Sf5 derivatives as par1 inhibitors, production thereof, and use as medicaments

A compound of formula I

• or a stereoisomeric or tautomeric form thereof, or a physiologically compatible salt of any of them, where
• Ar is a fused benzene, pyridine, pyrimidine, pyridazine or pyrazine ring, where the fused ring is unsubstituted or mono-, di-, tri- or tetrasubstituted independently by —(C1-C6)-alkyl, —(C3-C6)-cycloalkyl, —O—(C1-C8)-alkyl, —O—(C3-C6)-cycloalkyl, —(C0-C4)-alkylene-C(O)—N(R11)-R12, —(C0-C4)-alkylene-C(O)—O—R11, —(C0-C4)-alkylene-C(O)—R11, —(C0-C4)-alkylene-N(R11)-R12, —(C0-C4)-alkylene-N(R11)-C(O)—R12, halogen, OH, —CN, —NO2, —SO2CH3, —SO2CF3, —SF5, —Si[—C1-C4)-alkyl]3, —(C1-C6)-alkylene-O—(C1-C6)-alkyl, —(C6-C14)-aryl, where aryl is unsubstituted or mono-, di- or trisubstituted independently by —O—(C1-C6)-alkyl, —(C1-C4)-alkyl, OH, —(C3-C6)-cycloalkyl or —O—(C3-C6)-cycloalkyl, —(C4-C15)-Het where Het is unsubstituted or mono-, di- or trisubstituted independently by —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl, or —O—(C1-C6)-alkylene-O—(C1-C6)-alkyl,
• where alkyl, alkylene and cycloalkyl are each unsubstituted or mono-, di- or trisubstituted independently by —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl, —(C6-C14)-aryl where aryl is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted independently by halogen, —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl,
• —(C4-C15)-Het where Het is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted independently by halogen, —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl, or
• —O—(C3-C6)-cycloalkyl,
• where all or some of the hydrogen atoms in alkyl, alkylene or cycloalkyl may be replaced by fluorine,
• Q1 is a hydrogen atom, —(C1-C6)-alkyl, —(C3-C6)-cycloalkyl, —OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl, where alkyl and cycloalkyl are each unsubstituted or mono-, di- or trisubstituted independently by
• —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl, where all or some of the hydrogen atoms in alkyl or cycloalkyl may be replaced by fluorine,
• Q2 and Q3 are the same or different and each independently a hydrogen atom, —(C1-C6)-alkyl or —(C3-C6)-cycloalkyl, where all or some of the hydrogen atoms in alkyl or cycloalkyl may be replaced by fluorine,
• R11 and R12 are each independently a hydrogen atom, —(C1-C6)-alkyl, —(C3-C6)-cycloalkyl, —(C0-C4)-alkylene-(C6-C14)-aryl, —(C0-C4)-alkylene-(C4-C15)-Het, —SO2CH3 or —SO2CF3,
• where all or some of the hydrogen atoms in alkyl, alkylene or cycloalkyl may be replaced by fluorine, or
• R11 and R12 in the “N(R11)-R12” and “N(R11)-C(O)—R12” fragments are a 5- to 8-membered ring which is formed together with the nitrogen atom “N” or the “N—C(O)” group to form cyclic amines, imides or lactams which contain up to 2 further heteroatoms from the group of N, O and S, where the ring is unsubstituted or mono- or disubstituted independently by —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl, where all or some of the hydrogen atoms in alkyl or cycloalkyl may be replaced by fluorine, R1, R2, R3, R4 and R5 are the same or different and are each independently a hydrogen atom, —(C1-C6)-alkyl, —(C3-C6)-cycloalkyl, OH, —CN, —NO2, —O—(C1-C6)-alkyl, —O—(C3-C6)-cycloalkyl,
• —(C0-C4)-alkylene-(CO)—N(R21)-R22, —SO2CH3, —SO2CF3,
• —(C0-C4)-alkylene-C(O)—O—R21, halogen, —SF5,
• —(C0-C4)-alkylene-C(O)—R21, —(C0-C4)-alkylene-N(R21)-R22,
• —(C0-C4)-alkylene-N(R21)-C(O)—R22, —(C1-C6)-alkylene-O—(C1-C6)-alkyl, —O—(C1-C6)-alkylene-O—(C1-C6)-alkyl, —(C6-C14)-aryl where aryl is unsubstituted or mono-, di- or trisubstituted independently by —O—(C1-C6)-alkyl, —(C1-C4)-alkyl, OH, —(C3-C6)-cycloalkyl or —O—(C3-C6)-cycloalkyl, —Si[(C1-C4)-alkyl]3 or —(C4-C15)-Het where Het is unsubstituted or mono-, di- or trisubstituted independently by —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl,
• where alkyl, alkylene and cycloalkyl are each unsubstituted or mono-, di- or trisubstituted independently by —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl, —(C6-C14)-aryl where aryl is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted independently by halogen, —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl,
• —(C4-C15)-Het where Het is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted independently by halogen, —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl, or
• —O—(C3-C6)-cycloalkyl,
• where all or some of the hydrogen atoms in alkyl, alkylene or cycloalkyl may be replaced by fluorine,
• with the proviso that at least one R1, R2, R3, R4 or R5 is —SF5,
• R9 is a hydrogen atom, —(C1-C6)-alkyl, —(C3-C6)-cycloalkyl, —(C0-C4)-alkylene-(C6-C14)-aryl where aryl is unsubstituted or mono-, di- or trisubstituted independently by —O—(C1-C6)-alkyl, —(C1-C4)-alkyl, OH, —(C3-C6)-cycloalkyl or —O—(C3-C6)-cycloalkyl,
• —(C0-C4)-alkylene-(C4-C15)-Het where Het is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted independently by halogen, —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl, and where all or some of the hydrogen atoms in alkyl, alkylene or cycloalkyl may be replaced by fluorine,
• R21 and R22 are each independently a hydrogen atom, —(C1-C6)-alkyl, —(C3-C6)-cycloalkyl, —(C0-C4)-alkylene-(C6-C14)-aryl, —(C0-C4)-alkylene-(C4-C15)-Het, —SO2CH3 or —SO2CF3,
• where some or all of the hydrogen atoms in alkyl, alkylene or cycloalkyl may be replaced by fluorine, or
• R21 and R22 in the “N(R21)-R22” and “N(R21)-C(O)—R22” fragments are a 5- to 8-membered ring which is formed together with the nitrogen atom “N” or the “N—C(O)” group to form cyclic amines, imides or lactams which contain up to two further heteroatoms from the group of N, O and S, where the ring is unsubstituted or mono- or disubstituted independently by —(C1-C4)-alkyl, —(C3-C6)-cycloalkyl, OH, —O—(C1-C6)-alkyl or —O—(C3-C6)-cycloalkyl, where some or all of the hydrogen atoms in alkyl or cycloalkyl may be replaced by fluorine.