| 摘要 |
This invention relates to novel benzazepine dicarboxamide compounds of the formula;wherein R1 to R4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases. |
| 主权项 |
1. A method of treating a disease selected from the group consisting of cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases, the method comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula I wherein R1 is C3-7-alkyl or C3-7-cycloalkyl; R2 is selected from the group consisting of C1-7-alkyl, hydroxy-C1-7-alkyl, C2-7-alkenyl, C3-7-alkinyl, amino-C1-7-alkoxy-C1-7-alkyl, amino-C1-7-alkoxy-C1-7-alkoxy-C1-7-alkyl, halogen-C1-7-alkyl, C3-7-cycloalkyl-C1-7-alkyl and phenyl-C1-7-alkyl, wherein phenyl is unsubstituted or substituted by amino-C1-7-alkyl; R3 is hydrogen; R4 is selected from the group consisting of
phenyl, said phenyl being unsubstituted or substituted by one or two groups selected from the group consisting of C1-7-alkyl, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, hydroxy-C1-7-alkyl, amino-C1-7-alkyl, C1-7-alkyl-amino-C1-7-alkyl, di-C1-7-alkyl-amino-C1-7-alkyl, amino-C2-7-alkenyl, C1-7-alkyl-amino-C2-7-alkenyl, di-C1-7-alkyl-amino-C2-7-alkenyl, amino-C2-7-alkinyl, C1-7-alkyl-amino-C2-7-alkinyl, di-C1-7-alkyl-amino-C2-7-alkinyl, benzyloxycarbonylamino-C1-7-alkyl, amino-C1-7-alkoxy, amino-C1-7-alkoxy-C1-7-alkoxy, amino-C1-7-alkoxy-C1-7-alkyl, amino-C1-7-alkoxy-C1-7-alkoxy-C1-7-alkyl, C1-7-alkylsulfonyl, heterocyclylcarbonyl and phenyl-C1-7-alkyl, wherein phenyl is unsubstituted or substituted by C1-7-alkoxy or amino-C1-7-alkyl, andheteroaryl, said heteroaryl being a 5- or 6-membered aromatic ring containing one, two or three heteroatoms selected from N, O or S and being unsubstituted or substituted by one or two groups selected from the group consisting of C1-7-alkyl, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, hydroxy-C1-7-alkyl, amino-C1-7-alkyl, C1-7-alkyl-amino-C1-7-alkyl, di-C1-7-alkyl-amino-C1-7-alkyl, amino-C2-7-alkenyl, C1-7-alkyl-amino-C2-7-alkenyl, di-C1-7-alkyl-amino-C2-7-alkenyl, amino-C2-7-alkinyl, C1-7-alkyl-amino-C2-7-alkinyl, di-C1-7-alkyl-amino-C2-7-alkinyl, benzyloxycarbonylamino-C1-7-alkyl, amino-C1-7-alkoxy, amino-C1-7-alkoxy-C1-7-alkoxy, amino-C1-7-alkoxy-C1-7-alkyl, amino-C1-7-alkoxy-C1-7-alkoxy-C1-7-alkyl, C1-7-alkylsulfonyl, heterocyclylcarbonyl and phenyl-C1-7-alkyl, wherein phenyl is unsubstituted or substituted by C1-7-alkoxy or amino-C1-7-alkyl, or a pharmaceutically acceptable salt thereof. |
