公开(公告)号：US20230340010A1

公开(公告)日：2023-10-26

申请号：US18188341

申请日：2023-03-22

申请人： Intercept Pharmaceuticals, Inc.

发明人： André STEINER ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： C07J9/00 ,  A61K9/20 ,  C07J51/00 ,  A61K31/575

CPC分类号： C07J9/005 ,  A61K9/2054 ,  A61K31/575 ,  C07J51/00 ,  C07B2200/13

摘要： The present invention relates to obeticholic acid:





or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

公开(公告)号：US09732116B2

公开(公告)日：2017-08-15

申请号：US14947492

申请日：2015-11-20

申请人： Intercept Pharmaceuticals, Inc.

发明人： André Steiner ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： A61K31/56 ,  C07J9/00 ,  C07J51/00 ,  A61K9/20 ,  A61K31/575

CPC分类号： C07J9/005 ,  A61K9/2054 ,  A61K31/575 ,  C07B2200/13 ,  C07J51/00

摘要： The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

公开(公告)号：US20170226149A1

公开(公告)日：2017-08-10

申请号：US15496398

申请日：2017-04-25

申请人： Intercept Pharmaceuticals, Inc.

发明人： André Steiner ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： C07J9/00

CPC分类号： C07J9/005 ,  A61K9/2054 ,  A61K31/575 ,  C07B2200/13 ,  C07J51/00

摘要： The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

公开(公告)号：US20160074419A1

公开(公告)日：2016-03-17

申请号：US14947658

申请日：2015-11-20

申请人： Intercept Pharmaceuticals, Inc.

发明人： André Steiner ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： A61K31/575

CPC分类号： C07J9/005 ,  A61K9/2054 ,  A61K31/575 ,  C07B2200/13 ,  C07J51/00

摘要： The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

公开(公告)号：US10174073B2

公开(公告)日：2019-01-08

申请号：US15496398

申请日：2017-04-25

申请人： Intercept Pharmaceuticals, Inc.

发明人： André Steiner ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： A61K31/56 ,  C07J9/00

摘要： The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

公开(公告)号：US10155787B2

公开(公告)日：2018-12-18

申请号：US14947680

申请日：2015-11-20

申请人： Intercept Pharmaceuticals, Inc.

发明人： André Steiner ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： A61K31/58 ,  C07J9/00 ,  C07J51/00 ,  A61K9/20 ,  A61K31/575

摘要： The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

公开(公告)号：US20160215014A1

公开(公告)日：2016-07-28

申请号：US14947680

申请日：2015-11-20

申请人： Intercept Pharmaceuticals, Inc.

发明人： André Steiner ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： C07J9/00

CPC分类号： C07J9/005 ,  A61K9/2054 ,  A61K31/575 ,  C07B2200/13 ,  C07J51/00

摘要： The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

公开(公告)号：US20160176913A1

公开(公告)日：2016-06-23

申请号：US14947492

申请日：2015-11-20

申请人： Intercept Pharmaceuticals, Inc.

发明人： André Steiner ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： C07J9/00

CPC分类号： C07J9/005 ,  A61K9/2054 ,  A61K31/575 ,  C07B2200/13 ,  C07J51/00

摘要： The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

公开(公告)号：US20160108082A1

公开(公告)日：2016-04-21

申请号：US14979005

申请日：2015-12-22

申请人： Intercept Pharmaceuticals, Inc.

发明人： André Steiner ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： C07J9/00

CPC分类号： C07J9/005 ,  A61K9/2054 ,  A61K31/575 ,  C07B2200/13 ,  C07J51/00

摘要： The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

公开(公告)号：US20130345188A1

公开(公告)日：2013-12-26

申请号：US13919734

申请日：2013-06-17

申请人： Intercept Pharmaceuticals, Inc.

发明人： André Steiner ,  Heidi Waenerlund Poulsen ,  Emilie Jolibois ,  Melissa Rewolinski ,  Ralf Gross ,  Emma Sharp ,  Fiona Dubas-Fisher ,  Alex Eberlin

IPC分类号： C07J9/00

CPC分类号： C07J9/005 ,  A61K9/2054 ,  A61K31/575 ,  C07B2200/13 ,  C07J51/00

摘要： The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

摘要翻译： 本发明涉及炔丙酸或其药学上可接受的盐，溶剂化物或氨基酸缀合物。 炔雌醇可用于治疗或预防FXR介导的疾病或病症，心血管疾病或胆汁淤积性肝病，并用于降低HDL胆固醇，降低哺乳动物中的甘油三酯或抑制纤维化。 本发明还涉及合成辛酸的方法。