公开(公告)号：US20210087194A1

公开(公告)日：2021-03-25

申请号：US17009215

申请日：2020-09-01

申请人： Novartis AG

发明人： Hao Wang ,  Jiong Ye ,  Bo Han ,  Dietmar Flubacher ,  Hans Stettler ,  Fabrice Gallou ,  Franck Mallet ,  Matthias Napp ,  Michael Haller

IPC分类号： C07D487/04

摘要： The present disclosure relates to a method of synthesizing imidazopyrrolidinone derivative, such as compound of formula (I), or a solvate including hydrate thereof, or a co-crystal thereof, and/or intermediates thereof, their use as pharmaceuticals and the use of intermediates.

公开(公告)号：US20200031824A1

公开(公告)日：2020-01-30

申请号：US16495275

申请日：2018-03-29

申请人： Novartis AG

发明人： Fabrice Gallou ,  Philipp Lustenberger ,  Christian Mathes ,  Qiangbiao Pan ,  Benli Zou

IPC分类号： C07D471/04 ,  B01J27/128 ,  B01J23/44

摘要： This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.

公开(公告)号：US20190337952A1

公开(公告)日：2019-11-07

申请号：US16462266

申请日：2017-11-20

申请人： Novartis AG

发明人： Hao Wang ,  Jiong Ye ,  Bo Han ,  Dietmar Flubacher ,  Hans Stettler ,  Fabrice Gallou ,  Franck Mallet ,  Matthias Napp ,  Michael Haller

IPC分类号： C07D487/04

摘要： The present disclosure relates to a method of synthesizing imidazopyrrolidi-none derivative, such as compound of formula (I), or a solvate including hydrate thereof, or a co-crystal thereof, and/or intermediates thereof, their use as pharmaceuticals and the use of intermediates.

公开(公告)号：US11235316B2

公开(公告)日：2022-02-01

申请号：US16316709

申请日：2017-07-10

申请人： Novartis AG

发明人： Fabrice Gallou ,  Pengfei Guo ,  Jianguang Zhou ,  Michael Parmentier

IPC分类号： C07C211/04 ,  B01J31/22 ,  B01J13/00 ,  B01J31/02 ,  B01J31/24 ,  C08L71/00 ,  B01J31/18 ,  C07C231/02 ,  C07C233/73

摘要： 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：US20200299281A1

公开(公告)日：2020-09-24

申请号：US16088374

申请日：2017-03-27

申请人： Novartis AG

发明人： Fabrice Gallou ,  Michael PARMENTIER ,  Jianguang ZHOU ,  Pengfei GUO

IPC分类号： C07D405/14 ,  C07D401/04 ,  C07D403/14 ,  C07C269/06 ,  C07D333/64 ,  C07C211/52 ,  C07D487/04 ,  C07D241/20

摘要： The present invention is directed to reaction mixtures comprising a water-surfactant mixture and a co-solvent. This technology reduced the amount of organic solvents needed for performing chemical reactions. Furthermore, compared to reaction mixtures lacking the co-solvent, solvation of the reactants and products of the chemical reaction is greatly enhanced, leading to a significantly improved yield, purity, reproducibility and robustness.

公开(公告)号：US09604914B2

公开(公告)日：2017-03-28

申请号：US14376143

申请日：2013-02-01

申请人： NOVARTIS AG

发明人： Fabrice Gallou ,  Joerg Matthias Sedelmeier ,  Caspar Vogel

IPC分类号： C07C249/12 ,  C07D205/04 ,  C07C47/55 ,  C07C22/08 ,  C07C17/12 ,  C07C17/14 ,  C07C17/26 ,  C07C17/35 ,  C07C17/354 ,  C07C25/18 ,  C07C259/04 ,  C07C33/50 ,  C07C49/82 ,  C07C17/04 ,  C07C29/14 ,  C07C29/147 ,  C07C29/44 ,  C07C45/27 ,  C07C51/15 ,  C07C251/52

CPC分类号： 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 ,  C07C2101/14 ,  C07C2101/16 ,  C07C2601/14 ,  C07C2601/16 ,  C07D205/04

摘要： 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：US11236076B2

公开(公告)日：2022-02-01

申请号：US16088374

申请日：2017-03-27

申请人： Novartis AG

发明人： Fabrice Gallou ,  Michael Parmentier ,  Jianguang Zhou ,  Pengfei Guo

IPC分类号： C07D405/14 ,  C07C211/52 ,  C07C269/06 ,  C07D241/20 ,  C07D333/64 ,  C07D401/04 ,  C07D403/14 ,  C07D487/04

摘要： The present invention is directed to reaction mixtures comprising a water-surfactant mixture and a co-solvent. This technology reduced the amount of organic solvents needed for performing chemical reactions. Furthermore, compared to reaction mixtures lacking the co-solvent, solvation of the reactants and products of the chemical reaction is greatly enhanced, leading to a significantly improved yield, purity, reproducibility and robustness.

公开(公告)号：US11220681B2

公开(公告)日：2022-01-11

申请号：US16478149

申请日：2018-01-11

申请人： Novartis AG

发明人： Yu Gai ,  Fabrice Gallou ,  Feng Gao ,  Pengfei Guo ,  Weiyong Kong ,  Michael Parmentier ,  Jianguang Zhou

IPC分类号： C12N9/96 ,  C12P7/22 ,  C12N9/04 ,  C12N9/02 ,  C12P17/06 ,  C12P17/12

摘要： The present invention is directed to aqueous reaction mixtures for enzymatic synthesis reactions comprising a surfactant. The surfactant in the reaction mixture increases stability and yield of the enzymatic reaction. Furthermore, method for performing an enzymatic reaction using said aqueous reaction mixtures are provided.

公开(公告)号：US10723735B2

公开(公告)日：2020-07-28

申请号：US16495275

申请日：2018-03-29

申请人： Novartis AG

发明人： Fabrice Gallou ,  Philipp Lustenberger ,  Christian Mathes ,  Qiangbiao Pan ,  Benli Zou

IPC分类号： C07D471/04 ,  B01J23/44 ,  B01J27/128

摘要： This invention relates to novel processes for synthesizing [1-(4-Methanesulfonyl-2-trifluoromethyl-benzyl)-2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl]-acetic acid and to intermediates that are used in such processes.