Pyrazolopyrimidine compounds that inhibit PI3K and methods of use

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专利权人:

GENENTECH, INC.;F. HOFFMANN-LA ROCHE AG

发明人:

DOTSON, JENNAFER,HEFFRON, TIM,OLIVERO, ALAN,SUTHERLIN, DANIEL P.,WANG, SHUMEI,ZHU, BING-YAN,CHUCKOWREE, IRINA,FOLKES, ADRIAN,WAN, NAN CHI

申请号：

ES09706948

公开号：

ES2494365T3

申请日:

2009.01.29

申请国别(地区):

ES

年份:

2014

代理人:

摘要：

A compound selected from Formula I: and stereoisomers, geometric isomers, tautomers, or pharmaceutically acceptable salts thereof, wherein: R1 is selected from H, C1-C12 alkyl, -C (>； = O) NR10R11, -NR12C ( >； = O) R10, -NR12C (>； = O) OR11, -NR12C (>； = O) NR10R11, and C1-C20 heteroaryl where C1-C20 heteroaryl is optionally substituted with one or more groups independently selected from C1-C12 alkyl, (C1-C12) -NR10R11 alkyl, (C1-C12) alkyl -OR10, C6-C20 aryl, F, Cl, Br, I, -CN, -CF3, -CO2H, -C (>； = O) NR10R11, - NO2, -NR10R11, -NHCOR10, -OR10, -S (O) 2NR10R11, and -S (O) 2R10； R2 is C1-C12 alkyl； R3 is selected from carbon-linked C2-C20 heterocyclyl and carbon-linked C1-C20 heteroaryl, where carbon-linked C2-C20 heterocyclyl and carbon-linked C1-C20 heteroaryl are optionally substituted with one or more groups independently selected from C1- alkyl C12, aryl C6-C20, F, Cl, Br, I, -CH3, -CN, -CF3, -CH2OH, -CO2H, -CONH2, -CON (CH3) 2, -NO2, -NH2, -NHCH3, - NHCOCH3, -OH, -OCH3, -SH, -NHC (>； = O) NHCH3, and -S (O) 2CH3； R4 is selected from -NR10R13, -NR12C (>； = O) R10, -NR10 (C1-C12 alkyl) NR10R13, -NR10 (C1-C12 alkyl) OR10, -NR10 (C1-C12 alkyl) C (>； = O) NR10R13, -NR10 ((C1-C12 alkylene)) - (C3-C12 carbocyclyl), -NR10 ((C1-C12 alkylene)) - (C2-C20 heterocyclyl), -NR10 ((C1-C12 alkylene)) - ( C6-C20 aryl), -NR10 (C1-C12 alkylene) - (C1-C20 heteroaryl), -OR10, -O ((C1-C12 alkylene)) - (C3-C12 carbocyclyl), -O ((C1- alkylene C12)) - (C2-C20 heterocyclyl), -O ((C1-C12 alkylene)) - (C6-C20 aryl), -O ((C1-C12 alkylene)) - (C1-C20 heteroaryl), - (( C1-C12 alkylene)) NR10R13, - ((C1-C12 alkylene)) - (C3-C12 carbocyclyl), - ((C1-C12 alkylene)) - (C2-C20 heterocyclyl), - ((C1-C12 alkylene) ) - (C6-C20 aryl), - ((C1-C12 alkylene)) - (C1-C20 heteroaryl), - (C2-C8 alkynylene) NR10R13, - (C2-C8 alkynylene) - (C3-C12 carbocyclyl), - (C2-C8 alkynylene) - (C2-C20 heterocyclyl), - (C2-C8 alkynylene) - (C6-C20 aryl), - (C2-C8 alkynylene) - (C1-C20 heteroaryl), - (C1-

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