TYK2 INHIBITORS AND THEIR USE Russian patent published in 2024 - IPC C07D401/12 C07D403/14 C07D213/74 C07D401/04 C07D401/14 C07D405/14 C07D413/14 C07D471/04 C07D471/10 C07D487/04 C07D498/04 A61K31/4439 A61K31/444 A61K31/501 A61P11/00 A61P25/00 A61P35/00 

Abstract RU 2813233 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (XII), where:

represents ring B is selected from the group consisting of phenyl and pyridyl; R16 is -C(=O)R11; R3 represents hydrogen; R4 represents -ORb; L represents bond; ring A is a 5-membered heteroaryl containing three nitrogen atoms, where ring A may be optionally replaced by one RA; RA is selected from the group consisting of C1-C6alkyl and C1-C6 deuteroalkyl; R5 is selected from the group consisting of -NR9R10, -NR8S(=O)R7, NR8C (=O) NR9R10, NR8C(=O)R7 and 4–5-membered heterocycloalkyl containing two nitrogen atoms; where heterocycloalkyl is substituted with two substituents, each of which is independently selected from the group consisting of oxo and C1-C6alkyl; R7 is selected from the group consisting of C1-C6alkyl and C3-cycloalkyl; R8 represents hydrogen; R9 and R10 are independently selected from the group consisting of hydrogen, C1-C6alkyl and 5–6-membered heteroaryl containing one or two nitrogen atoms; wherein the heteroaryl is optionally substituted with one or two substituents, each independently selected from the group consisting of oxo, halogen, -CN, C1-C6alkyl and morpholinyl; or R9 and R10 together with the nitrogen atom to which they are attached form a 4-membered heterocycloalkyl containing one nitrogen atom optionally substituted by two substituents selected from C1-C6alkyl; R11 is selected from the group consisting of C1-C6alkyl, C1-C6deuteroalkyl and C3-cycloalkyl; wherein each alkyl and cycloalkyl is optionally substituted with one R11a; R11a is selected from halogen; Rb is selected from C1-C6alkyl. The invention also relates to specific compounds and a pharmaceutical composition based on these compounds and the compound of formula (XII).

EFFECT: obtaining new compounds and a pharmaceutical composition based on them which can be used in medicine in the treatment and prevention of cancer.

12 cl, 10 tbl, 203 ex

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RU 2 813 233 C2

Authors

Jin, Bohan

Dong, Qing

Hung, Gene

Kaldor, Stephen W.

Dates

2024-02-08Published

2019-10-22Filed