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.

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.

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.

公开(公告)号：US09682983B2

公开(公告)日：2017-06-20

申请号：US14776302

申请日：2014-03-13

申请人： THE BRIGHAM AND WOMEN'S HOSPITAL, INC. ,  THE UNITED STATES OF AMERICA, 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.

公开(公告)号：US20170197968A1

公开(公告)日：2017-07-13

申请号：US15326262

申请日：2015-07-14

申请人： Arthur LEE ,  John C. MCKEW ,  Paresma R. PATEL ,  Paul B. YU ,  Agustin H. MOHEADS ,  Philip E. SANDERSON ,  Wei ZHENG ,  Xiuli HUANG ,  THE BRIGHAM AND WOMEN'S HOSPITLAL, INC. ,  THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN ,  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

CPC分类号： C07D487/04 ,  C07D519/00

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 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.