公开(公告)号：US20220184099A1

公开(公告)日：2022-06-16

申请号：US17384555

申请日：2021-07-23

申请人： Intercept Pharmaceuticals, Inc.

发明人： Jeffrey EDWARDS ,  Sharon KARAN ,  Jason CAMPAGNA ,  Leigh A. MACCONELL

IPC分类号： A61K31/575 ,  A61P1/16

摘要： The disclosure relates to methods of using obeticholic acid or pharmaceutically acceptable salt or amino acid conjugate thereof for slowing down or reversing the progression of compensated cirrhosis.

公开(公告)号：US20220133745A1

公开(公告)日：2022-05-05

申请号：US17542923

申请日：2021-12-06

申请人： Intercept Pharmaceuticals, Inc.

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

IPC分类号： A61K31/575 ,  A61K47/50 ,  A61K9/16 ,  A61K9/14 ,  C07J9/00 ,  A61K9/20 ,  A61K45/06

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：US20210269473A1

公开(公告)日：2021-09-02

申请号：US17092612

申请日：2020-11-09

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto PELLICCIARI

IPC分类号： C07J9/00 ,  C07J31/00 ,  C07J41/00

摘要： The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

公开(公告)号：US11066437B2

公开(公告)日：2021-07-20

申请号：US16016486

申请日：2018-06-22

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari ,  Antimo Gioiello ,  Gabriel Galvin ,  Ronald D. Lewis, II ,  Mathew Yanik ,  Myoung Goo Kim ,  Frederik Ronald Leusink ,  Bartjan Koning ,  Thomas Hensel

IPC分类号： C07J9/00 ,  C07J31/00

摘要： The present disclosure relates to methods and novel intermediates useful in the preparation of a compound of formula I or pharmaceutically acceptable salt, hydrate, solvate or amino acid, sulfate or glucuronide conjugate, or prodrug thereof, comprising the step of reacting a compound of formula I-4 with a halogenating reagent to provide a compound of formula I-5a

公开(公告)号：US20210139528A1

公开(公告)日：2021-05-13

申请号：US16491798

申请日：2018-03-07

申请人： INTERCEPT PHARMACEUTICALS, INC.

发明人： Gabriel M. GALVIN ,  Melissa REWOLINSKI

IPC分类号： C07J9/00

摘要： The crystalline forms of obeticholic acid and methods of preparation and use thereof are described.

公开(公告)号：US11000532B2

公开(公告)日：2021-05-11

申请号：US16695528

申请日：2019-11-26

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari

IPC分类号： A61K31/575 ,  C07J41/00 ,  A61P1/16 ,  A61P1/00 ,  C07J9/00 ,  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：US10987362B2

公开(公告)日：2021-04-27

申请号：US16228944

申请日：2018-12-21

申请人： Intercept Pharmaceuticals, Inc.

发明人： Stefano Fiorucci ,  Roberto Pellicciari ,  Mark Pruzanski

IPC分类号： A61K31/575 ,  A61P1/16 ,  A61K9/00

摘要： The present invention relates to a method for inhibiting fibrosis that occurs in an organ where the farnesoid X receptor (FXR) is expressed. This method involves the step of administering a high potency, activating ligand of FXR in an effective amount to a patient who is not suffering from a cholestatic condition. The invention also provides pharmaceutical compositions containing an effective amount of an FXR ligand and kits for dispensing the pharmaceutical compositions.

公开(公告)号：USRE48286E1

公开(公告)日：2020-10-27

申请号：US16448503

申请日：2019-06-21

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari

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

摘要： The invention relates to compounds of formula (I): wherein R is ethyl 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：US10646499B2

公开(公告)日：2020-05-12

申请号：US16030141

申请日：2018-07-09

申请人： Intercept Pharmaceuticals, Inc. ,  Sumitomo Dainippon Pharma Co., Ltd.

发明人： Richard Gail Lancaster ,  Kay K. Olmstead ,  Masashi Kagihiro ,  Mitsuhiro Matono ,  Ikuko Taoka ,  Mark Pruzanski ,  David Shapiro ,  Roya Hooshmand-Rad ,  Richard Pencek ,  Cathi Sciacca ,  Lise Eliot ,  Jeffrey Edwards ,  Leigh A. MacConell ,  Tonya K. Marmon

IPC分类号： A61K31/575 ,  A61K47/50 ,  A61K9/16 ,  A61K9/14 ,  C07J9/00 ,  A61K9/20 ,  A61K45/06

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：US10258633B2

公开(公告)日：2019-04-16

申请号：US15299559

申请日：2016-10-21

申请人： Stefano Fiorucci ,  Roberto Pellicciari ,  Mark Pruzanski

发明人： Stefano Fiorucci ,  Roberto Pellicciari ,  Mark Pruzanski

IPC分类号： A61K31/56 ,  A61K31/575

摘要： The present invention relates to a method for inhibiting fibrosis that occurs in an organ where the farnesoid X receptor (FXR) is expressed. This method involves the step of administering a high potency, activating ligand of FXR in an effective amount to a patient who is not suffering from a cholestatic condition. The invention also provides pharmaceutical compositions containing an effective amount of an FXR ligand and kits for dispensing the pharmaceutical compositions.