Patent RU-2764069-C1 (RU)
Title: Erbb/btk inhibitors
Inventor: LI ZHENGTAO
IPC: A61K31/505
Filed: 2019-01-28
Granted: 2022-01-13
Abstract: FIELD: pharmaceuticals. 
     SUBSTANCE: invention relates to a compound by the formula (I) or a pharmaceutically acceptable salt, ester, hydrate, solvate or stereoisomer thereof. In the formula (I): A 1  represents N or CR 8 , each from A 2 , A 3 , A 4  and A 5  independently represents N or CR 9 , wherein no more than one from A 2 , A 3 , A 4  and A 5  represents N, each from R 1  and R 2  independently represents hydrogen or a C 1-12 alkyl, possibly monosubstituted with an -NR a R b , C 1-12 alkyl, 3-10-membered saturated carbocyclyl or 3-6-membered saturated heterocyclyl containing one heteroatom selected from N and O, wherein each from the 3-10-membered saturated carbocyclyl and the 3-6-membered saturated heterocyclyl can be not substituted or be mono- or polysubstituted with a C 1-12 alkyl, wherein each from R a  and R b  is independently selected from hydrogen or a C 1-12  alkyl, possibly monosubstituted or independently polysubstituted with deuterium or tritium, or R a  and R b , taken together with the nitrogen atom whereto they are linked, form a 3-10-membered saturated heterocyclyl possibly monosubstituted with a C 1-12 alkyl, or R 1  and R 2 , taken together with the nitrogen atom whereto they are linked, form a 3-12-membered monocyclic or polycyclic ring, possibly containing one additional heteroatom selected from N and O, possibly monosubstituted or independently polysubstituted with a halogen, C 1-12 alkyl, -NR a R b  or a -C 1-12 alkyl-NR a R b  group, R 3  represents H, a C 1-12 alkyl or -C 1-12 alkyl-NR a R b , each from R 4  and R 5  independently represents a C 1-6 alkyl, possibly monosubstituted or independently polysubstituted with one or more than one deuterium, tritium or halogen, or R 4  and R 5 , taken together with the carbon atom whereto they are linked, form a 3-10-membered monocyclic ring, possibly containing one oxygen heteroatom O, possibly monosubstituted or independently polysubstituted with one or more than one deuterium or tritium, R 6  represents hydrogen, R 7  represents a C 1-12 alkyl, possibly mono- or polysubstituted with deuterium or tritium, R 8  represents hydrogen, deuterium, tritium, halogen, cyano, C 1-12 alkyl, C 1-12 alkoxyl possibly monosubstituted or independently polysubstituted with one or more than one deuterium, tritium or a halogen, R 9  is absent or represents hydrogen, deuterium or tritium, n equals 0, 1, 2, 3, or 4, each R independently represents halogen, a C 1-12 alkyl, 3-10-membered saturated carbocyclyl or 3-6-membered saturated or unsaturated heterocyclyl containing one hetero-atom N, wherein said heterocyclyl is condensed with a ring whereto it is linked, possibly monosubstituted or independently polysubstituted with one or more than one deuterium, tritium, halogen or a C 1-12 alkyl. Also proposed are a pharmaceutical composition and a method for treating a tyrosine kinase-associated disease. 
     EFFECT: proposed ErbB and BTK inhibiting compounds can effectively treat diseases associated with ErbB (in particular, mutant forms of ErbB) or BTK, including cancer. 
     
       
     
     25 cl, 9 tbl, 104 ex