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Bruton Tyrosine Kinase Inhibitors and Methods of their use
专利权人:
JANSSEN PHARMACEUTICA N.V.
发明人:
申请号:
ARP160103789
公开号:
AR107042A1
申请日:
2016.12.12
申请国别(地区):
AR
年份:
2018
代理人:
摘要:
1. This specification refers to the compound, its use and preparation method, and the compound forming the compound. 1. Claim 1: a formula compound (1),where R¹ is H; R² is selected from the group consisting of: CH₂-cyclohexyl, wherein the cyclohexyl is optionally substituted with OH; 3-hydroxyamantan-1-yl; and C₃₋₆ cycloalkyl optionally substituted with 1, 2 or 3 substituents, each independently selected from the group consisting of: OH, halogen, C₁₋₆-alkyl,haloalkyl C₁₋₆,O-asphalt c83218c31832626;Cn, No. 8310; r8311;NR -C (O) H NR -C (O) -alquilo CNr.831222-c (o) - halide c83221;831222-c (o) - o-asphalt c832138;NR⁸-C (O) -alq C₁₋₆-OH, NR⁸-C (O) -alq C₁₋₆-NR⁶R⁷ and NR⁸-C (O) -C (R³) = CR⁴ (R⁵);where R³ is selected from the group consisting of: H, CN, halogen, C₁₋₆ haloalkyl and C₁₋₆ alkyl;R⁴ and R⁵ are each independently selected from the group consisting of: H; alq C₀₋₆-NR⁶R⁷;Cq-al-C--alkyl;C₃₋₆ cycloalkyl;heterocycloalkyl optionally substituted with C₁₋₆-alkyl;and linker-PEG-biotin; R⁶ and R⁷ are each independently selected from the group consisting of: H, C₁₋₆ alkyl,C / 8333o 8334h 696 CN; 6966 r831222 es h; or R 1 and R 2,They combine with nitrogen atoms to form a pyrethroid ring, which is replaced by NR8310R8311;wherein R⁶ and R⁷ are each independently selected from the group consisting of H; C₁₋₆-alkyl;NR⁸-C (O) -C₁₋₆ alkyl;y NR -C (O) -C (R) 3DCR (R)where R³ is H or CN; R⁴ is H; and R⁵ is H or cyclopropyl; A is selected from the group consisting of: pyridyl; phenyl; pyrimidinyl; pyrazinyl; pyridin-2 (1H) -one; and pyridazinyl; wherein A is optionally substituted with 1, 2 or 3 substituents, each independently selected from the group consisting of halogen, C₁₋₆-alkyl,C₁₋₆ haloalkyl and C₁₋₆ O-alkyl;E selected from the group consisting of O, link and ch832222;G selected from: H; halogen; c832131; anda. Halogenated tar c83218d31832626;NH (C₁₋₆-alkyl);C₃₋₆ cycloalkyl;phenyl; pyrimidinyl; pyridyl; pyridazinyl; pyridin-2 (1H) -one; heterocycloalkyl containing an
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