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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),KATTAR Solomon (US),КАТТАР Соломон (US),KATTS Dzhejson D. (US),КАТЦ Дже,ACHAB Abdelgkhani Abe,АЧАБ Абделгхани Абе,ALTMAN Majkl D.,АЛЬТМАН Майкл Д.,DENG Jongki,ДЕНГ Йонгки,KATTAR Solomon,КАТТАР Соломон,KATTS Dzhejson D.,КАТЦ Джейсон Д.,METOT Dzhon L.,МЕТОТ Джон Л.,CHZHOU K
申请号:
RU2015122894
公开号:
RU0002661896C2
申请日:
2013.11.15
申请国别(地区):
RU
年份:
2018
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: in the general formula I R1 are selected from methyl, ethyl, propyl, cyclopropyl, cyclopropylmethyl, difluoroethyl and 2,2,2-trifluoroethyl; R2 is selected from hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylaminoC1-6alkyl, C3-6cycloalkyl, saturated 4-6-membered heterocycloalkyl containing 1-2 heteroatoms selected from nitrogen, oxygen or nitrogen and oxygen, phenyl and mono- or bicyclic C5-10heteroaryl containing in the ring 1 to 2 nitrogen atoms or a nitrogen atom and a sulphur atom, where R2 is substituted with 0, 1, 2 or 3 R3 substitutes; n is 1, 2, 3; A is selected from pyrrolidinyl, piperidinyl, azetidinyl, azaspiro[2.4]hept-7-yl and azepanyl; L is selected from NH and N(C1-10alkyl); K is selected from a chemical bond, C(O), CH2, -C(O)N(Rb)-(CH2)m- and C2-4alkynylene; Rb is H or C1-10alkyl, m is 0, 1, 2, or 3; R3 are independently selected from: halogen, C1-6alkyl, C2-6alkenyl, C1-6alkyl(oxy), C1-6alkyl(oxy)(carbonyl), C1-6alkyl(carbonyl), phenyl(oxy), phenyl(oxy)(carbonyl), phenylC1-4alkyl(oxy)(carbonyl), phenylC1-4alkyl(carbonyl), C3-12cycloalkyl(carbonyl), C3-12cycloalkylC1-4alkyl, C5-12bicycloalkyl(carbonyl), C7-8spirocycloalkyl(carbonyl), 5-10 membered mono- or bicyclic heteroaryl containing 1 to 3 heteroatoms in a ring selected from nitrogen or nitrogen and sulphur, 5-10 membered mono- or bicyclic heteroaryl(carbonyl), wherein the heteroaryl contains 1 to 3 ring heteroatoms selected from nitrogen or nitrogen and / or sulphur, (C3-7)heterocycloalkyl containing 1-2 heteroatoms selected from nitrogen and oxygen, (C3-7)heterocycloalkyl (carbonyl), wherein heterocycloalkyl contains 1-2 heteroatoms selected from nitrogen and oxygen, C1-6alkylamino(carbonyl), C3-6cycloalkylamino(carbonyl), -C(O)2(C1-10alkyl), -(C0-6alkyl)CO2H, oxo(=O); C1-10alkylS(O)2, amino, (C0-10alkyl)1-2amino, C1-4acylamino, hydroxyl, (C1-6alkyl)OH, cyano; where R3 each is substituted with 0, 1, 2 R4 substitutes, and each R4 are independently selected from halogen,
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