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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
Applicant: Francesca Rocchetti , Novartis AG
Inventor： 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 classification number: A61K47/6867 , A61K47/6889 , A61P35/00 , A61K47/6803
Abstract: 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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2.发明授权Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders 有权苯并噻吩衍生物及其组合物作为选择性雌激素受体降解物公开(公告)号：US09321746B2
公开(公告)日：2016-04-26
申请号：US14768341
申请日：2014-02-12
Applicant: Novartis AG
Inventor： Heather Elizabeth Burks , Michael A. Dechantsreiter , Guo He , Jill Nunez , Stefan Peukert , Clayton Springer , Yingchuan Sun , Noel Marie-France Thomsen , George Scott Tria , Bing Yu
IPC: A61K31/00 , C07D333/64 , A61K31/381 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/4436 , A61K31/506 , A61K45/06 , C07D333/66 , C07D409/12 , C07D413/04 , C07D413/12 , C07D409/04 , C07D409/10 , C07D417/12 , A61K31/397 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/428 , A61K31/5377
CPC classification number: A61K31/381 , A61K31/397 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/428 , A61K31/4436 , A61K31/4745 , A61K31/506 , A61K31/5377 , A61K45/06 , A61P35/00 , C07D333/64 , C07D333/66 , C07D409/04 , C07D409/10 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12
Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. 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 aberrant estrogen receptor activity.
Abstract translation: 本发明涉及式I化合物：其中n，m，X，Y 1，R 1，R 2，R 3，R 4和R 5在发明概述中定义; 能够成为雌激素受体的有效拮抗剂和降解物。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与异常雌激素受体活性相关的疾病或病症的方法。
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3.发明授权公开(公告)号：US09931317B2
公开(公告)日：2018-04-03
申请号：US15399562
申请日：2017-01-05
Applicant: NOVARTIS AG
Inventor： Heather Elizabeth Burks , Michael A. Dechantsreiter , Guo He , Jill Nunez , Stefan Peukert , Clayton Springer , Yingchuan Sun , Noel Marie-France Thomsen , George Scott Tria , Bing Yu
IPC: A61K31/381 , C07D333/64 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/4436 , A61K31/506 , A61K45/06 , C07D333/66 , C07D409/12 , C07D413/04 , C07D413/12 , C07D409/04 , C07D409/10 , C07D417/12 , A61K31/397 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/428 , A61K31/5377 , A61K31/4745
CPC classification number: A61K31/381 , A61K31/397 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/428 , A61K31/4436 , A61K31/4745 , A61K31/506 , A61K31/5377 , A61K45/06 , A61P35/00 , C07D333/64 , C07D333/66 , C07D409/04 , C07D409/10 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12
Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. 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 aberrant estrogen receptor activity.
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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
Applicant: Novartis AG , Les Laboratoires Servier
Inventor： 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 classification number: A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6889 , A61P35/00
Abstract: 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
Applicant: NOVARTIS AG , LES LABORATOIRES SERVIER
Inventor： 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: A61K47/68 , A61K47/65 , A61K31/505 , A61P35/00
Abstract: 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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Patent Agency Ranking
公开(公告)号：US10287266B2
公开(公告)日：2019-05-14
申请号：US15736925
申请日：2016-06-15
Applicant: NOVARTIS AG
Inventor： 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: C07D401/14 , C07D401/04 , C07D471/10 , C07D491/107 , C07D498/10
Abstract: 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：US11905283B2
公开(公告)日：2024-02-20
申请号：US17130374
申请日：2020-12-22
Applicant: Novartis AG
Inventor： Zhuoliang Chen , Jorge Garcia Fortanet , Rajesh Karki , Matthew J. Lamarche , Dyuti Majumdar , Lawrence Blas Perez , Martin Sendzik , Troy Douglas Smith , Fan Yang , Bing Yu
IPC: C07D471/04 , C07D401/14 , C07D403/14 , C07D455/02 , C07D487/04 , C07D495/04 , C07D513/04 , C07D519/00
CPC classification number: C07D471/04 , C07D401/14 , C07D403/14 , C07D455/02 , C07D487/04 , C07D495/04 , C07D513/04 , C07D519/00
Abstract: The present invention relates to compounds of formula I:
in which Y1, Y2, R1, R2 and R3 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.-
公开(公告)号：US20230081720A1
公开(公告)日：2023-03-16
申请号：US17613020
申请日：2020-05-19
Applicant: NOVARTIS AG , LES LABORATOIRES SERVIER
Inventor： 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: A61K47/68
Abstract: 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：US10934285B2
公开(公告)日：2021-03-02
申请号：US16309076
申请日：2017-06-12
Applicant: Novartis AG
Inventor： Zhuoliang Chen , Jorge Garcia Fortanet , Rajesh Karki , Matthew J. Lamarche , Dyuti Majumdar , Lawrence Blas Perez , Martin Sendzik , Troy Douglas Smith , Fan Yang , Bing Yu
IPC: C07D487/14 , C07D471/04 , C07D401/14 , C07D403/14 , C07D455/02 , C07D487/04 , C07D495/04 , C07D513/04 , C07D519/00
Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, R1, R2 and R3 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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10.发明授权公开(公告)号：US10058534B2
公开(公告)日：2018-08-28
申请号：US15898561
申请日：2018-02-17
Applicant: NOVARTIS AG
Inventor： Heather Elizabeth Burks , Michael A. Dechantsreiter , Guo He , Jill Nunez , Stefan Peukert , Clayton Springer , Yingchuan Sun , Noel Marie-France Thomsen , George Scott Tria , Bing Yu
IPC: A61K31/381 , A61K45/06 , A61K31/506 , A61K31/4436 , A61K31/4245 , A61K31/422 , A61K31/4196 , C07D413/12 , C07D413/04 , C07D409/12 , C07D333/66 , C07D333/64 , A61K31/5377 , A61K31/404 , A61K31/41 , A61K31/428 , A61K31/397 , A61K31/4025 , A61K31/4745 , C07D417/12 , C07D409/10 , C07D409/04
CPC classification number: A61K31/381 , A61K31/397 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/428 , A61K31/4436 , A61K31/4745 , A61K31/506 , A61K31/5377 , A61K45/06 , A61P35/00 , C07D333/64 , C07D333/66 , C07D409/04 , C07D409/10 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12
Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. 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 aberrant estrogen receptor activity.
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