公开(公告)号：US10414791B2

公开(公告)日：2019-09-17

申请号：US15748716

申请日：2016-07-22

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari ,  Antimo Gioiello

IPC分类号： C07J9/00 ,  C07J1/00 ,  C07J7/00 ,  C07J13/00 ,  C07J41/00 ,  C07J71/00

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-OH, or an oxo group.

公开(公告)号：US10548906B2

公开(公告)日：2020-02-04

申请号：US15760769

申请日：2016-09-21

申请人： Intercept Pharmaceuticals, Inc.

发明人： Peter Leonardus Maria Jansen ,  Stephanus Willibrordus Maria Olde Damink ,  Franciscus Gerardus Schaap ,  Isabelle Anne Leclercq

IPC分类号： A61K31/575 ,  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：US09777038B2

公开(公告)日：2017-10-03

申请号：US14438323

申请日：2013-10-25

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari ,  Antimo Gioiello

IPC分类号： C07J31/00 ,  C07J9/00

CPC分类号： C07J31/006 ,  C07J9/00 ,  C07J9/005

摘要： The present invention relates to processes for preparing compounds of formula I: or a pharmaceutically acceptable salt or solvate thereof.

公开(公告)号：US10532061B2

公开(公告)日：2020-01-14

申请号：US16124139

申请日：2018-09-06

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari

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

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：US10604544B2

公开(公告)日：2020-03-31

申请号：US15750683

申请日：2016-08-05

申请人： Intercept Pharmaceuticals, Inc.

发明人： Gabriel M Galvin

IPC分类号： C07J9/00 ,  C07J31/00

摘要： The present application relates to a method of preparing compounds of Formula (A) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof.

公开(公告)号：US10550146B2

公开(公告)日：2020-02-04

申请号：US16094535

申请日：2017-04-18

申请人： Intercept Pharmaceuticals, Inc.

发明人： Benjamin List ,  Chandra Kanta De ,  Qinggang Wang

IPC分类号： C07J9/00 ,  C07J31/00

摘要： The present application relates to a safe method of preparing a bile acid derivative or a pharmaceutical acceptable salt, solvate, or amino acid conjugate thereof, on a large scale from 7-keto lithocholic acid (KLCA), comprising reacting Compound 2 with paraldehyde to form Compound 3 at a temperature between 10° C. and 30° C.:

公开(公告)号：US10421772B2

公开(公告)日：2019-09-24

申请号：US15645136

申请日：2017-07-10

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari

IPC分类号： A61K31/575 ,  C07J9/00 ,  C07J43/00 ,  C07J41/00 ,  C07C215/08 ,  C07C215/10 ,  C07C215/12

摘要： The invention relates to compounds of formula (I): wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.

公开(公告)号：US09763964B2

公开(公告)日：2017-09-19

申请号：US14743295

申请日：2015-06-18

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari ,  Stefano Fiorucci ,  Mark Pruzanski

IPC分类号： A61K31/575 ,  C07J9/00 ,  C07J31/00

CPC分类号： A61K31/575 ,  C07J9/00 ,  C07J31/006

摘要： The present invention relates to compounds of formula (I): wherein R is hydrogen or alpha-hydroxy, the hydroxyl group in position 7 is in the alpha or beta position; and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.