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：US20190211022A1

公开(公告)日：2019-07-11

申请号：US16311638

申请日：2017-06-19

Applicant: NOVARTIS AG

Inventor： Ying HUANG ,  Bo LIU ,  Liang MAO ,  Long WANG ,  Liladhar Murlidhar WAYKOLE ,  Lijun ZHANG

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P35/02 ,  C07B2200/13

Abstract: Provided herein are crystalline forms of a triazolopyrimidine compound, which is useful for treating a PRC2-mediated disease or disorder.

公开(公告)号：US20250011307A1

公开(公告)日：2025-01-09

申请号：US18687609

申请日：2022-08-30

Applicant: Novartis AG

Inventor： Runyan LI ,  Bo LIU ,  Michael MUTZ ,  Lina YUAN ,  Yingcong ZHOU

IPC: C07D405/04 ,  A61K31/343 ,  A61K31/4025 ,  C07D307/81

Abstract: The present invention generally relates to crystalline polymorphic forms of the biaryl YAP/TAZ-TEAD protein-protein interaction inhibitors 4-((2S,4S)-5-Chloro-6-fluoro-2-phenyl-2-((S)-pyrrolidin-2-yl)-2,3-dihydrobenzofuran-4-yl)-5-fluoro-6-(2-hydroxyethoxy)-N-methylnicotinamide and 2-((2S,3S,4S)-5-Chloro-6-fluoro-3-methyl-2-((methylamino)methyl)-2-phenyl-2,3-dihydrobenzofuran-4-yl)-3-fluoro-4-methoxybenzamide and salts thereof, as well as methods of using the forms in the treatment of cancer.

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：US20250092016A1

公开(公告)日：2025-03-20

申请号：US18580986

申请日：2022-07-20

Applicant: NOVARTIS AG

Inventor： Denghui BAO ,  Fengfeng GUO ,  Matthew James HESSE ,  Viktor HORNAK ,  Sajan JOSEPH ,  Thomas Martin KIRRANE, JR. ,  Haiyao LIN ,  Bo LIU ,  Yanan MIAO ,  Heinz Ernst MOSER ,  Julien PAPILLON ,  Yang QU ,  Lei SHI ,  Jun YUAN ,  Teng ZHANG

IPC: C07D401/14 ,  A61K31/4725 ,  A61K31/501 ,  A61K31/506 ,  A61P31/14 ,  C07D401/04

Abstract: Provided herein are compounds and compositions for treating, managing or preventing coronaviral related diseases. In particular, provided herein are compounds which are inhibitors of SARS-CoV-2 main protease (Mpro), pharmaceutical compositions comprising such compounds, method for synthesizing such compounds and methods of using such compounds and compositions for the treatment, management or prevention of coronaviral related diseases.