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PURINE INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA
专利权人:
MERK SHARP I DOUM KORP.
发明人:
ACHAB Abdelgkhani Abe (US),АЧАБ Абделгхани Абе (US),ALTMAN Majkl D. (US),АЛЬТМАН Майкл Д. (US),DENG Jongki (US),ДЕНГ Йонгки (US),GYUZI Timoti (US),ГЮЗИ Тимоти (US),KATTAR Solomon (US),КАТТАР Соломон (,ACHAB Abdelgkhani Abe,АЧАБ Абделгхани Абе,ALTMAN Majkl D.,АЛЬТМАН Майкл Д.,DENG Jongki,ДЕНГ Йонгки,GYUZI Timoti,ГЮЗИ Тимоти,KATTAR Solomon,КАТТАР Соломон,KATTS Dzhejson D.,КАТЦ Джейсон Д.,METOT Dzhon
申请号:
RU2015122895
公开号:
RU0002658006C2
申请日:
2013.11.15
申请国别(地区):
RU
年份:
2018
代理人:
摘要:
FIELD: medicine; pharmaceuticals.SUBSTANCE: present invention relates to a novel compound of formula I, or a pharmaceutically acceptable salt or stereoisomer thereof, having properties of a PI3K-alpha inhibitor and relative selectivity for PI3K-delta. In formula I I R1 is selected from hydrogen, C1-5alkyl or C3-8cycloalkyl, where R1 is optionally substituted with 0, 1 or 2 groups independently selected from hydrogen, fluorine and chlorine; R2 is selected from cyclopropyl, isobutyl, 2-methylpropyl, methyl, ethyl, iodine, pyridazinyl, pyrimidinyl, pyrazinyl, pyridinyl, pyrrolidinyl, piperidinyl, ethoxycarbonyl, cyclohexyl, phenyl, quinazolinyl, isoquinolinyl, pyrazolyl, imidazolyl, indolyl, indazolyl, thiazolyl, pyrazolo[1,5-a]pyrimidinyl, 3,6-dihydro-2H-pyranyl, 1H-pyrrolo[2,3-b]pyridinyl, cyclobutyl, 1H-pyrazolo[3,4-b]pyridinyl, pyrrolo[2,3-b]pyridinyl, benzimidazolyl, morpholinyl, 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridinyl, 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazolyl, where R2 is substituted with 0, 1 or 2 independently selected R3; n is 0, 1, 2, or 3; A is C3-12cycloalkyl, mono- or bicyclic C3-7heterocycloalkyl, containing a nitrogen atom as a heteroatom, and C6-12spirocyclyl containing a nitrogen atom in the ring; L is selected from O, S, SO2 and -CH2; K is selected from a bond, O, N((C1-5)alkyl)1-2 and -C(O)N(Rb)-(CH2)m; Rb is H or C1-10alkyl; m has the value 0; R3 is independently selected from a fluorine atom, chlorine atom, methyl, ethyl, propyl, methoxy, pyrazolyl, thiazolyl, benzisoxazolyl, pyrazinyl, cyclopropyl, pyridinyl, cyclopropylmethyl, hydroxy, oxo, dimethylamino, morpholinyl, imidazolyl, pyrrolidinyl, piperidinyl, tert-butyl, trifluoromethyl, methoxymethyl, isoxybutylcarboxy, tert-butylcarboxy, phenylcarboxy, hydrogen, methylpropylcarboxy, ethoxycarbonyl and others indicated in the claims, where each R3 is substituted with 0, 1, 2 or 3 substituents R4 and each R4 is independently selected from methyl, trifluoromethyl, methoxy, amino, dimethylamino, flu
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