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公开(公告)号：US20200179389A1
公开(公告)日：2020-06-11
申请号：US16608489
申请日：2018-04-26
申请人： The Brigham and Women's Hospital Inc. , The United States of America, as Represented By the Secretary, Deprt. of Health and Human Services
发明人： Paul B. Yu , Wenwei Huang , Philip Edward Sanderson , Jian-Kang Jiang , Khalida Shamim , Wei Zheng , Xiuli Huang , Gregory Tawa , Arthur Lee , Asaf Alimardanov , Junfeng Huang
IPC分类号： A61K31/519 , A61K45/06 , A61P19/08 , C07D487/04 , C07D519/00 , C07F9/6561 , A61K31/551 , A61K31/5377 , A61K31/675
摘要： The present invention provides small-molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to treat subjects with Sjögren's syndrome, or diffuse intrinsic pontine glioma (DIPG).
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公开(公告)号：US20160046633A1
公开(公告)日：2016-02-18
申请号：US14776302
申请日：2014-03-13
申请人： THE BRIGHAM AND WOMEN'S HOSPITAL, INC. , THE U.S.A., AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH & HUMAN SERVICES
发明人： Asaf Alimardanov , Gregory D. Cuny , Gurmit Singh Grewal , Arthur Lee , John C. McKew , Agustin H. Mohedas , Min Shen , Xin Xu , Paul B. Yu
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.
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公开(公告)号：US11027014B2
公开(公告)日：2021-06-08
申请号：US16260914
申请日：2019-01-29
发明人： Lai-Ming Yung , Paul B. Yu
IPC分类号： A61K39/395 , A61P11/00 , C07K16/22 , C07K14/475 , C07K14/495 , A61K39/00 , A61K38/18
摘要： The technology described herein is directed to methods and compositions for the treatment of hypertension, e.g. pulmonary arterial hypertension, relating to inhibition of TGFβ1, TGFβ3, and/or GDF-15.
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4.发明申请公开(公告)号：US20190231779A1
公开(公告)日：2019-08-01
申请号：US16380525
申请日：2019-04-10
发明人： Paul B. Yu , Jana Bagarova , Devaveena Dey
IPC分类号： A61K31/517 , C07D487/04 , C07D491/056 , A61K45/06 , C07D401/12 , C07D405/14
CPC分类号： A61K31/517 , A61K45/06 , A61K2300/00 , C07D401/12 , C07D405/14 , C07D487/04 , C07D491/056
摘要： Provided herein are methods and compositions for the treatment and/or prevention of abnormal bone formation in a soft tissue. In certain embodiments, the methods and compositions treat and/or prevent a disease or disorder comprising abnormal bone formation in soft tissue. Exemplary diseases or disorders that can be treated with the methods and compositions described herein include, but are not limited to, heterotopic ossification diseases such as fibrodysplasia ossificans progressive, anklyosing spondylosis, traumatic heterotopic ossification, burn- or blast-injury associated heterotopic ossification, and joint replacement surgery associated heterotopic ossification.
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公开(公告)号：US09045484B2
公开(公告)日：2015-06-02
申请号：US13940641
申请日：2013-07-12
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519
摘要： The present invention provides pyridinyl-substituted pyrazolyl pyrimidine small molecule inhibitors of bone morphogenetic protein (BMP) signaling having the structure of formula (I), wherein variables A, B, E, F, X, Y, Z, Ar, L1, R4 and R15 are as defined in the specification. The compounds of the invention are useful in modulating cell growth, differentiation, proliferation, and apoptosis, and thus are useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation.
摘要翻译： 本发明提供具有式（I）结构的吡啶基取代的吡唑基嘧啶小分子抑制剂骨形态发生蛋白（BMP）信号转导酶，其中变量A，B，E，F，X，Y，Z，Ar，L1，R4 和R 15如说明书中所定义。 本发明的化合物可用于调节细胞生长，分化，增殖和凋亡，因此可用于治疗与BMP信号相关的疾病或病症，包括炎症，心血管疾病，血液病，癌症和骨骼疾病 用于调节细胞分化和/或增殖。
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公开(公告)号：US20240083991A1
公开(公告)日：2024-03-14
申请号：US18326335
申请日：2023-05-31
发明人： Paul B. Yu , James Reasoner Apgar , Susan Adam Benard , Stephen Peter Berasi , Christine Huard , Oleg Victorovich Kovalenko , Lidia Mosyak , Xianchun Tang , Kathleen Elisabeth Tumelty , Luca Troncone , Ying Zhong
CPC分类号： C07K16/22 , A61P9/12 , A61K2039/505 , C07K2317/34 , C07K2317/76 , C07K2317/92
摘要： Antibodies, and antigen-binding fragments thereof, that specifically bind to bone morphogenetic protein-9 (BMP9) are provided. Embodiments include uses, and associated methods of using the antibodies, and antigen-binding fragments thereof.
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公开(公告)号：US11654147B2
公开(公告)日：2023-05-23
申请号：US17340589
申请日：2021-06-07
申请人： The Brigham and Women's Hospital, Inc. , The United States of America, as Represented by the Secretary, Department of Health and Human Services
发明人： Paul B. Yu , Wenwei Huang , Philip Edward Sanderson , Jian-Kang Jiang , Khalida Shamim , Wei Zheng , Xiuli Huang , Gregory Tawa , Arthur Lee , Asaf Alimardanov , Junfeng Huang
IPC分类号： A61K31/519 , A61P19/08 , A61K31/5377 , A61K31/551 , A61K31/675 , A61K45/06 , C07D487/04 , C07D519/00 , C07F9/6561
CPC分类号： A61K31/519 , A61K31/5377 , A61K31/551 , A61K31/675 , A61K45/06 , A61P19/08 , C07D487/04 , C07D519/00 , C07F9/6561
摘要： The present invention provides small-molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to treat subjects with Sjögren's syndrome, or diffuse intrinsic pontine glioma (DIPG).
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公开(公告)号：US10017516B2
公开(公告)日：2018-07-10
申请号：US15598540
申请日：2017-05-18
申请人： The Brigham and Women's Hospital, Inc. , The United States of America, as represented by the Secretary, Department of Health and Human Services, National Institute of Health
发明人： Asaf Alimardanov , Gregory D. Cuny , Gurmit S. Grewal , Arthur Lee , John C. McKew , Agustin H. Mohedas , Min Shen , Xin Xu , Paul B. Yu
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.
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公开(公告)号：US10513521B2
公开(公告)日：2019-12-24
申请号：US15326262
申请日：2015-07-14
申请人： The Brigham and Women's Hospital, Inc. , The United States of America, as Represented by the Secretary, Department of Health and Human Services, National Institutes of Health , University of Houston System
发明人： Arthur Lee , John C. McKew , Paresma R. Patel , Paul B. Yu , Agustin H. Mohedas , Philip E. Sanderson , Gregory D. Cuny , Wei Zheng , Xiuli Huang
IPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides bicyclic heteroaryl inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. Exemplary compounds include those of Formula I: These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.
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10.发明授权公开(公告)号：US10369152B2
公开(公告)日：2019-08-06
申请号：US15550139
申请日：2016-02-12
发明人： Paul B. Yu , Jana Bagarova , Devaveena Dey
IPC分类号： A61K31/517 , A61K45/06 , C07D405/14 , C07D401/12 , C07D487/04 , C07D491/056
摘要： Provided herein are methods and compositions for the treatment and/or prevention of abnormal bone formation in a soft tissue. In certain embodiments, the methods and compositions treat and/or prevent a disease or disorder comprising abnormal bone formation in soft tissue. Exemplary diseases or disorders that can be treated with the methods and compositions described herein include, but are not limited to, heterotopic ossification diseases such as fibrodysplasia ossificans progressive, anklyosing spondylosis, traumatic heterotopic ossification, burn- or blast-injury associated heterotopic ossification, and joint replacement surgery associated heterotopic ossification.
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