[EN] COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 1 PROTEINS<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR LA DÉGRADATION CIBLÉE DE PROTÉINES DE KINASE 1 ASSOCIÉS AU RÉCEPTEUR DE L'INTERLEUKINE 1
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2021018118A1
公开(公告)日:2021-02-04
The present invention relates to compounds comprising an interleukin-1 receptor-associated kinase 1 (IRAK1) protein binding moiety and a Von Hippel-Lindau (VHL) E3 ubiquitin ligase binding moiety, and associated methods of use. The compounds are useful as modulators of targeted ubiquitination, especially with respect to IRAK1, which is degraded by the compounds according to the invention.
[EN] AMINOPYRROLOTRIAZINES AS KINASE INHIBITORS<br/>[FR] AMINOPYRROLOTRIAZINES EN TANT QU'INHIBITEURS DE KINASE
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2019147782A1
公开(公告)日:2019-08-01
The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications.
The invention relates to novel pyrrolidine derivatives of formula (I):
wherein R
1
, R
2
and R
3
are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
3-ACETYLENYL-PYRAZOLE-PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USES THEREOF
申请人:Si Chuan University
公开号:US20170305920A1
公开(公告)日:2017-10-26
The present invention relates to the field of chemical and medicine, more particularly, 3-ethynylpyrazolopyrimidine derivatives and their preparation methods and uses. The invention provides a 3-ethynylpyrazolopyrimidine derivative, and the structure is shown in formula I. The present invention also provides preparation methods and use of 3-ethynylpyrazolopyrimidine derivatives, comprising the compounds and derivatives, and their pharmaceutical compositions for the use of the treatment and prevention of tumors.
The present invention relates to compounds of Formula I:
as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.