ANNELATED ASAHETEROCYCLES INCLUDING PYRIMIDINE FRAGMENT, METHOD OF PRODUCTION THEREOF AND PI3K KINASE INHIBITORS

FIELD: medicine; pharmacology. ^ SUBSTANCE: new annelated asaheterocycles include pyrimidine fragment of general formula I in the form of free bases or pharmaceutically acceptable salts. Compounds of this invention possess properties of PI3 kinase inhibitors. In general formula I X represents oxygen...

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Hauptverfasser: IVASHCHENKO ALEKSANDR VASIL'EVICH, TKACHENKO SERGEJ EVGEN'EVICH, RYZHOVA ELENA ALEKSANDROVNA, PAPADOPOULOS NIKOLAS, OKUN' IL'JA MATUSOVICH, KINZLER KENNET V, SHMIDT-KITTLER OLEG, VELKUELSKU VIKTOR, TRIFILENKOV ANDREJ SERGEEVICH, VOGELSTAIN BERT, KRAVCHENKO DMITRIJ VLADIMIROVICH, RAGO KARLO, SAVCHUK NIKOLAJ FILIPPOVICH, DZHUKSIJANG ZHU, IVASHCHENKO ANDREJ ALEKSANDROVICH
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: medicine; pharmacology. ^ SUBSTANCE: new annelated asaheterocycles include pyrimidine fragment of general formula I in the form of free bases or pharmaceutically acceptable salts. Compounds of this invention possess properties of PI3 kinase inhibitors. In general formula I X represents oxygen atom or sulphur atom; Z represents oxygen atom, R1 represents hydrogen atom or optionally substituted C1-C6alkyl, or Z represents nitrogen atom together with bound carbon atom forming through Z and R1 optionally substituted annelated imidazoline cycle; R2 represents optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted phenyl, possibly annelated with 5-6-term heterocyclyl containing heteroatoms chosen from oxygen and nitrogen, optionally substituted 5-6-term heterocyclyl containing heteroatoms chosen from nitrogen, oxygen and/or sulphur, possibly annelated with phenyl ring. Invention also concerns method of production of compounds, pharmaceutical compositions and medical products. ^ EFFECT: effective application for preparation of medical products for oncologic therapy. ^ 14 cl, 3 dwg, 1 tbl, 4 ex