DIHYDROPYRIMIDINE COMPOUNDS AND THEIR APPLICATION IN PHARMACEUTICALS Russian patent published in 2019 - IPC C07D417/14 C07D417/06 C07D405/14 A61K31/506 A61K31/541 A61P35/00 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to new dihydropyrimidine derivatives of formula (I) or (Ia) possessing the properties of hepatitis virus inhibitor (HBV). In formula (I) or (Ia) , R¹ is phenyl; R³ is thiazolyl or 1-methyl-1H-imidazolyl; A is -O-; R² independently is hydrogen, methyl or ethyl, wherein each thiazolyl and 1-methyl-1H-imidazolyl described in R³, phenyl, described in R¹, and methyl or ethyl, described in R², is optionally and independently substituted with one or more substituents independently selected from hydrogen, C_1-4 alkyl, fluorine, chlorine or bromine; R is where Y is -(CR⁸R^8a)_k-S(=O)_q- or -(CR⁷R⁶)_n-; Q is -(CR^8tR^8a)_k-; every R⁷ independently is hydrogen, C_1-4 alkyl or F; every R⁶ independently is F or C_1-4 alkyl; every R⁸ and R^8a independently is hydrogen or C_1-4 alkyl; every R⁹ is independently -(CR¹⁰R^10a)_t-OH, -(CR¹⁰R^10a)_m-C(=O)O-R¹¹, -(CR¹⁰R^10a)_k-C(=O)O-(CR¹⁰R^10a)_k-OC(=O)OR¹¹, -C(=O)OR^11a or - (CR¹⁰R^10a)_k-C(=O)N(R¹¹)₂; every R¹⁰ and R^10a independently is hydrogen, halogen or C_1-4 alkyl, or R¹⁰ and R^10a together with the carbon atom to which they are attached form C_3-6 cycloalkyl or -C(=O)-; every R¹¹ independently is hydrogen, C_1-6 alkyl, C_1-6 alkoxy, C_1-6 alkyl-S(=O)_q-, C_1-9 heteroaryl, C_3-6 cycloalkyl-S(=O)_q- or C_6-10 aryl-S(=O)_q-; and R^11a is C_1-6 alkyl; each n is independently 1, 2 or 3; each t and m are independently 1, 2, 3, or 4; each q is independently 1 or 2 and each k is independently 0, 1, 2, 3 or 4.

EFFECT: compound can be used to manufacture a drug suitable for preventing, controlling, treating or reducing a disease caused by the hepatitis B virus, for example, cirrhosis or hepatocellular carcinoma.

13 cl, 3 tbl, 46 ex