BENZAZEPINE DICARBOXAMIDE COMPOUND Russian patent published in 2020 - IPC C07D403/12 C07D223/16 A61K31/55 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to benzazepine dicarboxamide compounds of formula I, where R¹ is C_1-7-alkyl, R² is selected from a group consisting of C_1-7-alkyl, hydroxy-C_1-7-alkyl, C_3-7-alkynyl, amino-C_1-7-alkoxy-C_1-7-alkyl, amino-C_1-7-alkoxy-C_1-7-alkoxy-C_1-7-alkyl, halogen-C_1-7-alkyl, C_3-7-cycloalkyl-C_1-7-alkyl and phenyl-C_1-7-alkyl, where phenyl is substituted with amino-C_1-7-alkyl; R³ is hydrogen; R⁴ is selected from a group consisting of: phenyl, where phenyl is unsubstituted or substituted with one or two groups selected from a group consisting of C_1-7-alkyl, halogen, halogen-C_1-7-alkyl, C_1-7-alkoxy, amino-C_1-7-alkyl, amino-C_1-7-alkoxy-C_1-7-alkoxy, amino-C_1-7-alkoxy-C_1-7-alkoxy-C_1-7-alkyl, C_1-7-alkylsulphonyl and pyrrolidinylcarbonyl or heteroaryl, where heteroaryl is 5- or 6-membered aromatic ring containing one, two or three heteroatoms selected from N, O or S, and is unsubstituted or substituted with one or two groups selected from the group consisting of C_1-7-alkyl, halogen, C_1-7-alkoxy, hydroxy-C_1-7-alkyl, amino-C_1-7-alkyl, C_1-7-alkyl-amino-C_1-7-alkyl, di-C_1-7-alkyl-amino-C_1-7-alkyl, amino-C_2-7-alkenyl, amino-C_2-7-alkynyl, benzyloxycarbonylamino-C_1-7-alkyl, amino-C_1-7-alkoxy, pyrrolidinylcarbonyl and phenyl-C_1-7-alkyl, where phenyl is unsubstituted or substituted with C_1-7-alkoxy or amino-C_1-7-alkyl. Invention also relates to a method for preparing said compounds and a pharmaceutical composition possessing TLR agonist activity based thereon.

EFFECT: technical result is obtaining novel compounds and a pharmaceutical composition based thereon, which can be used in medicine as drugs for treating diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, transplant rejection, graft versus host disease, immunodeficiencies and infectious diseases.

17 cl, 80 ex