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：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：US20170305961A1

公开(公告)日：2017-10-26

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： C07J9/00 ,  C07J43/00 ,  C07C215/10 ,  C07C215/08 ,  C07C215/12 ,  C07J41/00

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：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：US11345721B2

公开(公告)日：2022-05-31

申请号：US17010505

申请日：2020-09-02

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari ,  Antimo Gioiello ,  Antonio Macchiarulo ,  Francoise Perron-Sierra ,  Klaus Seedorf

IPC分类号： C07J9/00 ,  C07J43/00 ,  A61P1/16 ,  C07J41/00 ,  A61P3/08

摘要： The application relates to compounds of formula A: or a salt, solvate, ester, tautomer, amino acid conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

公开(公告)号：US11319337B2

公开(公告)日：2022-05-03

申请号：US17025475

申请日：2020-09-18

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari ,  Antimo Gioiello

IPC分类号： C07J11/00 ,  A61K47/54 ,  C07J9/00 ,  C07J31/00

摘要： The present application provides Compound 1: or a pharmaceutically acceptable salt or amino acid conjugate thereof. The present invention relates to an FXR activator and to methods of making and using said compound.

公开(公告)号：US10800807B2

公开(公告)日：2020-10-13

申请号：US15742595

申请日：2016-06-16

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari ,  Antimo Gioiello ,  Antonio Macchiarulo ,  Francoise Perron-Sierra ,  Klaus Seedorf

IPC分类号： C07J9/00 ,  C07J43/00 ,  A61P1/16 ,  C07J41/00 ,  A61P3/08

摘要： The application relates to compounds of formula A: or a salt, solvate, ester, tautomer, amino acid conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

公开(公告)号：US20170260225A1

公开(公告)日：2017-09-14

申请号：US15451818

申请日：2017-03-07

申请人： Intercept Pharmaceuticals, Inc.

发明人： Roberto Pellicciari ,  Antimo Gioiello

IPC分类号： C07J11/00

摘要： The present application provides Compound 1: or a pharmaceutically acceptable salt or amino acid conjugate thereof. The present invention relates to an FXR activator and to methods of making and using said compound.