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JAK inhibitors pyrazolopyrimidine compounds and methods
专利权人:
INC.;GENENTECH
发明人:
BLANEY, JEFFREY,GIBBONS, PAUL A.,HANAN, EMILY,LYSSIKATOS, JOSEPH P.,MAGNUSON, STEVEN R.,PASTOR, RICHARD,RAWSON, THOMAS E.,ZHOU, AIHE,ZHU, BING-YAN
申请号:
ES09824234
公开号:
ES2545541T3
申请日:
2009.11.02
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Compound of Formula Ia: ** Formula ** enantiomers, diastereomers or pharmaceutically acceptable salts thereof, wherein: R1 is H; R2 is -OR4, -NR3R4, -NR3NR12R4, -NR3S (O) R4 or -NR3S (O) 2R4; R3 is H or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, wherein said alkyl, alkenyl and alkynyl are optionally substituted with oxo, F, ORa or NRaRb; R4 is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, - (C0-C5 alkyl) (C1-C9 heterocyclyl), - (C0-C5 alkyl) (C3-C6 cycloalkyl), - (alkyl C0-C5) (C1-C9 heteroaryl), - (C0-C5 alkyl) (C6-C10 aryl), wherein said alkyl, alkenyl and alkynyl are optionally substituted with R8, and said aryl, cycloalkyl, heteroaryl and heterocyclyl are optionally substituted with R9; or R3 and R4 are taken together with the nitrogen to which they are attached to form a C1-C9 heterocyclyl optionally substituted with R13; Z is -NR5R6; R5 is H; R6 is H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, - (C0-C5 alkyl) (C1-C9 heterocyclyl), - (C0-C5 alkyl) (C3-C8 cycloalkyl), - (alkyl C0-C5) (C1-C9 heteroaryl), - (C0-C5 alkyl) (C6-C9 aryl), wherein said alkyl, alkenyl and alkynyl are optionally substituted with R10, and said aryl, cycloalkyl, heteroaryl and heterocyclyl are optionally substituted with R11; R7 is H; R8 is independently oxo, halo, ORa or NRaRb; R9 is independently oxo, -CN, -CF3, halo, -C (O) C1-C6 alkyl, -C (O) ORa, -C (O) NRaRb, - (C0-C5 alkyl) NRaRb, - (C0 alkyl -C5) ORa, - (C0-C5 alkyl) SRa, -O [C (Ra) 2] 1-3O-, C1-C3 alkyl optionally substituted with oxo or F, - (C0-C5 alkyl) (C3 cycloalkyl) C6) optionally substituted with oxo or F, - (C0-C5 alkyl) C1-C9 heterocyclyl optionally substituted with halo, oxo, C1-C3 alkyl or C (O) C1-C3 alkyl, - (C0-C5 alkyl) C6 aryl optionally substituted with halo or C1-C3 alkyl, -O (C1-C3 alkyl), or - (C0-C5 alkyl) C1-C9 heteroaryl optionally substituted with halo or C1-C3 alkyl; R10 is independently oxo, halo, ORa or NRaRb; R11 is independently oxo, -CN, -CF3, halo, -O [C (Ra) 2] 1-3O-, -C (O) C1-C6 alkyl, -C (O) O
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