PYRIDINONE AND PYRIDAZINONE DERIVATIVES Russian patent published in 2017 - IPC C07D213/64 C07D237/14 C07D401/04 C07D401/10 C07D401/12 C07D401/14 C07D403/04 C07D403/10 C07D403/12 C07D405/04 C07D405/12 C07D413/10 C07D417/04 A61K31/435 A61K31/50 A61K31/501 A61K31/5377 A61P35/00 

Abstract RU 2632915 C2

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of formula (I) or its pharmaceutically acceptable salts: , wherein J is a group of formula IIa, R1a is C1-C3alkyl; Y1a is N or CRxa, where Rxa is H, X2a is selected from the group consisting of: H, C1-C4alkyl; X1a is selected from the group consisting of: hydrogen, halogen, C1-C6alkyl, C1-C4haloalkyl,-O-C1-C4alkyl, -O-C1-C3alkylene-C3-C7cycloalkyl, -O-C1-C4haloalkyl, -O-C1-C3alkylene(5-membered heterocycloalkyl having 1 heteroatom selected from O), -O-C1-C6alkylene-N(R10)2, -O-C1-C3alkylene-C(O)OC1-C4alkyl, -C2-C4alkenylene-C(O)-O-C1-C4alkyl, -C(O)-C1-C4alkyl, C(O)O-C1-C4alkyl, C(O)NR10R12, -NR10-C1-C3alkylene-C(O)-C1-C4alkyl, -SO2NR10R12 and any of the groups: ii) 6-membered heterocycloalkenyl, which may be substituted with 1 R2; iii) 5-6 membered heterocycloalkyl with 1 to 2 heteroatoms selected from N, which may be substituted with 1-2 R3; iv) 5-6 membered heteroaryl with 1-3 heteroatoms independently selected from N, O, 9-10 membered bicyclic heteroaryl with 1 to 3 heteroatoms independently selected from N, S, which may be substituted with 1-2 R4; v) phenyl which may be substituted with 1-2 R6; X3 is LG where L is absent or is selected from the group consisting of: -O-, -O-C1-C3alkylene; and G is selected from the group consisting of: phenyl, 6-membered heteroaryl with 1 heteroatom selected from N, 9-membered bicyclic heteroaryl with 2 heteroatoms, selected from N, C3-C7cycloalkyl, 6-membered heterocycloalkyl with 1 heteroatom selected from N, O, where G may be substituted with 1-2 groups, A2 is CR18, and A1, A3 and A4 are CR19, values of the remaining substituents are indicated in the claims. The invention also relates to individual compounds, to a pharmaceutical composition and to a method for cancer treatment.

EFFECT: new compounds with proliferative activity are obtained.

20 cl, 6 tbl, 293 ex

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RU 2 632 915 C2

Authors

Khabbard Robert Dejl

Makdeniel Kit F.

Park Chang Khoon

Pratt Dzhon K.

Soltvedel Todd

Sun Chaokhun

Van Le

Uendt Majkl D.

Dates

2017-10-11Published

2012-06-12Filed