公开(公告)号：US20240269304A1

公开(公告)日：2024-08-15

申请号：US18038435

申请日：2021-11-23

申请人： Novartis AG ,  Les Laboratoires Servier

发明人： Matthew T. Burger ,  Zhuoliang Chen ,  Joseph Anthony D'Alessio ,  Eric McNeill ,  Katsumasa Nakajima ,  Richard Vaughan Newcombe ,  Mark G. Palermo ,  Bing Yu ,  Qiang Zhang ,  Frédéric Colland ,  James Edward Paul Davidson ,  Lea Delacour ,  Patrice Desos ,  Olivier Geneste ,  Vesela Kostova ,  Andras Kotschy ,  Ana Leticia Maragno ,  James Brooke Murray ,  Tibor Novak ,  Jérôme Benoit Starck

IPC分类号： A61K47/68 ,  A61P35/00

CPC分类号： A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6889 ,  A61P35/00

摘要： Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise a Bcl-xL inhibitor drug moiety. The disclosure farther relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising Bcl-xL inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20230092679A1

公开(公告)日：2023-03-23

申请号：US17613006

申请日：2020-05-19

申请人： NOVARTIS AG ,  LES LABORATOIRES SERVIER

发明人： Matthew T. Burger ,  Maia Chanrion ,  Frédéric Colland ,  Marton Csekei ,  Lea Delacour ,  Patrice Desos ,  Olivier Geneste ,  Jean-Michel Henlin ,  Vesela Kostova ,  Andras Kotschy ,  Ana Leticia Maragno ,  Eric McNeill ,  Mark G. Palermo ,  Francesca Rocchetti ,  Jérôme Starck ,  Bing Yu ,  Qiang Zhang ,  Ágnes Proszenyák ,  Szabolcs Sipos ,  Zhuoliang Chen ,  Katsumasa Nakajima ,  Joseph Anthony D'Alessio

IPC分类号： A61K47/68 ,  A61K47/65 ,  A61K31/505 ,  A61P35/00

摘要： Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20230081720A1

公开(公告)日：2023-03-16

申请号：US17613020

申请日：2020-05-19

申请人： NOVARTIS AG ,  LES LABORATOIRES SERVIER

发明人： Matthew T. Burger ,  Maia Chanrion ,  Frédéric Colland ,  Marton Csekei ,  Lea Delacour ,  Patrice Desos ,  Olivier Geneste ,  Jean-Michel Henlin ,  Vesela Kostova ,  Andras Kotschy ,  Ana Leticia Maragno ,  Eric McNeill ,  Mark G. Palermo ,  Francesca Rocchetti ,  Jérôme Starck ,  Bing Yu ,  Qiang Zhang ,  Ágnes Proszenyák ,  Szabolcs Sipos ,  Zhuoliang Chen ,  Katsumasa Nakajima ,  Joseph Anthony D'Alessio ,  John William Blankenship

IPC分类号： A61K47/68

摘要： Anti-CD74 antibody-drug conjugates are disclosed. The anti-CD74 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD74 antibody or antigen-binding fragment thereof that binds an antigen target, e.g., an antigen expressed on a tumor or other cancer cell. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20240042051A1

公开(公告)日：2024-02-08

申请号：US18038437

申请日：2021-11-23

申请人： Francesca Rocchetti ,  Novartis AG

发明人： Matthew T. Burger ,  Zhuoliang Chen ,  Joseph Anthony D'Alessio ,  Claudia Judith Klinter ,  Eric McNeill ,  Cornelia Anne Mundt ,  Katsumasa Nakajima ,  Richard Vaughan Newcombe ,  Mark G. Palermo ,  Tamas Schweighoffer ,  Bing Yu ,  Katharina Winkelbach ,  Qiang Zhang ,  Laura Bresson ,  Frédéric Colland ,  Ana Leticia Maragno ,  Francesca Rocchetti

IPC分类号： A61K47/68 ,  A61P35/00

CPC分类号： A61K47/6867 ,  A61K47/6889 ,  A61P35/00 ,  A61K47/6803

摘要： Anti-CD48 antibody-drug conjugates are disclosed. The anti-CD48 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD48 antibody or antigen-binding fragment thereof that binds an antigen target, e.g., an antigen expressed on a tumor or other cancer cell. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

公开(公告)号：US20240182464A1

公开(公告)日：2024-06-06

申请号：US18275379

申请日：2022-02-01

申请人： Les Laboratoirens Serviece ,  Novartis AG

发明人： András Herner ,  Piroska Markacz ,  Gang Liu ,  Katsumasa Nakajima ,  Tibor Novak ,  Georges-Alain Franzetti ,  Jérôme-Benoît Starck ,  Frédéric Colland ,  Patrice Desos ,  Attila Paczal ,  Bianka Szokol ,  Mátyás Pál Timari ,  Vilibald Kun ,  Matthew T. Burger ,  Joseph Anthony D'Alessio ,  Katherine Elizabeth Seiss ,  Rany Mathew Thomas ,  Liang Zhao

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07D417/14

CPC分类号： C07D471/04 ,  A61P35/00 ,  C07D417/14

摘要： The present disclosure provides PROTAC compounds represented by Formula (A): D-L-DSM (A), or an enantiomer, a diastereoisomer, and/or a pharmaceutically acceptable salt of any one of the foregoing, wherein: DSM is a degradation signaling compound {e.g., an E3 ubiquitin ligase recruitment ligand, such as a CRBN ligand or a VHL ligand) covalently attached to a linker L; L is a linker that covalently attaches DSM to D; and D is a Bcl-xL inhibitor compound of Formula (I) or Formula (II) covalently attached to the linker L: (I); (II) wherein the definitions for the variables are described herein. Also provided are pharmaceutical compositions comprising the PROTAC compounds of the present disclosure and methods of use and methods of making thereof.

公开(公告)号：US11377656B2

公开(公告)日：2022-07-05

申请号：US16083327

申请日：2017-03-08

申请人： Novartis AG

发明人： Shari Lynn Caplan ,  Katsumasa Nakajima

IPC分类号： C07H21/04 ,  C12N15/11 ,  C07H21/02 ,  C12N15/87

摘要： This invention provides messenger RNA (mRNA) molecules comprising an open reading frame that encodes a protein of interest, wherein said modified RNA comprises a modified nucleoside selected from the group consisting of: (I), (II), and (III), gene therapy vectors comprising same, methods of synthesizing same, and methods for gene replacement, gene therapy, gene transcription silencing, and the delivery of therapeutic proteins to tissue in vivo, comprising the molecules. The present invention also provides methods of reducing the immunogenicity of mRNA molecules.

公开(公告)号：US20240270738A1

公开(公告)日：2024-08-15

申请号：US18602126

申请日：2024-03-12

申请人： NOVARTIS AG

发明人： Christopher ADAIR ,  Katsumasa Nakajima ,  Rukundo Ntaganda ,  Julien Papillon ,  Troy Douglas Smith

IPC分类号： C07D417/12 ,  A61K45/06

CPC分类号： C07D417/12 ,  A61K45/06

摘要： A method of preparing compound of Formula (1), or a pharmaceutically acceptable salt thereof,




wherein R1 through R6 are as defined herein.

公开(公告)号：US11958846B2

公开(公告)日：2024-04-16

申请号：US17268512

申请日：2019-08-12

申请人： Novartis AG

发明人： Christopher Adair ,  Katsumasa Nakajima ,  Rukundo Ntaganda ,  Julien Papillon ,  Troy Douglas Smith

IPC分类号： C07D417/12 ,  A61K45/06

CPC分类号： C07D417/12 ,  A61K45/06

摘要： A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a BRM-mediated and/or BRG1-mediated disease or disorder: Formula (I) wherein R1 through R6 are as defined herein.

公开(公告)号：US11970497B2

公开(公告)日：2024-04-30

申请号：US16973836

申请日：2020-07-31

申请人： Novartis AG

发明人： Chris Adair ,  Tracy Chen ,  Jian Ding ,  Christy Fryer ,  Yuko Isome ,  Marie-Helene Larraufie ,  Katsumasa Nakajima ,  Nik Savage ,  Ariel Sterling Twomey

IPC分类号： C07D471/10 ,  A61P35/00 ,  A61K31/4747

CPC分类号： C07D471/10 ,  A61P35/00 ,  A61K31/4747

摘要： The present invention relates to novel tricyclic compounds that are AKR1C3 dependent KARS inhibitor, processes for their preparation, pharmaceutical compositions, and medicaments containing them, and their use in diseases and disorders mediated by an AKR1C3 dependent KARS inhibitor.