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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
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.
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公开(公告)号：US20230092679A1
公开(公告)日：2023-03-23
申请号：US17613006
申请日：2020-05-19
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.
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公开(公告)号：US10287266B2
公开(公告)日：2019-05-14
申请号：US15736925
申请日：2016-06-15
申请人： NOVARTIS AG
发明人： Zhuoliang Chen , Jorge Garcia Fortanet , Andriana Jouk , Rajesh Karki , Matthew J. LaMarche , Gang Liu , Mark G. Palermo , Lawrence Blas Perez , Patrick James Sarver , Michael David Shultz , Martin Sendzik , Bakary-Barry Toure , Bing Yu
IPC分类号： C07D401/14 , C07D401/04 , C07D471/10 , C07D491/107 , C07D498/10
摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2, R4a, R4b, R5a, R5b, R6a and R6b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
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公开(公告)号：USRE46942E1
公开(公告)日：2018-07-10
申请号：US15786125
申请日：2017-10-17
申请人： NOVARTIS AG
发明人： Christine Hiu-Tung Chen , Donovan Noel Chin , Lucien V. DiPietro , Jianmei Fan , Mark G. Palermo , Michael David Shultz , Bakary-Barry Toure
IPC分类号： C07D491/052 , C07D493/04 , C07D401/12 , C07D401/04 , C07D401/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
CPC分类号： C07D401/04 , C07D401/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/052 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
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公开(公告)号：US20230081720A1
公开(公告)日：2023-03-16
申请号：US17613020
申请日：2020-05-19
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.
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公开(公告)号：US20240269304A1
公开(公告)日：2024-08-15
申请号：US18038435
申请日：2021-11-23
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
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.
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