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公开(公告)号：US10889866B2
公开(公告)日：2021-01-12
申请号：US15755225
申请日：2016-08-30
发明人： Lihua Yu , Kian Huat Lim , Jacob D. Feala , Silvia Buonamici , Yoshiharu Mizui , Peter G. Smith , Ping Zhu , Eunice Sun Park , Michael W. Seiler , Marco Peter Fekkes
IPC分类号： C12Q1/6886 , A61P35/00 , A61K31/4545 , A61K31/495 , A61K31/55 , C12Q1/02 , C12Q1/6806 , C12Q1/6841
摘要： Splice variants associated with neomorphic SF3B1 mutations are described herein. This application also relates to methods of detecting the described splice variants, and uses for diagnosing cancer, evaluating modulators of SF3B1, and methods of treating cancer associated with mutations in SF3B1.
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公开(公告)号：US11945807B2
公开(公告)日：2024-04-02
申请号：US17661909
申请日：2022-05-03
发明人： Ermira Pazolli , Silvia Buonamici , Thiwanka Samarakoon , Sudeep Prajapati , Nathan Fishkin , James Palacino , Michael Seiler , Ping Zhu , Andrew Cook , Peter Smith , Xiang Liu , Shelby Ellery , Dominic Reynolds , Lihua Yu , Zhenhua Wu , Shouyong Peng , Nicholas Calandra , Megan Sheehan , Yonghong Xiao
IPC分类号： C07D405/12 , A61K9/127 , A61K9/51 , A61K31/365 , A61K31/496 , A61K39/00 , A61K39/395 , A61K45/06 , A61K47/60 , A61K47/68 , A61P35/00 , C07D313/00 , C07D405/06 , C07K16/24 , C07K16/28 , C07K16/30 , C07K16/32 , C07K16/40 , C12Q1/6886 , G01N33/50 , G01N33/574
CPC分类号： C07D405/12 , A61K9/127 , A61K9/51 , A61K31/365 , A61K31/496 , A61K39/0011 , A61K39/3955 , A61K39/39558 , A61K45/06 , A61K47/60 , A61K47/6845 , A61K47/6849 , A61K47/6851 , A61K47/6857 , A61K47/6869 , A61K47/6871 , A61K47/6889 , A61P35/00 , C07D313/00 , C07D405/06 , C07K16/24 , C07K16/28 , C07K16/2803 , C07K16/2818 , C07K16/2827 , C07K16/2896 , C07K16/3007 , C07K16/3092 , C07K16/32 , C07K16/40 , C12Q1/6886 , G01N33/5011 , G01N33/574 , A61K2039/505 , A61K2039/53 , A61K2039/545 , C07K2317/565 , C07K2317/76 , C12Q2600/106 , G01N2500/10
摘要： Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.
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公开(公告)号：US20210130909A1
公开(公告)日：2021-05-06
申请号：US17098940
申请日：2020-11-16
发明人： Lihua Yu , Kian Huat Lim , Jacob D. Feala , Silvia Buonamici , Yoshiharu Mizui , Peter G. Smith , Ping Zhu , Eunice Sun Park , Michael W. Seiler , Marco Peter Fekkes
IPC分类号： C12Q1/6886 , A61P35/00 , A61K31/4545 , A61K31/495 , A61K31/55 , C12Q1/02 , C12Q1/6806
摘要： Splice variants associated with neomorphic SF3B1 mutations are described herein. This application also relates to methods of detecting the described splice variants, and uses for diagnosing cancer, evaluating modulators of SF3B1, and methods of treating cancer associated with mutations in SF3B1.
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公开(公告)号：US20190100513A1
公开(公告)日：2019-04-04
申请号：US15529798
申请日：2016-11-17
发明人： Gregg F. Keaney , John Wang , Baudouin Gerard , Kenzo Arai , Xiang Liu , Guo Zhu Zheng , Kazunobu Kira , Parcharee Tivitmahaisoon , Sudeep Prajapati , Nicholas C. Gearhart , Yoshihiko Kotake , Satoshi Nagao , Regina Mikie Kanada Sonobe , Masayuki Miyano , Norio Murai , Silvia Buonamici , Lihua Yu , Eunice Sun Park , Betty Chan , Peter G. Smith , Michael P. Thomas , Ermira Pazolli , Kian Huat Lim , Atsushi Endo , Arani Chanda
IPC分类号： C07D405/14 , A61P35/02
摘要： The present disclosure provides a novel solid state form of pladienolide pyridine compounds, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.
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公开(公告)号：US11998544B2
公开(公告)日：2024-06-04
申请号：US17059876
申请日：2019-05-31
发明人： Ermira Pazolli , Silvia Buonamici , James Palacino , Michael Seiler , Ping Zhu , Evan Barry , Lihua Yu
IPC分类号： A61K31/496 , A61K35/17 , A61K38/19 , A61K38/20 , A61K38/21 , A61K39/00 , A61K39/39 , A61K39/395 , A61K47/68
CPC分类号： A61K31/496 , A61K35/17 , A61K38/191 , A61K38/2013 , A61K38/2066 , A61K38/208 , A61K38/2086 , A61K38/217 , A61K39/0011 , A61K39/39 , A61K39/3955 , A61K47/6803 , A61K2039/6031 , A61K2039/6037 , A61K2039/6056 , A61K2039/6081
摘要： This disclosure relates to methods for the treatment of neoplastic disorders by administering Compound 1, or a pharmaceutically acceptably salt thereof, on its own and/or as part of a conjugate or composition, and inducing production of at least one neoantigen.
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公开(公告)号：US11761045B2
公开(公告)日：2023-09-19
申请号：US17098940
申请日：2020-11-16
发明人： Lihua Yu , Kian Huat Lim , Jacob D. Feala , Silvia Buonamici , Yoshiharu Mizui , Peter G. Smith , Ping Zhu , Eunice Sun Park , Michael W. Seiler , Marco Peter Fekkes
IPC分类号： C12Q1/6886 , A61P35/00 , A61K31/4545 , A61K31/495 , A61K31/55 , C12Q1/02 , C12Q1/6806 , C12Q1/6841
CPC分类号： C12Q1/6886 , A61K31/4545 , A61K31/495 , A61K31/55 , A61P35/00 , C12Q1/025 , C12Q1/6806 , C12Q1/6841 , C12Q2600/106 , C12Q2600/158
摘要： Splice variants associated with neomorphic SF3B1 mutations are described herein. This application also relates to methods of detecting the described splice variants, and uses for diagnosing cancer, evaluating modulators of SF3B1, and methods of treating cancer associated with mutations in SF3B1.
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公开(公告)号：US09481669B2
公开(公告)日：2016-11-01
申请号：US14710687
申请日：2015-05-13
发明人： Gregg F. Keaney , John Wang , Baudouin Gerard , Kenzo Arai , Xiang Liu , Guo Zhu Zheng , Kazunobu Kira , Parcharee Tivitmahaisoon , Sudeep Prajapati , Nicholas C. Gearhart , Yoshihiko Kotake , Satoshi Nagao , Regina Mikie Kanada Sonobe , Masayuki Miyano , Norio Murai , Silvia Buonamici , Lihua Yu , Eunice Sun Park , Betty Chan , Peter G. Smith , Michael P. Thomas , Ermira Pazolli , Kian Huat Lim
IPC分类号： C07D405/06 , C07D405/14 , A61K31/496
CPC分类号： C07D405/14 , C07D405/06
摘要： The present invention provides novel pladienolide pyridine compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.
摘要翻译： 本发明提供新颖的扁桃苷内酰吡啶化合物，含有这些化合物的药物组合物，以及使用该化合物作为治疗剂的方法。 这些化合物可用于治疗癌症，特别是癌症，其中靶向剪接体的试剂和其中的突变已知是有用的。
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公开(公告)号：US11524009B2
公开(公告)日：2022-12-13
申请号：US16760313
申请日：2018-10-30
发明人： Daniel Aird , Laura Corson , Ping Zhu , Markus Warmuth , Silvia Buonamici , Peter Gerard Smith , Peter Fekkes
IPC分类号： A61K31/496 , A61P35/00 , A61K31/05 , A61K31/11 , A61K31/166 , A61K31/343 , A61K31/352 , A61K31/395 , A61K31/404 , A61K31/426 , A61K31/4355 , A61K31/4725 , A61K31/495 , A61K31/5355
摘要： The present disclosure provides pharmaceutical combinations comprising at least one spliceosome modulator and at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors. Also provided are methods of treating cancer comprising administering a therapeutically effective amount of at least one spliceosome modulator and a therapeutically effective amount of at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors.
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公开(公告)号：US11352348B2
公开(公告)日：2022-06-07
申请号：US17247117
申请日：2020-11-30
发明人： Ermira Pazolli , Silvia Buonamici , Thiwanka Samarakoon , Sudeep Prajapati , Nathan Fishkin , James Palacino , Michael Seiler , Ping Zhu , Andrew Cook , Peter Smith , Xiang Liu , Shelby Ellery , Dominic Reynolds , Lihua Yu , Zhenhua Wu , Shouyong Peng , Nicholas Calandra , Megan Sheehan , Yonghong Xiao
IPC分类号： C07D405/12 , A61P35/00 , A61K47/68 , A61K47/60 , A61K9/127 , A61K9/51 , A61K31/365 , A61K31/496 , A61K39/00 , A61K39/395 , A61K45/06 , C07D313/00 , C07D405/06 , C07K16/24 , C07K16/28 , C07K16/30 , C07K16/32 , C07K16/40 , C12Q1/6886 , G01N33/50 , G01N33/574
摘要： Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.
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公开(公告)号：US10745387B2
公开(公告)日：2020-08-18
申请号：US15529798
申请日：2016-11-17
发明人： Gregg F. Keaney , John Wang , Baudouin Gerard , Kenzo Arai , Xiang Liu , Guo Zhu Zheng , Kazunobu Kira , Parcharee Tivitmahaisoon , Sudeep Prajapati , Nicholas C. Gearhart , Yoshihiko Kotake , Satoshi Nagao , Regina Mikie Kanada Sonobe , Masayuki Miyano , Norio Murai , Silvia Buonamici , Lihua Yu , Eunice Sun Park , Betty Chan , Peter G. Smith , Michael P. Thomas , Ermira Pazolli , Kian Huat Lim , Atsushi Endo , Arani Chanda
IPC分类号： A61K31/496 , C07D295/182 , C07D405/14 , C07D405/06 , A61P35/02
摘要： The present disclosure provides a novel solid state form of pladienolide pyridine compounds having Formula I, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.
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