公开(公告)号：EP2861613A1

公开(公告)日：2015-04-22

申请号：EP13733181.5

申请日：2013-06-17

申请人： Intercept Pharmaceuticals, Inc.

发明人： STEINER, André ,  WAENERLUND POULSEN, Heidi ,  JOLIBOIS, Emilie ,  REWOLINSKI, Melissa ,  GROSS, Ralf ,  SHARP, Emma ,  DUBAS-FISHER, Fiona ,  EBERLIN, Alex

IPC分类号： C07J9/00 ,  A61K31/575 ,  A61P1/16 ,  C07J51/00

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，溶剂合物或氨基酸缀合物。 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，以及用于降低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。

公开(公告)号：EP3789394A1

公开(公告)日：2021-03-10

申请号：EP20190630.2

申请日：2013-06-17

申请人： Intercept Pharmaceuticals, Inc.

发明人： STEINER, André ,  WAENERLUND POULSEN, Heidi ,  JOLIBOIS, Emilie ,  REWOLINSKI, Melissa ,  GROSS, Ralf ,  SHARP, Emma ,  DUBAS-FISHER, Fiona ,  EBERLIN, Alex

IPC分类号： C07J9/00 ,  C07J51/00 ,  A61K9/20 ,  A61K31/575 ,  A61P1/16 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P13/04 ,  A61P31/14 ,  A61P43/00

摘要： The present invention relates to crystalline form C of obeticholic acid, pharmaceutical compositions thereof and medicinal indications thereof in the treatment of FXR mediated diseases.

公开(公告)号：EP3336097B1

公开(公告)日：2020-08-19

申请号：EP17202916.7

申请日：2013-06-17

申请人： Intercept Pharmaceuticals, Inc.

发明人： STEINER, André ,  WAENERLUND POULSEN, Heidi ,  JOLIBOIS, Emilie ,  REWOLINSKI, Melissa ,  GROSS, Ralf ,  SHARP, Emma ,  DUBAS-FISHER, Fiona ,  EBERLIN, Alex

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

公开(公告)号：EP3336097A1

公开(公告)日：2018-06-20

申请号：EP17202916.7

申请日：2013-06-17

申请人： Intercept Pharmaceuticals, Inc.

发明人： STEINER, André ,  WAENERLUND POULSEN, Heidi ,  JOLIBOIS, Emilie ,  REWOLINSKI, Melissa ,  GROSS, Ralf ,  SHARP, Emma ,  DUBAS-FISHER, Fiona ,  EBERLIN, Alex

IPC分类号： C07J9/00 ,  C07J51/00 ,  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：EP3992201A1

公开(公告)日：2022-05-04

申请号：EP21195801.2

申请日：2013-06-17

申请人： Intercept Pharmaceuticals, Inc.

发明人： STEINER, André ,  WAENERLUND POULSEN, Heidi ,  JOLIBOIS, Emilie ,  REWOLINSKI, Melissa ,  GROSS, Ralf ,  SHARP, Emma ,  DUBAS-FISHER, Fiona ,  EBERLIN, Alex

IPC分类号： C07J9/00 ,  C07J51/00 ,  A61P1/16 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P13/04 ,  A61P31/14 ,  A61P43/00 ,  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：EP3394081A1

公开(公告)日：2018-10-31

申请号：EP16714049.0

申请日：2016-01-08

申请人： Intercept Pharmaceuticals, Inc.

发明人： STEINER, André ,  WAENERLUND POULSEN, Heidi ,  JOLIBOIS, Emilie ,  REWOLINSKI, Melissa ,  GROSS, Ralf ,  SHARP, Emma ,  DUBAS-FISHER, Fiona ,  EBERLIN, Alex

IPC分类号： C07J9/00 ,  C07J17/00 ,  C07J51/00 ,  A61K31/575 ,  A61P1/16

CPC分类号： C07J9/005 ,  C07B2200/13 ,  C07J17/00 ,  C07J51/00

摘要： The present application relates to crystalline forms A, D, F, G and I of obeticholic acid. These crystalline forms are useful in the production of Obeticholic acid (in particular its purification), which is a drug 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.