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Benzimidazolone derivatives as bromodomain inhibitors
专利权人:
Inc.;Gilead Sciences
发明人:
AKTOUDIANAKIS, Evangelos,CHIN, Gregory,CORKEY, Britton Kenneth,DU, Jinfa,ELBEL, Kristyna,JIANG, Robert H.,KOBAYASHI, Tetsuya,MARTINEZ, Ruben,METOBO, Samuel E.,MISH, Michael,SHEVICK, Sophie,SPERANDIO,
申请号:
ES14729114
公开号:
ES2626397T3
申请日:
2014.03.27
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of Formula (I) ** Formula ** in which R1a and R1b are each independently C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy, C1-C6 hydroxyalkyl, C3- cycloalkyl C6 or CH2-C3-C6 cycloalkyl; R2a and R2b are each independently H or halogen; R3 is C5-C10 aryl, C5-C10 heteroaryl or C5-C10 heteroarylalkyl, each of which is optionally substituted with 1 to 5 R20 groups; or -S (O) 2NHR4, wherein R4 is C1-C6 alkyl or C3-C7 cycloalkyl, each of which is optionally substituted with 1 to 5 R20 groups; or a remainder of formula ** Formula ** in which R6 is H, OH or halogen; and R7 and R8 are each independently C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C1-C6 heteroalkyl, C5-C12 aryl, C5-C12 heteroaryl or C5-C12 heteroarylalkyl, each of which it is optionally substituted with 1 to 5 R20 groups; or R6 is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, phenyl, naphthyl or C3-C12 heteroaryl; and R7 and R8 together form a C1-C6 alkylidene group having a double bond with the carbon to which each of R6, R7 and R8 are attached where each of the C1-C6 alkyl, C2-C6 alkenyl, alkynyl groups C2-C6, -C3-C6 cycloalkyl, phenyl, naphthyl or C3-C12 heteroaryl is optionally substituted with 1 to 5 R20 groups; X is N-Q or O; Q is H, C1-C3 alkyl, C1-C3 haloalkyl, benzyl or substituted benzyl; each R20 is independently C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 heteroalkyl, C3-C6 heterocyclic, C5-C12 aryl, C5-C12 heteroaryl, halogen, oxo, -ORa, -C (O) Ra, -C (O) ORa, -C (O) NRaRb, -OC (O) NRaRb, NRaRb, - NRaC (O) Rb, -NRaC (O) ORb, -S (O) 0-2Ra, -S (O) 2NRaRb , -NRaS (O) 2Rb, -N3, -CN or -NO2, wherein each C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 heteroalkyl, C3-C6 heterocyclic, C5-C12 aryl, C5-C12 heteroaryl is optionally substituted with one to five halogens, oxo, -ORa, -C (O) Ra, -C (O) ORa, -C (O) NRaRb, -OC (O) NRaRb, NRaRb, NRaC (O) Rb, - NRaC (O) ORb, -S (O) 0-2Ra, -S (O) 2NRaRb, -NRaS (O) 2Rb, -N3, -CN or NO2; each Ra and Rb is independently H; or C1
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