[EN] DIHYDROIMIDAZO [ 1, 5-F] PTERIDINES AS POLO-LIKE KINASE INHIBITORS<br/>[FR] DIHYDROIMIDAZO [ 1, 5-F] PTÉRIDINES EN TANT QU'INHIBITEURS DE KINASES DE TYPE POLO (PLK)
申请人:TAKEDA PHARMACEUTICAL
公开号:WO2010025073A1
公开(公告)日:2010-03-04
The present invention provides PLK inhibitors of the formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using the compounds.
[EN] DEGRADATION OF (EGFR) BY CONJUGATION OF EGFR INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE<br/>[FR] DÉGRADATION D'EGFR PAR CONJUGAISON D'INHIBITEURS D'EGFR AVEC UN LIGAND DE LIGASE E3 ET PROCÉDÉS D'UTILISATION
申请人:BEIGENE LTD
公开号:WO2022012622A1
公开(公告)日:2022-01-20
Disclosed herein are novel bifunctional compounds formed by conjugating EGFR inhibitor moieties with E3 ligase ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.
The present invention provides PLK inhibitors of the formula
wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using the compounds.
PYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
申请人:Hollick Jonathan James
公开号:US20110046093A1
公开(公告)日:2011-02-24
The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR
7
; Y is O or N—(CH
2
)
n
R
19
; n is 1, 2 or 3; m is 1 or 2; R
1
and R
2
are each independently H, alkyl or cycloalkyl; R
4
and R
4′
each independently H alkyl; or R
4
and R
4′
together form a spiro cycloalkyl group; R
19
is H, alkyl, aryl or a cycloalkyl group; R
6
is OR
8
or halogen; and R
7
and R
8
are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like.
Pyrimidine derivatives as protein kinase inhibitors
申请人:Hollick Jonathan James
公开号:US08563542B2
公开(公告)日:2013-10-22
The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N—(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4′ each independently H alkyl; or R4 and R4′ together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like.