主权项 |
1. A method of treating a disorder or a disease in a subject mediated by plasmakallikrein, wherein the method comprises administering to the subject a therapeutically effective amount of a compound of formula (I) in free form or in pharmaceutically acceptable salt form wherein R1 and R2 are each independently hydrogen or methyl; A is a 5- to 10-membered monocyclic or fused polycyclic aromatic ring system, which may contain 1, 2, 3, or 4 heteroatoms selected from N, O and S, wherein the ring system A is unsubstituted or substituted once, twice or three times by R3; wherein A is neither unsubstituted phenyl nor unsubstituted pyridinyl; each R3 is independently selected from halogen, C1-C4alkyl, C1-C4alkoxy, oxo, cyano, C1-C4halogenalkyl, NR4R5; or R3 is a 5- to 6-membered monocyclic ring system which may be aromatic, saturated or unsaturated non-aromatic and which may contain 1, 2, 3 or 4 heteroatoms selected from N, O and S, wherein the ring system R3 is attached to A via bond, C1-C2alkylene or SO2, wherein the ring system R3 is in turn optionally substituted with oxo; R4 and R5 are independently selected from hydrogen or C1-C4alkyl; B is selected from: wherein the bond marked with * is attached to the carboxamide group C is a 5- to 10-membered monocyclic or fused polycyclic aromatic ring system, which may contain 1, 2, 3, or 4 heteroatoms selected from N, O and S, wherein the ring system C is unsubstituted or substituted once, twice or three times by R6, each R6 is independently selected from halogen, C1-C4alkyl, C1-C4alkoxy, C1-C4halogenalkyl, amino, aminoC1-C4alkyl, cyano, C2-C4alkynyl; wherein C is neither a 2-aminopyridinyl nor a 6-aminopyridinyl residue. |