公开(公告)号：US11203595B2

公开(公告)日：2021-12-21

申请号：US16941395

申请日：2020-07-28

Applicant: NOVARTIS AG

Inventor： Badry Bursulaya ,  Andreas Fisch ,  James Paul Lajiness ,  Rainer Machauer ,  Swapnil Malekar ,  Hank Michael James Petrassi ,  Farshad Ramazani ,  Anne-Catherine Remond ,  Thomas Ullrich ,  Peggy Usselmann ,  Eric Vangrevelinghe

IPC: C07D471/04 ,  A61K9/19 ,  A61P21/00 ,  A61K9/00 ,  A61K9/50 ,  A61K31/437 ,  A61K31/496 ,  A61K31/538

Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US10683287B2

公开(公告)日：2020-06-16

申请号：US16378887

申请日：2019-04-09

Applicant: Novartis AG

Inventor： Sangamesh Badiger ,  Murali Chebrolu ,  Konstanze Hurth ,  Sebastien Jacquier ,  Rainer Martin Lueoend ,  Rainer Machauer ,  Heinrich Rueeger ,  Marina Tintelnot-Blomley ,  Siem Jacob Veenstra ,  Markus Voegtle

IPC: C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/5377 ,  C07B59/00

Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.

公开(公告)号：US20220363670A1

公开(公告)日：2022-11-17

申请号：US17125335

申请日：2020-12-17

Applicant: NOVARTIS AG

Inventor： Simona Cotesta ,  Marc Gerspacher ,  Catherine Leblanc ,  Edwige Liliane Jeanne Lorthiois ,  Bo Liu ,  Rainer Machauer ,  Robert Mah ,  Christophe Mura ,  Pascal Rigollier ,  Nadine Schneider ,  Stefan Stutz ,  Andrea Vaupel ,  Nicolas Warin ,  Rainer Wilcken

IPC: C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D401/14 ,  C07D471/04 ,  C07D413/14 ,  C07D487/04

Abstract: The present invention provides a compound of formula (I) or a stereoisomer thereof, or an atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a stereoisomer thereof, or a pharmaceutically acceptable salt of an atropisomer thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：US20210251996A1

公开(公告)日：2021-08-19

申请号：US16981208

申请日：2019-03-25

Applicant: NOVARTIS AG

Inventor： Luca Arista ,  Christina Hebach ,  Gregory John Hollingworth ,  Philipp Holzer ,  Patricia Imbach-Weese ,  Rainer Machauer ,  Niko Schmiedeberg ,  Anna Vulpetti ,  Thomas Zoller

IPC: A61K31/519 ,  C07D519/00 ,  C07D487/04 ,  A61P35/00

Abstract: The invention relates to compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

公开(公告)号：US10301296B2

公开(公告)日：2019-05-28

申请号：US16020212

申请日：2018-06-27

Applicant: Novartis AG

Inventor： Sangamesh Badiger ,  Murali Chebrolu ,  Konstanze Hurth ,  Sebastien Jacquier ,  Rainer Martin Lueoend ,  Rainer Machauer ,  Heinrich Rueeger ,  Marina Tintelnot-Blomley ,  Siem Jacob Veenstra ,  Markus Voegtle

IPC: C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/5377 ,  C07B59/00

Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.

公开(公告)号：US11702409B2

公开(公告)日：2023-07-18

申请号：US17125335

申请日：2020-12-17

Applicant: NOVARTIS AG

Inventor： Simona Cotesta ,  Marc Gerspacher ,  Catherine Leblanc ,  Edwige Liliane Jeanne Lorthiois ,  Bo Liu ,  Rainer Machauer ,  Robert Mah ,  Christophe Mura ,  Pascal Rigollier ,  Nadine Schneider ,  Stefan Stutz ,  Andrea Vaupel ,  Nicolas Warin ,  Rainer Wilcken

IPC: C07D403/14 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D403/14 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07B2200/13

Abstract: The present invention provides a compound of formula (I) or a stereoisomer thereof, or an atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a stereoisomer thereof, or a pharmaceutically acceptable salt of an atropisomer thereof;




a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：US10766894B2

公开(公告)日：2020-09-08

申请号：US16335496

申请日：2017-09-21

Applicant: NOVARTIS AG

Inventor： Badry Bursulaya ,  Andreas Fisch ,  James Paul Lajiness ,  Rainer Machauer ,  Swapnil Malekar ,  Hank Michael James Petrassi ,  Farshad Ramazani ,  Anne-Catherine Remond ,  Thomas Ullrich ,  Peggy Usselmann ,  Eric Vangrevelinghe

IPC: C07D471/04 ,  A61P21/00 ,  A61K9/00 ,  A61K9/50 ,  A61K31/437 ,  A61K31/496 ,  A61K31/538

Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US20190062319A1

公开(公告)日：2019-02-28

申请号：US16020212

申请日：2018-06-27

Applicant: Novartis AG

Inventor： Sangamesh Badiger ,  Murali Chebrolu ,  Konstanze Hurth ,  Sebastien Jacquier ,  Rainer Martin Lueoend ,  Rainer Machauer ,  Heinrich Rueeger ,  Marina Tintelnot-Blomley ,  Siem Jacob Veenstra ,  Markus Voegtle

IPC: C07D413/14 ,  C07D487/04 ,  C07D471/04 ,  A61K31/5377 ,  C07B59/00

Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.

公开(公告)号：US11613543B2

公开(公告)日：2023-03-28

申请号：US16981059

申请日：2019-03-22

Applicant: NOVARTIS AG

Inventor： Luca Arista ,  Christina Hebach ,  Gregory John Hollingworth ,  Philipp Holzer ,  Patricia Imbach-Weese ,  Julien Lorber ,  Rainer Machauer ,  Niko Schmiedeberg ,  Anna Vulpetti ,  Thomas Zoller

IPC: A61K31/519 ,  C07D487/04 ,  C07D519/00 ,  A61K45/06

Abstract: The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

公开(公告)号：US20210002285A1

公开(公告)日：2021-01-07

申请号：US16981059

申请日：2019-03-22

Applicant: NOVARTIS AG

Inventor： Luca Arista ,  Christina Hebach ,  Gregory John Hollingworth ,  Philipp Holzer ,  Patricia Imbach-Weese ,  Julien Lorber ,  Rainer Machauer ,  Niko Schmiedeberg ,  Anna Vulpetti ,  Thomas Zoller

IPC: C07D487/04 ,  C07D519/00

Abstract: The invention relates to compounds of the formula (I) (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.