公开(公告)号：US20250092016A1

公开(公告)日：2025-03-20

申请号：US18580986

申请日：2022-07-20

Applicant: NOVARTIS AG

Inventor： Denghui BAO ,  Fengfeng GUO ,  Matthew James HESSE ,  Viktor HORNAK ,  Sajan JOSEPH ,  Thomas Martin KIRRANE, JR. ,  Haiyao LIN ,  Bo LIU ,  Yanan MIAO ,  Heinz Ernst MOSER ,  Julien PAPILLON ,  Yang QU ,  Lei SHI ,  Jun YUAN ,  Teng ZHANG

IPC: C07D401/14 ,  A61K31/4725 ,  A61K31/501 ,  A61K31/506 ,  A61P31/14 ,  C07D401/04

Abstract: Provided herein are compounds and compositions for treating, managing or preventing coronaviral related diseases. In particular, provided herein are compounds which are inhibitors of SARS-CoV-2 main protease (Mpro), pharmaceutical compositions comprising such compounds, method for synthesizing such compounds and methods of using such compounds and compositions for the treatment, management or prevention of coronaviral related diseases.

公开(公告)号：US20250101006A1

公开(公告)日：2025-03-27

申请号：US18834099

申请日：2023-01-30

Applicant: NOVARTIS AG

Inventor： Markus BAENZIGER ,  Fabrice GALLOU ,  Fengfeng GUO ,  Rudolf HÄNGGI ,  Enjian HAN ,  Guido JORDINE ,  Jialiang LI ,  Weipeng LIU ,  Bukeyan MIAO ,  Shaofeng RONG ,  Ernesto SANTANDREA ,  Paul Bernd SCHIRNER ,  Xiaodong SHEN ,  Can WANG ,  Hao ZHANG

IPC: C07D403/14 ,  B01J31/22 ,  B01J31/24

Abstract: The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.