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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：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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3.发明申请公开(公告)号：US20190201404A1
公开(公告)日：2019-07-04
申请号：US16296766
申请日：2019-03-08
发明人： András KOTSCHY , Zoltán Szlávik , Márton Csékei , Attila Paczal , Zoltán Szabó , Szabolcs Sipos , Gábor Radics , Ágnes Proszenyák , Balázs Bálint , Alain Bruno , Olivier Geneste , James Edward Paul Davidson , James Brooke Murray , I-Jen Chen , Françoise Perron-Sierra
IPC分类号： A61K31/519 , A61N5/10 , A61K45/06 , C07D495/04 , A61K31/538 , A61K31/5377 , A61K31/55
CPC分类号： A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/55 , A61K45/06 , A61N5/10 , C07D495/04
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description.Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
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公开(公告)号：US10323041B2
公开(公告)日：2019-06-18
申请号：US15738186
申请日：2016-06-22
发明人： Balazs Balint , Márton Csékei , Zoltán Szabó , Zoltan Szlavik , András Kotschy , Maïa Chanrion , Olivier Geneste , I-Jen Chen , James Edward Paul Davidson , James Brooke Murray , Szabolcs Sipos , Levente Ondi , Ágnes Proszenyák
IPC分类号： C07D491/048 , A61K31/519 , C07D495/04 , C07D403/12 , C07D333/56 , C07D405/04 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D209/12 , C07D307/80 , C07D307/81 , A61P35/02 , A61K45/06
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, W, A and n are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.
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5.发明申请公开(公告)号：US20190248805A1
公开(公告)日：2019-08-15
申请号：US16394308
申请日：2019-04-25
发明人： Balázs Bálint , Márton Csékei , Zoltán Szabó , Zoltán Szlávik , András Kotschy , Maïa Chanrion , Olivier Geneste , I-Jen Chen , James Edward Paul Davidson , James Brooke Murray , Szabolcs Sipos , Levente Ondi , Ágnes Proszenyák
IPC分类号： C07D495/04 , C07D491/048 , C07D491/04 , C07D333/56 , A61P35/02 , C07D307/81 , C07D307/80 , C07D209/12 , C07D403/12 , C07D487/04 , C07D471/04 , C07D409/12 , C07D405/12 , C07D405/04
CPC分类号： C07D495/04 , A61K45/06 , A61K2300/00 , A61P35/02 , C07D209/12 , C07D307/80 , C07D307/81 , C07D333/56 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, W, A and n are as defined in the description.Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.
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公开(公告)号：US09670227B2
公开(公告)日：2017-06-06
申请号：US14576683
申请日：2014-12-19
发明人： András Kotschy , Zoltán Szlávik , Márton Csékei , Attila Paczal , Zoltán Szabó , Szabolcs Sipos , Gábor Radics , Ágnes Proszenyák , Balázs Bálint , Alain Bruno , Olivier Geneste , James Edward Paul Davidson , James Brooke Murray , I-Jen Chen , Françoise Perron-Sierra
IPC分类号： C07D239/00 , C07D333/00 , C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/55 , A61K45/06 , A61N5/10
CPC分类号： A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/55 , A61K45/06 , A61N5/10 , C07D495/04
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
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公开(公告)号：US10457687B2
公开(公告)日：2019-10-29
申请号：US15737783
申请日：2016-06-22
发明人： Zoltán Szlávik , Zoltán Szabó , Márton Csékei , Attila Paczal , András Kotschy , Alain Bruno , Olivier Geneste , I-Jen Chen , James Edward Paul Davidson , James Brooke Murray , Levente Ondi , Gábor Radics , Szabolcs Sipos , Ágnes Proszenyák , Françoise Perron-Sierra , Balázs Bálint
IPC分类号： C07D495/04 , A61K31/519 , A61P37/00 , A61P35/00
摘要： Compounds of formula (I): wherein R1, R2, R5, R6, R7, R12, X, Y, A, E and n are as defined in the description. Medicinal products containing the same which are useful in treating a condition requiring a pro-apoptotic agent.
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公开(公告)号：US10322131B2
公开(公告)日：2019-06-18
申请号：US15738601
申请日：2016-06-22
发明人： Zoltan Szlavik , Attila Paczal , Balazs Balint , András Kotschy , Maïa Chanrion , Olivier Geneste , James Edward Paul Davidson , James Brooke Murray , Szabolcs Sipos , Ágnes Proszenyák
IPC分类号： A61K31/519 , C07D495/04 , A61P35/00 , A61K31/215 , A61K31/381
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, A and n are as defined in the description.
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公开(公告)号：US10278972B2
公开(公告)日：2019-05-07
申请号：US15492306
申请日：2017-04-20
发明人： András Kotschy , Zoltán Szlávik , Márton Csékei , Attila Paczal , Zoltán Szabó , Szabolcs Sipos , Gábor Radics , Ágnes Proszenyák , Balázs Bálint , Alain Bruno , Olivier Geneste , James Edward Paul Davidson , James Brooke Murray , I-Jen Chen , Françoise Perron-Sierra
IPC分类号： A61K31/519 , C07D495/04 , A61K31/5377 , A61K31/538 , A61K31/55 , A61K45/06 , A61N5/10
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
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10.发明申请THIENOPYRIMIDINE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权三硝基嘧啶衍生物及其制备方法及含有它们的药物组合物公开(公告)号：US20150175623A1
公开(公告)日：2015-06-25
申请号：US14576683
申请日：2014-12-19
发明人： András Kotschy , Zoltán Szlávik , Márton Csékei , Attila Paczal , Zoltán Szabó , Szabolcs Sipos , Gábor Radics , Ágnes Proszenyák , Balázs Bálint , Alain Bruno , Olivier Geneste , James Edward Paul Davidson , James Brooke Murray , I-Jen Chen , Françoise Perron-Sierra
IPC分类号： C07D495/04 , A61K45/06 , A61N5/10 , A61K31/55 , A61K31/538 , A61K31/519 , A61K31/5377
CPC分类号： A61K31/519 , A61K31/5377 , A61K31/538 , A61K31/55 , A61K45/06 , A61N5/10 , C07D495/04
摘要： Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description.Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
摘要翻译： 式（I）化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 12，X，A和n如说明书中所定义。 含有该物质的药物可用于治疗涉及细胞凋亡缺陷的病症，如癌症，自身免疫疾病和免疫系统疾病。
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