, Br, I, CF3, —C≡N, —NO2, CH2OR17, CO-R6 or O-R7;
• R17 is hydrogen or alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;
• R6 is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, OR30 or phenyl,
• said phenyl being unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, methyl, methoxy, hydroxyl and NR(31)R(32);
• R(31) and R(32) independently of one another are H or (C1-C4)-alkyl;
• R30 is hydrogen or alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;
• R7 is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, phenyl,
• said phenyl being unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, methyl, methoxy, hydroxyl and NR(12)R(13);
• R(12) and R(13)
• independently of one another are H or (C1-C4)-alkyl;
• or
• R7 is (C1-C9)heteroaryl,
• which is unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, CH3, methoxy, hydroxyl and NR(14)R(15);
• R(14) and R(15)
• independently of one another are H or (C1-C4)-alkyl;
• or
• R2 and R3
• independently of one another are alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms or —CgH2g-phenyl,
• said —CgH2g-phenyl being unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, methyl, methoxy, hydroxyl and NR(18)R(19);
• R(18) and R(19)
• independently of one another are H or (C1-C4)alkyl;
• g is zero, 1 or 2;
• or
• R2 and R3
• independently of one another are —C1H21-(C1-C9)heteroaryl,
• which is unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, CH3, methoxy, hydroxyl and NR(20)R(21);
• R(20) and R(21)
• independently of one another are H or (C1-C4)-alkyl;
• I is zero, 1 or 2;
• or
• R2 and R3
• independently of one another are SOn-R22;
• n is zero, 1 or 2;
• R22 is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms or —CsH2s-phenyl,
• said -CsH2s-phenyl being unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, methyl, methoxy, hydroxyl and NR(34)R(35);
• R(34) and R(35)
• independently of one another are H or (C1-C4)-alkyl;
• s is zero, 1 or 2;
• R4 and R5
• independently of one another are hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, F, Cl, Br, I, CF3, —C≡N, —NO2, SOp-R16, CO-R23 or O-R24;
• p is zero, 1 or 2;
• R16 is alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or phenyl,
• said phenyl being unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, methyl, methoxy, hydroxyl and NR(26)R(27);
• R(26) and R(27)
• independently of one another are H or (C1-C4)-alkyl;
• R23 is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or OR25;
• R25 is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms;
• R24 is hydrogen, alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms or phenyl,
• said phenyl being unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, I, CF3, methyl, methoxy, hydroxyl and NR(28)R(29);
• R(28) and R(29)
• independently of one another are H or (C1-C4)-alkyl.