公开(公告)号：EP4371616A3

公开(公告)日：2024-08-28

申请号：EP24154375.0

申请日：2016-04-26

申请人： Intercept Pharmaceuticals, Inc.

发明人： LANCASTER,, Richard G. ,  OLMSTEAD,, Kay K. ,  KAGIHIRO,, Masashi ,  TAOKA,, Ikuko ,  MATONO,, Mitsuhiro ,  PRUZANSKI,, Mark ,  SHAPIRO,, David ,  HOOSHMAND-RAD,, Roya ,  PENCEK,, Richard ,  SCIACCA,, Cathi ,  ELIOT,, Lise ,  EDWARDS,, Jeffrey ,  MACCONELL,, Leigh A. ,  MARMON,, Tonya K.

IPC分类号： C07J9/00 ,  A61K31/575 ,  A61K9/14 ,  A61K9/20 ,  A61P1/16 ,  A61P31/14 ,  A61P43/00

CPC分类号： A61K9/14 ,  C07J9/005 ,  A61K31/575 ,  A61K9/2054 ,  A61K9/2059 ,  A61K45/06 ,  A61P1/16 ,  A61P31/14 ,  A61P43/00

摘要： The disclosure relates to obeticholic acid formulations with improved stability, dissolution, and/or solubility, methods of preparing the same for use and methods of treating various diseases and conditions

公开(公告)号：EP3445370B1

公开(公告)日：2021-12-01

申请号：EP17786465.9

申请日：2017-04-18

发明人： LIST, Benjamin ,  DE, Chandra ,  WANG, Qinggang

IPC分类号： C07J9/00 ,  C07J51/00 ,  C07J31/00

公开(公告)号：EP3437645B1

公开(公告)日：2021-09-22

申请号：EP17775388.6

申请日：2017-03-30

发明人： MATONO, Mitsuhiro ,  HAYAMA, Tetsuya

IPC分类号： A61K31/575 ,  A61K9/28 ,  A61K9/30 ,  A61K9/36 ,  A61P1/16

公开(公告)号：EP3175855B1

公开(公告)日：2020-07-15

申请号：EP16196645.2

申请日：2005-03-14

申请人： Intercept Pharmaceuticals, Inc.

发明人： FIORUCCI, Stefano ,  PELLICCIARI, Roberto ,  PRUZANSKI, Mark

IPC分类号： A61P1/16 ,  A61P1/00

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.

公开(公告)号：EP3360882A1

公开(公告)日：2018-08-15

申请号：EP18163623.4

申请日：2014-05-14

申请人： Intercept Pharmaceuticals, Inc.

发明人： PELLICCIARI, Roberto

IPC分类号： C07J9/00 ,  C07J41/00 ,  A61K31/575 ,  A61P1/16 ,  C07J71/00 ,  C07J31/00

CPC分类号： A61K31/575 ,  A61P1/00 ,  A61P1/16 ,  C07J9/005 ,  C07J31/006 ,  C07J41/0061 ,  C07J71/001

摘要： The present invention provides a compound of formula (I):

or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R 1 is a hydroxy group and R 2 , R 3 , R 4 , R 5 , and R 6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.

公开(公告)号：EP3352768A1

公开(公告)日：2018-08-01

申请号：EP16849506.7

申请日：2016-09-21

申请人： Intercept Pharmaceuticals, Inc.

发明人： JANSEN, Peter Leonardus Maria ,  OLDE DAMINK, Stephanus Willibrodus Maria ,  SCHAAP, Franciscus Gerardus ,  LECLERO, Isabelle Anne

IPC分类号： A61K31/79 ,  A61K31/58 ,  A61K31/56

CPC分类号： A61K31/575 ,  A61K31/56 ,  A61P1/16

摘要： The present invention relates to methods of accelerating, promoting or increasing hepatic regeneration, or increasing liver mass in a subject, by using a compound of formula (A): or a pharmaceutically acceptable salt thereof, and wherein R1, R2, R3, R4, R5, R6, m, and n are as described herein.

公开(公告)号：EP3328817A1

公开(公告)日：2018-06-06

申请号：EP16831137.1

申请日：2016-07-22

申请人： Intercept Pharmaceuticals, Inc.

发明人： PELLICCIARI, Roberto ,  GIOIELLO, Antimo

IPC分类号： C07B61/00 ,  C07J75/00 ,  C07J9/00

CPC分类号： C07J9/005 ,  C07J1/0011 ,  C07J7/0035 ,  C07J13/005 ,  C07J13/007 ,  C07J41/0005 ,  C07J41/005 ,  C07J71/0005

摘要： The present application relates to a method of preparing compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, R1 is H, α-OH, β-ΟΗ, or an oxo group.

公开(公告)号：EP2997035B8

公开(公告)日：2018-05-23

申请号：EP14723820.8

申请日：2014-05-14

申请人： Intercept Pharmaceuticals, Inc.

发明人： PELLICCIARI, Roberto

IPC分类号： C07J9/00 ,  C07J41/00 ,  A61K31/575 ,  A61P1/16 ,  C07J71/00 ,  C07J31/00

CPC分类号： A61K31/575 ,  A61P1/00 ,  A61P1/16 ,  C07J9/005 ,  C07J31/006 ,  C07J41/0061 ,  C07J71/001

摘要： The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1, R2, R3, R4, R5, and R6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.

公开(公告)号：EP3280421A1

公开(公告)日：2018-02-14

申请号：EP16777168.2

申请日：2016-04-06

申请人： Intercept Pharmaceuticals, Inc.

发明人： PRUZANSKI, Mark ,  ADORINI, Luciano

IPC分类号： A61K31/575 ,  C07J43/00 ,  C07J9/00 ,  A61K51/00

CPC分类号： A61K31/575 ,  A61K31/155 ,  A61K31/4985 ,  A61K31/7048 ,  A61K38/26 ,  A61K45/06 ,  A61K47/542 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10 ,  C07J9/005 ,  C07J51/00 ,  A61K2300/00

摘要： The present application relates to a pharmaceutical composition comprising a combination of an FXR agonist and at least one additional therapeutic agent that lowers the glucose level in the blood, stimulates insulin secretion, and/or increases insulin sensitivity. The present application relates to use of the pharmaceutical composition for the treatment or prevention of a FXR mediated disease or condition, such as NAFLD and NASH, a disease or condition related to an elevated level of glucose in the blood, decreased secretion of insulin, and/or decreased insulin sensitivity such as hyperglycemia, diabetes, obesity, and insulin resistance, or for lowering the glucose level in the blood, stimulating insulin secretion, and/or increasing insulin sensitivity.