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.

公开(公告)号：US20230348420A1

公开(公告)日：2023-11-02

申请号：US18002291

申请日：2021-06-24

Applicant: Novartis AG

Inventor： Nicolas AMIOT ,  Darija DEDIC ,  Peng FU ,  Fabrice GALLOU ,  Xingxian GU ,  Cornelius HARLACHER ,  Siqian LIU ,  Shuping YAO ,  Jiong YE ,  Jianguang ZHOU

IPC: C07D401/12 ,  C07D401/14 ,  C07D237/08 ,  C07D231/14

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D237/08 ,  C07D231/14

Abstract: The invention relates to a novel process, novel process step(s) and novel intermediate(s) useful for the preparation of 1,4-disubstituted pyridazine compounds, such as 5-(1H-Pyrazol-4-yl)-2-(6-((2,2,6,6-tetramethylpiperidin-4-yl)oxy)pyridazin-3-yl)phenol.

公开(公告)号：US20190308180A1

公开(公告)日：2019-10-10

申请号：US16316709

申请日：2017-07-10

Applicant: Novartis AG

Inventor： Fabrice GALLOU ,  Pengfei GUO ,  Jianguang ZHOU ,  Michael PARMENTiER

IPC: B01J31/22 ,  C08L71/00 ,  B01J13/00 ,  B01J31/24 ,  B01J31/02

Abstract: The present invention is directed to reaction mixtures comprising a water-surfactant mixture, wherein the catalyst comprises a compound with solubilizing groups. This technology improves the solubility of the reaction components in the water-surfactant mixture and thereby, greatly increases the productivity and selectivity of the chemical reaction.

公开(公告)号：US20170166517A1

公开(公告)日：2017-06-15

申请号：US15432213

申请日：2017-02-14

Applicant: Novartis AG

Inventor： Fabrice GALLOU ,  Joerg Matthias SEDELMEIER ,  Caspar VOGEL

IPC: C07C251/52 ,  C07C47/546 ,  C07C22/08 ,  C07C17/35 ,  C07C249/04 ,  C07C17/04 ,  C07C51/15 ,  C07C29/44 ,  C07C249/12 ,  C07C25/18 ,  C07C17/354

CPC classification number: C07C251/52 ,  C07C17/04 ,  C07C17/12 ,  C07C17/14 ,  C07C17/26 ,  C07C17/35 ,  C07C17/354 ,  C07C22/08 ,  C07C25/18 ,  C07C29/14 ,  C07C29/147 ,  C07C29/44 ,  C07C33/50 ,  C07C45/27 ,  C07C47/546 ,  C07C47/55 ,  C07C49/82 ,  C07C51/15 ,  C07C249/04 ,  C07C249/12 ,  C07C259/04 ,  C07C2601/14 ,  C07C2601/16 ,  C07D205/04

Abstract: This invention relates to novel processes for synthesizing N-(4-cyclohexyl-3-trifluoromethyl-benzyloxy)-acetimidic acid ethyl ester and to the compound of formula I below and other intermediates that are used in such processes.

公开(公告)号：US20220274966A1

公开(公告)日：2022-09-01

申请号：US17663285

申请日：2022-05-13

Applicant: Novartis AG

Inventor： Fabrice GALLOU ,  Michael PARMENTIER

IPC: C07D405/14 ,  C07B63/04

Abstract: The present invention is directed to methods for producing crystals or aggregates of organic compounds using a composition comprising a surfactant-water mixture, the organic compound and optionally an organic solvent as starting composition. This surfactant system enables the production of a high variety of different crystals and aggregates. The method is in particular suitable for obtaining crystals and aggregates optimized for isolation and purification during chemical synthesis processes.

公开(公告)号：US20200017482A1

公开(公告)日：2020-01-16

申请号：US16334970

申请日：2017-09-26

Applicant: Novartis AG

Inventor： Fabrice GALLOU ,  Michael PARMENTIER

IPC: C07D405/14 ,  C07B63/04

Abstract: The present invention is directed to methods for producing crystals or aggregates of organic compounds using a composition comprising a surfactant-water mixture, the organic compound and optionally an organic solvent as starting composition. This surfactant system enables the production of a high variety of different crystals and aggregates. The method is in particular suitable for obtaining crystals and aggregates optimized for isolation and purification during chemical synthesis processes.