公开(公告)号：US20220211718A1

公开(公告)日：2022-07-07

申请号：US17609874

申请日：2020-05-11

Applicant: LES LABORATOIRES SERVIER ,  NOVARTIS AG

Inventor： James Brooke MURRAY ,  Frèdéric COLLAND ,  Audrey CLAPERON

IPC: A61K31/5377 ,  A61P35/02

Abstract: The invention relates to a Bcl-2 inhibitor for use in the treatment of a Bcl-2 mediated cancer carrying at least 1, 2, 3, 4, 5 or all of the following mutations: (i) Gly101Val; (ii) Asp103Tyr; (iii) Asp103Val; (iv) Asp103Glu; (v) Arg129Leu and (vi) Ala113Gly; wherein the Bcl-2 inhibitor is N-(4-hydroxyphenyl)-3-{6-[((3S)-3-(4-morpholinylmethyl)-3,4-dihydro-2(1H)-isoquinolinyl)carbonyl]-1,3-benzodioxol-5-yl}-N-phenyl-5,6,7,8-tetrahydro-1-indolizine carboxamide (Compound A) or 5-(5-chloro-2-{[(3S)-3-(morpholin-4-ylmethyl)-3,4-dihydroisoquinolin-2(1H)-yl]carbonyl}phenyl)-N-(5-cyano-1,2-dimethyl-1H-pyrrol-3-yl)-N-(4-hydroxyphenyl)-1,2-dimethyl-iH-pyrrole-3-carboxamide (Compound B), or a pharmaceutically acceptable salt thereof.