公开(公告)号：US11945782B2

公开(公告)日：2024-04-02

申请号：US17098184

申请日：2020-11-13

申请人： SRX CARDIO, LLC

发明人： Thomas E. Barta ,  Jonathan William Bourne ,  Kyle D. Monroe ,  Michael M. Muehlemann ,  Anjali Pandey ,  Simeon Bowers

IPC分类号： C07D217/24 ,  A61K45/06 ,  C07D217/02

CPC分类号： C07D217/24 ,  C07D217/02 ,  A61K45/06

摘要： This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunctions; thus, there is also utility for small organic compound ligands and can raise LDL levels.

公开(公告)号：US20210236481A1

公开(公告)日：2021-08-05

申请号：US17020276

申请日：2020-09-14

申请人： SRX Cardio, LLC

发明人： Thomas E. Barta ,  Jonathan William Bourne ,  Kyle D. Monroe ,  Michael M. Muehlemann ,  Anjali Pandey ,  Simeon Bowers

IPC分类号： A61K31/495 ,  A61K45/06 ,  C07D213/64 ,  C07C237/20 ,  A61P3/06 ,  A61K31/4409

摘要： This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.

公开(公告)号：US12115154B2

公开(公告)日：2024-10-15

申请号：US17124357

申请日：2020-12-16

申请人： SRX Cardio, LLC

发明人： Simeon Bowers ,  Mark Karbarz ,  Jiang Zhu ,  Thomas E. Barta ,  Jonathan William Bourne ,  Anjali Pandey

IPC分类号： C07D211/14 ,  A61K31/451 ,  A61K31/4545 ,  A61P3/06 ,  C07D401/04

CPC分类号： A61K31/451 ,  A61K31/4545 ,  A61P3/06 ,  C07D211/14 ,  C07D401/04

摘要： The present disclosure relates to novel compounds capable of binding to PCSK9, thereby modulating PCSK9 biological activity. Also provided are compositions comprising these compounds, methods of preparing the compounds, and methods for use of the compounds in the treatment of PCSK9-related conditions and diseases.

公开(公告)号：US11925637B2

公开(公告)日：2024-03-12

申请号：US17217848

申请日：2021-03-30

申请人： SRX Cardio, LLC

发明人： Thomas E. Barta ,  Jonathan William Bourne ,  Kyle D. Monroe ,  Michael M. Muehlemann ,  Anjali Pandey ,  Simeon Bowers

IPC分类号： A61K31/495 ,  A61K31/4409 ,  A61K45/06 ,  A61P3/06 ,  C07C237/20 ,  C07D213/64

CPC分类号： A61K31/495 ,  A61K31/4409 ,  A61K45/06 ,  A61P3/06 ,  C07C237/20 ,  C07D213/64 ,  A61K2300/00 ,  C07B2200/07

摘要： This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.

公开(公告)号：US20220267269A1

公开(公告)日：2022-08-25

申请号：US17618873

申请日：2020-06-12

申请人： SRX Cardio, LLC

发明人： Simeon Bowers ,  Mark Karbarz ,  Jiang Zhu ,  Thomas E. Barta ,  Jonathan William Bourne ,  Anjali Pandey

IPC分类号： C07D211/42 ,  C07D207/08 ,  C07D211/14 ,  C07D211/18 ,  C07D211/38 ,  C07D211/56 ,  C07D233/10 ,  C07D233/22 ,  C07D265/30 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/14 ,  C07D498/04

摘要： The present disclosure relates to novel compounds capable of binding to PCSK9, thereby modulating PCSK9 biological activity. Also provided are compositions comprising these compounds, methods of preparing the compounds, and methods for use of the compounds in the treatment of PCSK9-related conditions and diseases.

公开(公告)号：US20210309613A1

公开(公告)日：2021-10-07

申请号：US17098184

申请日：2020-11-13

申请人： SRX Cardio, LLC

发明人： Thomas E. Barta ,  Jonathan William Bourne ,  Kyle D. Monroe ,  Michael M. Muehlemann ,  Anjali Pandey ,  Simeon Bowers

IPC分类号： C07D217/24 ,  C07D217/02

摘要： This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunctions; thus, there is also utility for small organic compound ligands and can raise LDL levels.

公开(公告)号：US20210032214A1

公开(公告)日：2021-02-04

申请号：US16861166

申请日：2020-04-28

申请人： SRX Cardio, LLC

发明人： Anjali Pandey ,  Simeon Bowers ,  Thomas E. Barta ,  Jonathan William Bourne

IPC分类号： C07D295/073 ,  C07D401/04 ,  C07D403/04 ,  C07D211/18 ,  C07D211/26 ,  C07D211/46 ,  C07D211/54 ,  C07D211/58 ,  C07D295/195 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/02 ,  C07D417/04 ,  C07D417/14 ,  C07D471/08

摘要： The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I).

公开(公告)号：US11944619B2

公开(公告)日：2024-04-02

申请号：US17020276

申请日：2020-09-14

申请人： SRX Cardio, LLC

发明人： Thomas E. Barta ,  Jonathan William Bourne ,  Kyle D. Monroe ,  Michael M. Muehlemann ,  Anjali Pandey ,  Simeon Bowers

IPC分类号： A61K31/495 ,  A61K31/4409 ,  A61K45/06 ,  A61P3/06 ,  C07C237/20 ,  C07D213/64

CPC分类号： A61K31/495 ,  A61K31/4409 ,  A61K45/06 ,  A61P3/06 ,  C07C237/20 ,  C07D213/64 ,  A61K2300/00 ,  C07B2200/07

摘要： This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.

公开(公告)号：US11891369B2

公开(公告)日：2024-02-06

申请号：US16861166

申请日：2020-04-28

申请人： SRX Cardio, LLC

发明人： Anjali Pandey ,  Simeon Bowers ,  Thomas E. Barta ,  Jonathan William Bourne

IPC分类号： A61K31/4709 ,  C07D295/073 ,  C07D401/04 ,  C07D403/04 ,  C07D211/18 ,  C07D211/26 ,  C07D211/46 ,  C07D211/54 ,  C07D211/58 ,  C07D295/195 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/02 ,  C07D417/04 ,  C07D417/14 ,  C07D471/08

CPC分类号： C07D295/073 ,  C07D211/18 ,  C07D211/26 ,  C07D211/46 ,  C07D211/54 ,  C07D211/58 ,  C07D295/195 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D407/02 ,  C07D417/04 ,  C07D417/14 ,  C07D471/08

摘要： The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity, for treatment of a disease or condition mediated, at least in part, by PCSK9. The compounds of the disclosure include compounds Formula (I).

公开(公告)号：US20220193058A1

公开(公告)日：2022-06-23

申请号：US17124357

申请日：2020-12-16

申请人： SRX Cardio, LLC

发明人： Simeon Bowers ,  Mark Karbarz ,  Jiang Zhu ,  Thomas E. Barta ,  Jonathan William Bourne ,  Anjali Pandey

IPC分类号： A61K31/451 ,  C07D211/14 ,  C07D401/04 ,  A61P3/06 ,  A61K31/4545

摘要： The present disclosure relates to novel compounds capable of binding to PCSK9, thereby modulating PCSK9 biological activity. Also provided are compositions comprising these compounds, methods of preparing the compounds, and methods for use of the compounds in the treatment of PCSK9-related conditions and diseases.