[EN] GRK2 INHIBITORS AND USES THEREOF [FR] INHIBITEURS DE GRK2 ET LEURS UTILISATIONS
摘要:
Provided herein are compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, isotopically labeled derivatives, solvates, hydrates, polymorphs, co-crystals, and prodrugs thereof, pharmaceutical compositions thereof, and kits comprising the same. The compounds provided herein are G protein-coupled receptor kinase (e.g., GRK2, GRK3) inhibitors and are therefore useful for, e.g., treating and/or preventing diseases (e.g., cancer) in a subject, for inhibiting tumor growth in a subject, for inhibiting GRK2 and/or GRK3 activity in vitro or in vivo, etc. In certain embodiments, the compounds provided herein are selective for GRK2 and/or GRK3. Also provided herein are methods and synthetic intermediates useful in the preparation of compounds described herein.
HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
申请人:Hilpert Kurt
公开号:US20140163035A1
公开(公告)日:2014-06-12
The invention relates to heterocyclic amide derivatives of formula (I), wherein R
1
, R
2
, R
3
, R
4
, R
5
, X, Y and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
[EN] HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS D'AMIDES HÉTÉROCYCLIQUES UTILISÉS COMME ANTAGONISTES DU RÉCEPTEUR P2X7
申请人:ACTELION PHARMACEUTICALS LTD
公开号:WO2013014587A1
公开(公告)日:2013-01-31
The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, X, Y and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
Heterocyclic amide derivatives as P2X7 receptor antagonists
申请人:Hilpert Kurt
公开号:US09221832B2
公开(公告)日:2015-12-29
The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, X, Y and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.