公开(公告)号：US20210299100A1

公开(公告)日：2021-09-30

申请号：US17201268

申请日：2021-03-15

Applicant: Novartis AG

Inventor： Vincent BORDAS ,  Cara BROCKLEHURST ,  Patrick CHENE ,  Zhongbo FEI ,  Pascal FURET ,  Vito GUAGNANO ,  Patricia IMBACH-WEESE ,  Joerg KALLEN ,  Mickael LE DOUGET ,  Jialiang LI ,  Wei LI ,  Edwige Liliane Jeanne LORTHIOIS ,  Joseph McKENNA ,  Bahaa SALEM ,  Tobias SCHMELZLE ,  Holger SELLNER ,  Nicolas SOLDERMANN ,  Markus VOEGTLE ,  Markus WARTMANN

IPC: A61K31/4155 ,  C07D307/81 ,  C07D405/12 ,  A61K31/343 ,  A61K31/443 ,  A61K31/426 ,  C07D417/04 ,  C07D407/04 ,  A61K31/357 ,  C07D405/04 ,  A61K31/403 ,  A61K31/4525 ,  A61K31/351 ,  C07D407/12 ,  A61K31/506 ,  A61K31/41 ,  A61K31/4025 ,  A61K31/4439 ,  C07D405/14 ,  A61P35/00

Abstract: The present invention provides a compound of formula (1) or a pharmaceutically acceptable salt 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：US20240382457A1

公开(公告)日：2024-11-21

申请号：US18776928

申请日：2024-07-18

Applicant: Novartis AG

Inventor： Vincent BORDAS ,  Cara BROCKLEHURST ,  Patrick CHENE ,  Pascal FURET ,  Vito GUAGNANO ,  Patricia IMBACH-WEESE ,  Joerg KALLEN ,  Mickael LE DOUGET ,  Edwige Liliane Jeanne LORTHIOIS ,  Joseph MCKENNA ,  Bahaa SALEM ,  Tobias SCHMELZLE ,  Holger SELLNER ,  Nicolas SOLDERMANN ,  Markus VOEGTLE ,  Markus WARTMANN

IPC: A61K31/4155 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/41 ,  A61K31/426 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/506 ,  A61P35/00 ,  C07D307/81 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D417/04

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt 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：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：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：US20220401422A1

公开(公告)日：2022-12-22

申请号：US17241981

申请日：2021-04-27

Applicant: Novartis AG

Inventor： Robin Alec FAIRHURST ,  Christine FRITSCH ,  Marc GERSPACHER ,  Jürgen Hans-Hermann HINRICHS ,  Jean-Baptiste Georges Armand LANGLOIS ,  Catherine LEBLANC ,  Tengfei LI ,  Edwige Liliane Jeanne LORTHIOIS ,  Christophe MURA ,  Cristina Montserrat NIETO-OBERHUBER ,  Milen TODOROV ,  Andrea VAUPEL ,  Nicolas WARIN ,  Rainer WILCKEN

IPC: A61K31/437 ,  A61P35/00 ,  C07D471/10 ,  C07D471/20 ,  A61K31/4747 ,  C07D491/20 ,  C07D491/22 ,  A61K31/4375 ,  C07D495/20 ,  C07D495/22 ,  A61K31/436 ,  A61K31/675 ,  A61K31/155 ,  A61K31/5377 ,  A61K31/519 ,  A61K31/635 ,  A61K31/53

Abstract: The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt form 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 the use of the compounds in the treatment of disease.

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.