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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：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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公开(公告)号：US20240252668A1
公开(公告)日：2024-08-01
申请号：US18286664
申请日：2022-04-15
申请人： Anne-Sophie BLUEMMEL , Kathrin BUNTIN , Joseph Anthony D'ALESSIO , Liqiong FAN , Boris FESSLER , Doris GABRIEL , Dominik HAINZL , Keith HOFFMASTER , Shwetha IYER , Eshita KHERA , Eusebio Manchado ROBLES , Pierre MAUDENS , Dominik PISTORIUS , Roee RAMOT , Vincent ROMANET , Kuno WUERSCH , Padmaja YERRAMILLI-RAO , Novartis AG
发明人： Liqiong Fan , Dominik Hainzl , Roee Ramot , Shwetha Iyer , Joseph Anthony D'Alessio , Kuno Wuersch , Dominik Pistorius , Eusebio Manchado Robles , Kathrin Buntin , Doris Gabriel , Boris Fessler , Pierre Maudens , Vincent Romanet , Anne-Sophie Bluemmel , Keith Hoffmaster , Eshita Khera , Padmaja Yerramilli-Rao
IPC分类号： A61K47/68 , A61P35/00 , C07K11/02 , C07K14/47 , C07K16/28 , C12N9/00 , C12N9/02 , C12N9/04 , C12N9/18 , C12N15/52 , C12P21/02 , C12R1/01 , G01N33/574
CPC分类号： A61K47/6849 , A61K47/6811 , A61K47/6865 , A61P35/00 , C07K11/02 , C07K14/4722 , C07K16/28 , C12N9/0006 , C12N9/0073 , C12N9/18 , C12N9/93 , C12N15/52 , C12P21/02 , C12Y301/01001 , G01N33/57492 , C12R2001/01
摘要： This application discloses microorganisms and methods of producing GNAQ/GNA11 inhibitors and methods of making antibody drug conjugates of anti-PMEL17 antibodies or antigen binding fragments conjugated to a GNAQ/GNA11 inhibitor. The disclosure also relates to formulations comprising antibody drug conjugates of anti-PMEL 17 antibodies or antigen binding fragments conjugated to a GNAQ/GNA1 inhibitor and methods of treating or preventing cancer using the formulations.
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公开(公告)号：US11779649B2
公开(公告)日：2023-10-10
申请号：US16718866
申请日：2019-12-18
申请人： Novartis AG
发明人： Matthew Burger , Joseph Anthony D'Alessio , Tony Fleming , Vivek Rauniyar , Eusebio Manchado Robles , Christian Kunz , Markus Waldhuber
IPC分类号： A61K47/68 , A61P35/00 , A61K31/4745 , C07K16/18 , A61K45/06
CPC分类号： A61K47/6803 , A61K31/4745 , A61P35/00 , C07K16/18 , A61K45/06
摘要： This application discloses anti-PMEL17 antibodies, antigen binding fragments thereof, and antibody drug conjugates comprising antibodies or antigen binding fragments conjugated to a GNAQ/GNA11 inhibitor. The application also discloses methods of treating or preventing cancer using the antibodies, antigen binding fragments, and antibody drug conjugates. Also disclosed herein are methods of making the antibodies, antigen binding fragments, and antibody drug conjugates, and methods of using the antibodies and antigen binding fragments as diagnostic reagents.
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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：US20240189439A1
公开(公告)日：2024-06-13
申请号：US18454457
申请日：2023-08-23
申请人： Novartis AG
发明人： Matthew Burger , Joseph Anthony D'Alessio , Tony Fleming , Vivek Rauniyar , Eusebio Manchado Robles , Christian Kunz , Markus Waldhuber
IPC分类号： A61K47/68 , A61K31/4745 , A61P35/00 , C07K16/18
CPC分类号： A61K47/6803 , A61K31/4745 , A61P35/00 , C07K16/18 , A61K45/06
摘要： This application discloses anti-PMEL17 antibodies, antigen binding fragments thereof, and antibody drug conjugates of said antibodies or antigen binding fragments conjugated to a GNAQ/GNA11 inhibitor. The invention also relates to methods of treating or preventing cancer using the antibodies, antigen binding fragments, and antibody drug conjugates. Also disclosed herein are methods of making the antibodies, antigen binding fragments, and antibody drug conjugates, and methods of using the antibodies and antigen binding fragments as diagnostic reagents.
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公开(公告)号：US11999786B2
公开(公告)日：2024-06-04
申请号：US17534126
申请日：2021-11-23
申请人： Novartis AG
发明人： Joseph Anthony D'Alessio , Claudia Judith Klinter , Cornelia Anne Mundt , Richard Vaughan Newcombe , Tamás Schweighoffer , Katharina Winkelbach
CPC分类号： C07K16/2803 , A61K45/06 , A61K47/6803 , A61K47/6851 , C07K2317/565 , C07K2317/92
摘要： Disclosed herein are antibodies, antigen binding fragments thereof, and antibody drug conjugates thereof that bind human CD48. Also disclosed are pharmaceutical compositions comprising the antibodies, antigen binding fragments thereof, and antibody drug conjugates thereof; and methods of making and using such pharmaceutical compositions for treating cancer in a patient in need of treatment.
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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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