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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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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：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：US20240182464A1
公开(公告)日：2024-06-06
申请号：US18275379
申请日：2022-02-01
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.
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公开(公告)号：US10392404B2
公开(公告)日：2019-08-27
申请号：US15510613
申请日：2015-09-11
申请人： NOVARTIS AG
发明人： Paul Andrew Barsanti , Matthew T. Burger , Yan Lou , Gisele A. Nishiguchi , Valery Rostislavovich Polyakov , Savithri Ramurthy , Sharadha Subramanian , Benjamin R. Taft , Huw Rowland Tanner , Lifeng Wan
IPC分类号： A61K31/444 , C07D498/08 , C07D401/14 , C07D413/14 , C07D213/74 , C07D401/04 , C07D401/10 , C07D407/14 , C07D411/14 , C07D413/12 , A61K31/4418 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/541 , C07D213/85 , C07D405/12 , C07D405/14 , C07D451/02
摘要： The present invention provides compounds of Formula (I) and (II) as described herein, and salts thereof and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
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公开(公告)号：US10245267B2
公开(公告)日：2019-04-02
申请号：US15601423
申请日：2017-05-22
申请人： NOVARTIS AG
发明人： Robert John Aversa , Paul Andrew Barsanti , Matthew T. Burger , Michael Patrick Dillon , Alan Dipesa , Cheng Hu , Yan Lou , Gisele A. Nishiguchi , Yue Pan , Valery Rostislavovich Polyakov , Savithri Ramurthy , Alice C. Rico , Lina Quattrocchio Setti , Aaron Smith , Sharadha Subramanian , Benjamin R. Taft , Huw Roland Tanner , Lifeng Wan , Naeem Yusuff
IPC分类号： C07D295/04 , A61K31/5377 , C07D413/04 , A61K31/541 , A61K45/06 , C07D213/74 , C07D237/20 , C07D239/42 , C07D239/47 , C07D239/48 , C07D277/42 , C07D401/12 , C07D403/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D493/10 , C07D403/12 , C07D401/14 , C07D405/14 , C07D213/75 , C07D233/88 , C07D401/04 , C07D405/04 , C07D405/12 , C07D241/20 , C07D471/04 , C07D487/04 , C07D263/58 , C07D491/107 , C07D493/04 , C07D495/04 , C07D498/08 , C07D513/04 , A61K31/5375 , C07D213/81 , C07D213/82 , C07D213/84 , C07D237/22 , C07D409/14 , C07D491/048 , A61K31/444 , A61K31/501 , C07B59/00 , C07D237/24 , C07D491/04 , C07D491/08
摘要： The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
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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：US10604547B2
公开(公告)日：2020-03-31
申请号：US16574500
申请日：2019-09-18
申请人： NOVARTIS AG
发明人： Matthew T. Burger , Yunho Jin , Tetsuo Uno
摘要： The invention disclosed herein relates to cytotoxic cyclic peptides of Formula (A), methods of inhibiting RNA polymerase with such cyclic peptides, immunoconjugates comprising such cyclic peptides (i.e Antibody Drug Conjugates), pharmaceutical compositions comprising such cyclic peptides immunoconjugates, compositions comprising such cyclic peptides immunoconjugates with a therapeutic co-agent and methods of treatment using such cyclic peptides immunoconjugates:
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公开(公告)号：US10377770B2
公开(公告)日：2019-08-13
申请号：US16062680
申请日：2016-12-15
申请人： Novartis AG
发明人： Robert John Aversa , Matthew T. Burger , Michael Patrick Dillon , Thomas A. Dineen, Jr. , Rajesh Karki , Savithri Ramurthy , Vivek Rauniyar , Richard Robinson , Patrick James Sarver
IPC分类号： C07D487/04 , C07D491/04 , C07D498/04 , A61P35/00 , C07D491/044
摘要： The present invention provides compounds of Formula (A): (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent, and methods of using the compositions and combinations to treat conditions including cancers.
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公开(公告)号：US10167279B2
公开(公告)日：2019-01-01
申请号：US15510609
申请日：2015-09-11
申请人： NOVARTIS AG
发明人： Robert John Aversa , Matthew T. Burger , Michael Patrick Dillon , Thomas A. Dineen, Jr. , Yan Lou , Gisele A. Nishiguchi , Savithri Ramurthy , Alice C. Rico , Vivek Rauniyar , Martin Sendzik , Sharadha Subramanian , Lina Quattrocchio Setti , Benjamin R. Taft , Huw Rowland Tanner , Lifeng Wan
IPC分类号： C07D405/14 , C07D405/12 , C07D305/06 , A61P35/00 , C07D413/14
摘要： The present invention provides compounds of Formula (I) and (II) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
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