公开(公告)号：US20240317721A1

公开(公告)日：2024-09-26

申请号：US18571588

申请日：2022-06-22

Applicant: NOVARTIS AG

Inventor： Claudio BOMIO-CONFAGLIA ,  Saskia Maria BRACHMANN ,  Simona COTESTA ,  Marc GERSPACHER ,  Catherine LEBLANC ,  Fabio LIMA ,  Edwige Liliane Jeanne LORTHIOIS ,  Rainer MACHAUER ,  Robert MAH ,  Sophie RACINE ,  Pascal RIGOLLIER ,  Stefan STUTZ ,  Andrea VAUPEL ,  Nicolas WARIN ,  Rainer WILCKEN ,  Frédéric ZECRI

IPC: C07D403/14 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/499 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/547 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/675 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/048 ,  C07D491/107 ,  C07D495/10 ,  C07D498/04 ,  C07D498/08 ,  C07D498/10 ,  C07D513/08 ,  C07F9/6584

CPC classification number: C07D403/14 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/499 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/547 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/675 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/048 ,  C07D491/107 ,  C07D495/10 ,  C07D498/04 ,  C07D498/08 ,  C07D498/10 ,  C07D513/08 ,  C07F9/6584

Abstract: The present invention provides a compound of formula (I), or a pharmaceutically acceptable salt thereof, and the therapeutic uses of said compound. The present invention further provides a pharmaceutical composition comprising said compound.

公开(公告)号：US20240382600A1

公开(公告)日：2024-11-21

申请号：US18687615

申请日：2022-08-30

Applicant: Novartis AG

Inventor： Emilie CHAPEAU ,  Patrick CHENE ,  Pascal FURET ,  Laurence KIEFFER ,  Rainer MACHAUER ,  Anne PICARD ,  Tobias SCHMELZLE ,  Holger SELLNER ,  Nicolas SOLDERMANN ,  Markus VOEGTLE ,  Markus WARTMANN

IPC: A61K47/54 ,  A61K47/55 ,  C07D405/14 ,  C07D417/12

Abstract: The present disclosure relates to a conjugate comprising a YAP/TAZ-TEAD Protein Protein Interaction Inhibitor (PPII) linked to a Ligase Binder via a linker, or a pharmaceutically acceptable salt thereof, as well as methods of using such conjugates.

公开(公告)号：US20240158399A1

公开(公告)日：2024-05-16

申请号：US18169361

申请日：2023-02-15

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

CPC classification number: C07D487/04 ,  C07D519/00 ,  A61K45/06

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：US20210188842A1

公开(公告)日：2021-06-24

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 ,  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：US20190300522A1

公开(公告)日：2019-10-03

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 ,  A61K9/00 ,  A61K9/50 ,  A61P21/00 ,  A61K31/437 ,  A61K31/538 ,  A61K31/496

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：US20240366567A1

公开(公告)日：2024-11-07

申请号：US18572518

申请日：2022-06-23

Applicant: NOVARTIS AG

Inventor： Saskia Maria BRACHMANN ,  Simona COTESTA ,  Xiaoming CUI ,  Ruben DE KANTER ,  Anna FARAGO ,  Marc GERSPACHER ,  Diana GRAUS PORTA ,  Jaeyeon KIM ,  Catherine LEBLANC ,  Edwige Liliane Jeanne LORTHIOIS ,  Rainer MACHAUER ,  Robert MAH ,  Christophe MURA ,  Pascal RIGOLLIER ,  Anirudh Cadapa PRAHALLAD ,  Nadine SCHNEIDER ,  Rowan STRINGER ,  Stefan STUTZ ,  Andrea VAUPEL ,  Nicolas WARIN ,  Rainer WILCKEN ,  Andreas WEISS

IPC: A61K31/416 ,  A61K31/519 ,  A61K39/00 ,  A61K45/06 ,  A61P35/00 ,  C07K16/22

Abstract: The present invention relates to a pharmaceutical combination comprising a KRAS G12C inhibitor and one or more therapeutic agents which is selected from an agent targeting the MARK pathway or an agent targeting parallel pathways; and pharmaceutical compositions comprising the same. The invention also relates to KRAS G12C inhibitors alone or said combinations for use in methods of treating a cancer or a tumor, in particular wherein the cancer or tumor is KRAS G12C mutant.

公开(公告)号：US20240082218A1

公开(公告)日：2024-03-14

申请号：US18267735

申请日：2021-12-20

Applicant: NOVARTIS AG

Inventor： Vasileios ASKOXYLAKIS ,  Saskia Maria BRACHMANN ,  Simona COTESTA ,  Xiaoming CUI ,  Jeffrey ENGELMAN ,  Anna FARAGO ,  Marc GERSPACHER ,  Diana GRAUS PORTA ,  Catherine LEBLANC ,  Edwige Liliane Jeanne LORTHIOIS ,  Bo LIU ,  Rainer MACHAUER ,  Robert MAH ,  Christophe MURA ,  Pascal RIGOLLIER ,  Nadine SCHNEIDER ,  Stefan STUTZ ,  Andrea Helga Emmi VAUPEL ,  Nicolas WARIN ,  Andreas WEISS ,  Rainer WILCKEN ,  Padmaja YERRAMILLI-RAO

IPC: A61K31/416 ,  A61K9/00 ,  A61K31/497 ,  A61K39/395 ,  A61P35/00

CPC classification number: A61K31/416 ,  A61K9/0053 ,  A61K31/497 ,  A61K39/3955 ,  A61P35/00

Abstract: It relates to a pharmaceutical combination comprising a KRAS G12C inhibitor, in particular 1-{6-[(4M)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro [3.3] heptan-2-yl} prop-2-en-1-one (Compound A) and one or more therapeutically active agents selected from a SHP2 inhibitor (e.g. TNO155) and a PD-1 inhibitor, pharmaceutical compositions comprising the same; and methods of using such combinations and compositions in the treatment or prevention of a cancer or a tumor, in particular wherein the cancer or tumor is KRAS G12C mutated.

公开(公告)号：US20240116900A1

公开(公告)日：2024-04-11

申请号：US18250466

申请日：2021-10-29

Applicant: NOVARTIS AG

Inventor： Simona COTESTA ,  Heng GE ,  Marc GERSPACHER ,  Catherine LEBLANC ,  Bo LIU ,  Edwige Liliane Jeanne LORTHIOIS ,  Rainer MACHAUER ,  Robert MAH ,  Tanja MEISTER ,  Christophe MURA ,  Pascal RIGOLLIER ,  Nadine SCHNEIDER ,  Stefan STUTZ ,  Andrea VAUPEL ,  Nicolas WARIN ,  Rainer WILCKEN ,  Lijun XUE ,  Marie-Anne LOZAC'H ,  Ross STRANG

IPC: C07D403/14

CPC classification number: C07D403/14

Abstract: Provided are crystalline forms of a KRAS G12C inhibitor compound and to processes for their preparation. Furthermore, provided is pharmaceutical composition comprising said crystalline forms, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition can be used as a medicament, in particular for the treatment of cancer, and KRAS G12C-mutant cancer.

公开(公告)号：US20230398117A1

公开(公告)日：2023-12-14

申请号：US18060796

申请日：2022-12-01

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 ,  A61P35/00 ,  C07D487/04 ,  C07D519/00

CPC classification number: A61K31/519 ,  A61P35/00 ,  C07D487/04 ,  C07D519/00

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：US20180086716A1

公开(公告)日：2018-03-29

申请号：US15711984

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: C07D231/56 ,  A61K9/16 ,  A61K9/00 ,  C07D403/12 ,  A61K31/416 ,  C07D401/12 ,  A61K31/454 ,  C07D405/12

CPC classification number: C07D231/56 ,  A61K9/0019 ,  A61K9/1647 ,  A61K31/416 ,  A61K31/454 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12

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.