2-AMINOPYRIDO[4,3-D]PYRIMIDIN-5-ONE DERIVATIVES AND THEIR USE AS WEE-1 INHIBITORS Russian patent published in 2018 - IPC C07D471/04 A61K31/519 A61P35/00 

Abstract RU 2656342 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof possessing the properties of kinase activity inhibitors Wee-1. In formula

R1 means a group represented by formula (a) or (h)

where each of the substituents R1a and R1b is independently selected from the group consisting of a hydrogen atom, a halogen atom; R2 is a hydrogen atom, C1-C4alkyl group, a halogen atom, an N-(mono- or di-C1-C4alkyl)amide group, C2-C3alkynyl group substituted by a hydroxy or amino group or a pyridyl group; R3 is a group represented by formula where Z is a nitrogen atom or an optionally substituted methine group; R3a is a hydrogen atom, a halogen atom, or a 6-membered nitrogen containing heterocyclyl group with one or two heteroatoms in the ring selected from nitrogen, oxygen, sulfur or a dioxide thereof selected from piperidine, piperazine, morpholine, thiomorpholine or dioxide thereof, optionally substituted with one or more substituents selected from the group consisting of a hydrogen atom or a C1-C6alkyl group, or in the case of piperidine or piperazine, optionally substituted on the ring nitrogen by substituent R4e, which includes a hydrogen atom, C1-C6alkyl group, optionally substituted with a hydroxyl group, an amino group, a (mono- or diC1 -C4alkyl) amino group, an oxogroup and a hydroxyl group, id est, for example, a CH2-COOH group, a C1-C3alkanoyl group (id est, C1-C3alkylC(= O)) and group -Q1-N(R4c)R4d, wherein Q1 is a single bond, a C1-C3alkyl group; R3b is a hydrogen atom, a halogen atom, an unsubstituted C1-C6alkyl group or a C1-C6alkyl group, substituted with hydroxy, amino, N-(mono- or di-C1-C4alkyl) amino, unsubstituted C1-C6alkoxy group or a C1-C6alkoxy group substituted with an N- (mono- or di-C1-C4-alkyl) amino group; R4c and R4d are each independently a hydrogen atom or a C1-C6alkyl group; and Q1 is a single bond or a C1-C3alkyl group.

EFFECT: compounds can be used in the treatment or prevention of cancer mediated by Wee-1 kinase.

14 cl, 2 tbl, 33 ex

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RU 2 656 342 C2

Authors

O'Doud Kolin Roderik

Rauntri Dzhejms Semyuel Shejn

Burkamp Frenk

Uilkinson Endryu Dzhon

Dates

2018-06-05Published

2014-04-11Filed