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NOVEL PHOSPHATE COMPOUNDS, SYNTHESIS METHOD THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
专利权人:
LES LABORATOIRES SERVIER
发明人:
LE-TIRAN Arno (FR),ЛЕ-ТИРАН Арно (FR),LE-DIGARER Terri (FR),ЛЕ-ДИГАРЕР Тьерри (FR),STARK Zherom-Benua (FR),СТАРК Жером-Бенуа (FR),ANLEN Zhan-Mishel (FR),АНЛЕН Жан-Мишель (FR),GIJUZI Anne-Fransua (FR),LE-TIRAN Arno,ЛЕ-ТИРАН Арно,LE-DIGARER Terri,ЛЕ-ДИГАРЕР Тьерри,STARK Zherom-Benua,СТАРК Жером-Бенуа,ANLEN Zhan-Mishel,АНЛЕН Жан-Мишель,GIJUZI Anne-Fransua,ГИЙУЗИ Анне-Франсуа,DE-NANTEJ Gijom,ДЕ-НАНТЁЙ
申请号:
RU2014130129
公开号:
RU0002617682C2
申请日:
2014.07.22
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I), its enantiomers and pharmaceutically acceptable salts and compositions based thereon, which can be used in oncology:where X and Y represent C or N, but cannot be identical, A1 and A2 together with atoms bearing them form heterocycle Het, selected from 5,6,7,8-tetrahydroindolizine or indolizine, or A1 and A2 represent H, (C1-C6)polyhaloalkyl or (C1-C6)alkyl, T represents H, (C1-C6)alkyl, optionally substituted with one-three halogen atoms, (C1-C4)alkyl-NR1R2, or (C1-C4)alkyl-OR6, R1 and R2 represent H or (C1-C6)alkyl, or R1 and R2 with a nitrogen atom bearing them form heterocycloalkyl, R3 represents a cycloalkyl, heterocycloalkyl, aryl or heteroaryl, R4 is phenyl, substituted in para-position with a group -OPO(OM)(OM'), -OPO(OM)(O-M1+), -OPO(O-M1+)(O-M2+), -OPO(O-)(O-)M32+, -OPO(OM)(O[CH2CH2O]nCH3), or -OPO(O-M1+)(O[CH2CH2O]nCH3), where M and M ' denote H, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, cycloalkyl or heterocycloalkyl from 5 or 6 members, while M1+ , M2+ and M32+ represent pharmaceutically acceptable cations, n ranges from 1 to 5, wherein carbon atoms of previous groups or their possible substitutes can be deuterated, R5 represents H or halogen, (C1-C6)alkyl or (C1-C6)alkoxy, R6 represents H or (C1-C6)alkyl, Ra, Rb, Rc and Rd represents R7, halogen, (C1-C6)alkoxy, hydroxy, NR7R7'-CO-(C0-C6)alkyl-O-, or substitutes of pair (Rb, Rc) together with carbon atoms, bearing them, form a ring of 5–7 members with 1 or 2 heteroatoms, selected from O and S, wherein one or more carbon atoms of ring can be deuterated or substituted with 1–3 groups, selected from halogen and (C1-C6)alkyl, R7 and R7' are H, (C1-C6)alkyl, or R7 and R7' together with a nitrogen atom, bearing them, form heterocycle, consisting of 5–7 members, "aryl" denotes phenyl, naphthyl, biphenyl or indenyl, "heteroaryl" denotes a mono- or bicyclic group, consisting of 5–10 members with at least one aromatic fragment and 1
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