PL3277286T3 - Pochodne kwasu żółciowego jako agonisty fxr/tgr5 i sposoby ich stosowania - Google Patents

Pochodne kwasu żółciowego jako agonisty fxr/tgr5 i sposoby ich stosowania

Info

Publication number
PL3277286T3
PL3277286T3 PL16774118T PL16774118T PL3277286T3 PL 3277286 T3 PL3277286 T3 PL 3277286T3 PL 16774118 T PL16774118 T PL 16774118T PL 16774118 T PL16774118 T PL 16774118T PL 3277286 T3 PL3277286 T3 PL 3277286T3
Authority
PL
Poland
Prior art keywords
fxr
methods
acid derivatives
bile acid
tgr5 agonists
Prior art date
Application number
PL16774118T
Other languages
English (en)
Inventor
Guoqiang Wang
Yat Sun Or
Ruichao Shen
Xuechao Xing
Jiang Long
Peng Dai
Brett GRANGER
Jing He
Original Assignee
Enanta Pharmaceuticals, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Enanta Pharmaceuticals, Inc. filed Critical Enanta Pharmaceuticals, Inc.
Publication of PL3277286T3 publication Critical patent/PL3277286T3/pl

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0088Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing unsubstituted amino radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
PL16774118T 2015-03-31 2016-03-30 Pochodne kwasu żółciowego jako agonisty fxr/tgr5 i sposoby ich stosowania PL3277286T3 (pl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562140927P 2015-03-31 2015-03-31
US201662287267P 2016-01-26 2016-01-26
PCT/US2016/025035 WO2016161003A1 (en) 2015-03-31 2016-03-30 Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
EP16774118.0A EP3277286B1 (en) 2015-03-31 2016-03-30 Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof

Publications (1)

Publication Number Publication Date
PL3277286T3 true PL3277286T3 (pl) 2021-11-08

Family

ID=57007583

Family Applications (1)

Application Number Title Priority Date Filing Date
PL16774118T PL3277286T3 (pl) 2015-03-31 2016-03-30 Pochodne kwasu żółciowego jako agonisty fxr/tgr5 i sposoby ich stosowania

Country Status (27)

Country Link
US (4) US10457703B2 (pl)
EP (1) EP3277286B1 (pl)
JP (1) JP6785788B2 (pl)
KR (1) KR102681304B1 (pl)
CN (1) CN107427527B (pl)
AU (1) AU2016242861B2 (pl)
CA (1) CA2981503C (pl)
CY (1) CY1124404T1 (pl)
DK (1) DK3277286T3 (pl)
ES (1) ES2886766T3 (pl)
HR (1) HRP20211066T1 (pl)
HU (1) HUE054960T2 (pl)
IL (1) IL254288B (pl)
LT (1) LT3277286T (pl)
MX (1) MX379579B (pl)
MY (1) MY192135A (pl)
NZ (1) NZ735126A (pl)
PH (1) PH12017501586B1 (pl)
PL (1) PL3277286T3 (pl)
PT (1) PT3277286T (pl)
RS (1) RS62110B1 (pl)
RU (1) RU2712099C2 (pl)
SG (2) SG10201910670RA (pl)
SI (1) SI3277286T1 (pl)
SM (1) SMT202100593T1 (pl)
WO (1) WO2016161003A1 (pl)
ZA (2) ZA201707212B (pl)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3871693A1 (en) 2005-09-27 2021-09-01 Special Water Patents B.V. Compositions for oral care
BR112017009657A2 (pt) 2014-11-06 2018-01-23 Enanta Pharmaceuticals, Inc análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
WO2016086115A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof
CA2968404A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
SI3277286T1 (sl) 2015-03-31 2021-09-30 Enanta Pharmaceuticals, Inc. Derivati žolčne kisline kot antagonisti FXR/TGR5 in metode za njihovo uporabo
KR102788843B1 (ko) * 2016-01-28 2025-03-28 치아타이 티안큉 파마수티컬 그룹 주식회사 스테로이드 유도체 fxr 작용체
WO2017147137A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid as fxr/tgr5 agonists and methods of use thereof
US10364267B2 (en) 2016-02-23 2019-07-30 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
US10323061B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Heteroaryl containing bile acid analogs as FXR/TGR5 agonists and methods of use thereof
EA038580B9 (ru) * 2016-05-18 2021-10-05 Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд. Агонист fxr, представляющий собой производное стероидов
US10584145B2 (en) 2016-11-29 2020-03-10 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonylurea bile acid derivatives
CN108218946B (zh) * 2016-12-15 2021-04-16 宁波百纳西药业有限公司 一种去氧胆酸类化合物、其制备方法及应用
CN108218945B (zh) * 2016-12-15 2021-05-28 宁波百纳西药业有限公司 去氧胆酸衍生物、其制备方法、药物组合物及用途
WO2018152171A1 (en) * 2017-02-14 2018-08-23 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr agonists and methods of use thereof
ES2971092T3 (es) * 2017-04-07 2024-06-03 Enanta Pharm Inc Procedimiento para la preparación de derivados de ácidos biliares de carbamato de sulfonilo
CN110945006A (zh) 2017-06-23 2020-03-31 英特塞普特医药品公司 用于制备胆汁酸衍生物的方法和中间体
CN110869381B (zh) * 2017-07-26 2021-11-19 正大天晴药业集团股份有限公司 甾体类衍生物fxr激动剂的制备方法
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
AU2020312735A1 (en) 2019-07-18 2021-12-16 Enyo Pharma Method for decreasing adverse-effects of interferon
JP2022552655A (ja) 2019-10-07 2022-12-19 キャリーオペ,インク. Gpr119アゴニスト
US20230060715A1 (en) 2020-01-15 2023-03-02 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of fxr agonists for treating an infection by hepatitis d virus
PH12022552277A1 (en) 2020-02-28 2024-03-04 Kallyope Inc Gpr40 agonists
US12215127B2 (en) 2020-04-17 2025-02-04 Cornell University Compositions and methods for profiling of gut microbiota-associated bile salt hydrolase (BSH) activity
US12030912B2 (en) * 2020-05-15 2024-07-09 Brigham Young University Cationic steroidal antimicrobial compounds with urethane linkages
JP2023526625A (ja) 2020-05-19 2023-06-22 キャリーオペ,インク. Ampkアクチベーター
CN116390925A (zh) 2020-06-26 2023-07-04 卡尔优普公司 Ampk活化剂
US20240100125A1 (en) 2021-01-14 2024-03-28 Enyo Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
JP2024517181A (ja) 2021-04-28 2024-04-19 ウエヌイグレックオ・ファーマ 組合せ治療としてfxrアゴニストを使用するtlr3アゴニストの効果の強い増強
WO2023288123A1 (en) 2021-07-16 2023-01-19 Interecept Pharmaceuticals, Inc. Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid

Family Cites Families (144)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1592791A (en) 1977-01-07 1981-07-08 Radiochemical Centre Ltd Selenium- or tellurium-containing bile acids and derivatives thereof
WO1987002367A2 (en) 1985-10-18 1987-04-23 The Upjohn Company Cyclic hydrocarbons with an aminoalkyl sidechain
US5571809A (en) 1989-04-20 1996-11-05 Boehringer Ingelheim Pharmaceuticals, Inc. The treatment of HIV-1 infection using certain pyridodiazepines
IT1255449B (it) 1992-06-30 1995-10-31 Fabio Berlati Uso di nor- e omo-derivati di acidi biliari come promotori di assorbimento di farmaci.
IT1255485B (it) 1992-08-04 1995-11-06 Erregierre Ind Chim Processo per preparare gli acidi biliari coniugati con la glicina e relative composizioni terapeutiche per il trattamento dell'insufficienza epatica
TW289757B (pl) 1993-05-08 1996-11-01 Hoechst Ag
TW289020B (pl) 1993-05-08 1996-10-21 Hoechst Sktiengesellschaft
US5541348A (en) * 1994-03-10 1996-07-30 National Research Council Of Canada Bile acids for biological and chemical applications and processes for the production thereof
ES2293638T3 (es) 1994-03-25 2008-03-16 Isotechnika, Inc. Mejora de la eficacia de farmacos por deuteracion.
US5646316A (en) 1994-04-08 1997-07-08 Osteoarthritis Sciences, Inc. Bile acid inhibitors of metalloproteinase enzymes
JPH1160594A (ja) 1997-08-25 1999-03-02 Sankyo Co Ltd 胆汁酸誘導体
JP3865890B2 (ja) 1997-09-30 2007-01-10 富士フイルムホールディングス株式会社 ポジ型感光性組成物
JP2002532729A (ja) 1998-12-23 2002-10-02 グラクソ グループ リミテッド 核内受容体のリガンドのアッセイ
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
IL146222A0 (en) 1999-04-30 2002-07-25 Univ Michigan Therapeutic applications of pro-apoptotic benzodiazepines
US20020098999A1 (en) * 2000-10-06 2002-07-25 Gallop Mark A. Compounds for sustained release of orally delivered drugs
EP1343805A4 (en) * 2000-10-06 2005-07-20 Xenoport Inc COMPOUNDS DERIVED FROM GALLENIC ACIDS FOR THE PROVISION OF CONTINUING SYSTEMIC CONCENTRATIONS OF MEDICINAL PRODUCTS AFTER ORAL ADMINISTRATION
EP1392714B1 (en) 2001-03-12 2005-08-31 Intercept Pharmaceuticals, Inc. Steroids as agonists for fxr
ATE381542T1 (de) 2001-08-13 2008-01-15 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
CA2482195A1 (en) 2002-04-12 2003-10-23 The University Of Chicago Farnesoid x-activated receptor agonists
ITMI20021080A1 (it) 2002-05-21 2003-11-21 Marcello Izzo Associazioni farmaceutiche per uso topico a base di chelati del ferroinibitori delle metalloproteasi e fattore xiii per il trattamento dell
AU2003290796A1 (en) 2002-11-14 2004-06-15 The Scripps Research Institute Non-steroidal fxr agonists
EP1562915A1 (en) 2002-11-22 2005-08-17 SmithKline Beecham Corporation Farnesoid x receptor agonists
WO2005054213A1 (ja) 2003-12-02 2005-06-16 Shionogi & Co., Ltd. ペルオキシソーム増殖活性化受容体アゴニスト活性を有するイソキサゾール誘導体
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
US9498484B2 (en) 2004-03-12 2016-11-22 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using FXR ligands
ITMI20050912A1 (it) 2005-05-19 2006-11-20 Erregierre Spa Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici
ES2374165T3 (es) 2005-12-19 2012-02-14 Glaxosmithkline Llc Agonistas del receptor x farnesoide.
EA200870217A1 (ru) 2006-01-30 2009-02-27 Экселиксис, Инк. 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции
EP1978968A2 (en) 2006-02-01 2008-10-15 Brigham Young University Cationic steroid antimicrobial compositions for treating or preventing hiv infections
BRPI0707427A2 (pt) 2006-02-03 2011-05-03 Lilly Co Eli composto ou um sal farmaceuticamente aceitável do mesmo, método para tratar dislipidemia, aterosclerose, e diabetes e complicações da mesma, para elevar os nìveis plásmicos de hdl, e para diminuir triglicerìdeos plásmicos, composição farmacêutica, e, uso de um composto ou de um sal farmaceuticamente aceitável do mesmo
EP1987051A2 (en) 2006-02-14 2008-11-05 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions
AU2007230991A1 (en) 2006-03-22 2007-10-04 Syndexa Pharmaceuticals Corporation Compounds and methods for treatment of disorders associated with ER stress
EA015632B9 (ru) 2006-05-24 2012-08-30 Эли Лилли Энд Компани Агонисты fxr
TW200811170A (en) 2006-06-27 2008-03-01 Sanofi Aventis Urea derivatives of tropane, their preparation and their therapeutic application
DK2040713T3 (da) 2006-06-27 2014-09-29 Intercept Pharmaceuticals Inc Galdesyrederivater som fxr-ligander til forebyggelsen eller behandlingen af fxr-medierede sygdomme eller tilstande
BRPI0714828A2 (pt) 2006-07-17 2013-04-09 Novartis Ag amidas de Ácido colÂnico
PE20110341A1 (es) 2006-08-15 2011-06-21 Novartis Ag COMPUESTOS HETEROCICLICOS QUE MODULAN LA ACTIVIDAD DE LA ESTEROIL-CoA-DESATURASA
EP1894928A1 (en) 2006-08-29 2008-03-05 PheneX Pharmaceuticals AG Heterocyclic fxr binding compounds
EP1894924A1 (en) 2006-08-29 2008-03-05 Phenex Pharmaceuticals AG Heterocyclic FXR binding compounds
BRPI0716777A2 (pt) 2006-09-15 2017-04-25 Volvo Lastvagnar Ab método para adaptação de uma transmissão mecânica automática em um veículo pesado
CL2007003035A1 (es) 2006-10-24 2008-05-16 Smithkline Beechman Corp Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos,
EP1918281A1 (en) 2006-11-02 2008-05-07 Laboratorios del Dr. Esteve S.A. Phenylamino-substituted piperidine compounds, their preparation and use as medicaments
CA2672373C (en) 2006-12-19 2011-08-30 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
WO2008091540A2 (en) * 2007-01-19 2008-07-31 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as tgr5 modulators and methods of use thereof
EP1947108A1 (en) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CN101668529A (zh) 2007-03-15 2010-03-10 先灵公司 用作葡聚糖合成酶抑制剂的哌嗪取代的哒嗪酮衍生物
EP2170072A4 (en) 2007-06-13 2010-10-27 Glaxosmithkline Llc Farnesoid X RECEPTOR AGONISTS
CA2690406A1 (en) 2007-07-02 2009-01-08 Glaxosmithkline Llc Farnesoid x receptor agonists
TW200906823A (en) 2007-07-16 2009-02-16 Lilly Co Eli Compounds and methods for modulating FXR
US8338628B2 (en) 2007-08-28 2012-12-25 City Of Hope Method of synthesizing alkylated bile acid derivatives
EP3293195A1 (en) 2007-09-06 2018-03-14 OHR Pharmaceutical, Inc. Compounds for use in treating diabetes
US20090163474A1 (en) 2007-10-19 2009-06-25 Wyeth FXR Agonists for the Treatment of Nonalcoholic Fatty Liver and Cholesterol Gallstone Diseases
KR101239008B1 (ko) * 2008-03-31 2013-03-04 한양대학교 산학협력단 바일산 유도체 및 그의 응용
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
EP2128158A1 (en) 2008-05-26 2009-12-02 Phenex Pharmaceuticals AG Heterocyclic cyclopropyl-substituted FXR binding compounds
AU2009276507B2 (en) 2008-07-30 2015-11-19 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
TW201022266A (en) 2008-10-23 2010-06-16 Boehringer Ingelheim Int Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use
KR20110119790A (ko) 2009-02-12 2011-11-02 엑셀리시스, 인코포레이티드 당뇨병 및 비만을 치료하는데 tgr5 효능제로서 사용되는 트리아졸 및 이미다졸 유도체
US8329904B2 (en) 2009-05-12 2012-12-11 Hoffmann-La Roche Inc. Azacyclic derivatives
EP2289883A1 (en) 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
WO2011021645A1 (ja) 2009-08-19 2011-02-24 大日本住友製薬株式会社 2環性ウレア誘導体、またはその薬学的に許容される塩
KR20120097508A (ko) 2009-11-05 2012-09-04 글락소스미스클라인 엘엘씨 벤조디아제핀 브로모도메인 억제제
WO2012087521A1 (en) 2010-12-20 2012-06-28 Irm Llc Compositions and methods for modulating farnesoid x receptors
CU24152B1 (es) 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
EP2655368A1 (en) 2010-12-20 2013-10-30 Irm Llc Compositions and methods for modulating farnesoid x receptors
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
CA2842707A1 (en) 2011-08-04 2013-02-07 Lumena Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of pancreatitis
WO2013037482A1 (en) 2011-09-15 2013-03-21 Phenex Pharmaceuticals Ag Farnesoid x receptor agonists for cancer treatment and prevention
US11154559B2 (en) 2011-09-29 2021-10-26 Ethicon Endo-Surgery, Inc. Methods and compositions of bile acids
AU2013256362A1 (en) 2012-05-01 2014-11-13 Catabasis Pharmaceuticals, Inc. Fatty acid conjugates of statin and FXR agonists: compositions and methods of use
SG10201607230SA (en) 2012-06-19 2016-10-28 Intercept Pharmaceuticals Inc Preparation, Uses And Solid Forms Of Obeticholic Acid
US9079935B2 (en) 2012-08-13 2015-07-14 The Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas Reducing risk of contracting Clostridium-difficile associated disease
WO2014036377A1 (en) 2012-08-31 2014-03-06 Metselex Methods of promoting cell viability
US9814733B2 (en) 2012-12-31 2017-11-14 A,arin Pharmaceuticals Ireland Limited Compositions comprising EPA and obeticholic acid and methods of use thereof
US20140187633A1 (en) 2012-12-31 2014-07-03 Amarin Pharmaceuticals Ireland Limited Methods of treating or preventing nonalcoholic steatohepatitis and/or primary biliary cirrhosis
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
DK2997035T3 (en) 2013-05-14 2018-07-02 Intercept Pharmaceuticals Inc 11-HYDROXY-6-SUBSTITUTED BALIC ACID DERIVATIVES AND AMINO ACID CONJUGATES THEREOF AS FARNESOID X RECEPTOR MODULATORS
WO2015017813A2 (en) 2013-08-01 2015-02-05 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of the farnesoid x receptor and uses in medicine
JP6366721B2 (ja) 2013-09-11 2018-08-01 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル B型肝炎ウイルス感染症を処置するための方法及び医薬組成物
US20150112089A1 (en) 2013-10-22 2015-04-23 Metselex, Inc. Deuterated bile acids
WO2015181275A1 (en) 2014-05-29 2015-12-03 Bar Pharmaceuticals S.R.L. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
BR112017009657A2 (pt) 2014-11-06 2018-01-23 Enanta Pharmaceuticals, Inc análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos
CN105669811B (zh) 2014-11-17 2020-09-04 正大天晴药业集团股份有限公司 新的7-酮-6β-烷基胆烷酸衍生物在制备奥贝胆酸以及其在医药领域的用途
CA2968404A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
US20160176917A1 (en) 2014-11-26 2016-06-23 Enanta Pharmaceuticals, Inc. Bile Acid Derivatives as FXR/TGR5 Agonists and Methods of Use Thereof
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
WO2016086115A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof
EP3034501A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Hydroxy containing FXR (NR1H4) modulating compounds
EP3034499A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
BR112017011972A2 (pt) 2014-12-18 2017-12-26 Novartis Ag derivados de azabicicloctano como agonistas de fxr para uso no tratamento de doenças hepáticas e gastrintestinais
RU2017130466A (ru) 2015-02-11 2019-03-12 Энанта Фармасьютикалс, Инк. Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения
TWI698430B (zh) 2015-02-13 2020-07-11 南北兄弟藥業投資有限公司 三環化合物及其在藥物中的應用
SI3277286T1 (sl) 2015-03-31 2021-09-30 Enanta Pharmaceuticals, Inc. Derivati žolčne kisline kot antagonisti FXR/TGR5 in metode za njihovo uporabo
WO2016173397A1 (zh) 2015-04-28 2016-11-03 上海翰森生物医药科技有限公司 胆酸衍生物及其制备方法和医药用途
CN106083978A (zh) 2015-04-28 2016-11-09 上海迪诺医药科技有限公司 磺酰基氨基羰基衍生物、其药物组合物及应用
WO2016173524A1 (zh) 2015-04-29 2016-11-03 正大天晴药业集团股份有限公司 鹅去氧胆酸衍生物
PT3310801T (pt) 2015-06-24 2021-06-18 Intercept Pharmaceuticals Inc Moduladores de tgr5 e métodos de utilização dos mesmos
WO2017027396A1 (en) 2015-08-07 2017-02-16 Intercept Pharmaceuticals, Inc. Methods for preparation of bile acids and derivatives thereof
CN105175473B (zh) 2015-08-19 2018-12-21 丽珠医药集团股份有限公司 一种奥贝胆酸晶型i及其制备方法、药物组合物和用途
CN106478759A (zh) 2015-08-31 2017-03-08 陕西合成药业股份有限公司 奥贝胆酸衍生物及其制备方法和用途
CN106518946A (zh) 2015-09-10 2017-03-22 上海迪诺医药科技有限公司 磺酰脲衍生物、其药物组合物及应用
HK1254057A1 (zh) 2015-09-24 2019-07-12 英特塞普特医药品公司 用於制备胆汁酸衍生物的方法和中间体
CN108348530B (zh) 2015-10-07 2023-09-29 英特塞普特医药品公司 法尼醇x受体调节剂
CN106946867B (zh) 2016-01-06 2019-11-12 广州市恒诺康医药科技有限公司 Fxr受体调节剂及其制备方法和用途
WO2017128896A1 (zh) 2016-01-26 2017-08-03 江苏豪森药业集团有限公司 Fxr激动剂及其制备方法和应用
CN106995416A (zh) 2016-01-26 2017-08-01 上海翰森生物医药科技有限公司 Fxr激动剂及其制备方法和应用
KR102788843B1 (ko) 2016-01-28 2025-03-28 치아타이 티안큉 파마수티컬 그룹 주식회사 스테로이드 유도체 fxr 작용체
CN107021957A (zh) 2016-02-01 2017-08-08 山东轩竹医药科技有限公司 Fxr受体激动剂
WO2017133521A1 (zh) 2016-02-01 2017-08-10 山东轩竹医药科技有限公司 Fxr受体激动剂
DK3419625T3 (da) 2016-02-22 2021-07-12 Novartis Ag Fremgangsmåder til anvendelse af fxr-agonister
WO2017147137A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid as fxr/tgr5 agonists and methods of use thereof
US10323061B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Heteroaryl containing bile acid analogs as FXR/TGR5 agonists and methods of use thereof
US10364267B2 (en) 2016-02-23 2019-07-30 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
PT3426348T (pt) 2016-03-11 2021-06-28 Intercept Pharmaceuticals Inc Derivado de 3-desoxi e composições farmacêuticas do mesmo
US10080742B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017189663A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
WO2017189652A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10138228B2 (en) 2016-05-18 2018-11-27 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use therof
US10149835B2 (en) 2016-05-18 2018-12-11 Elmore Patent Law Group, P.C. Isoxazole derivatives as FXR agonists and methods of use thereof
US10144729B2 (en) 2016-05-18 2018-12-04 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
AR108711A1 (es) 2016-06-13 2018-09-19 Gilead Sciences Inc Compuestos moduladores de fxr (nr1h4)
CA2968836C (en) 2016-06-13 2025-09-02 Gilead Sciences, Inc. FXR MODULATING COMPOUNDS (NR1H4)
ES2921432T3 (es) 2016-06-13 2022-08-25 Gilead Sciences Inc Derivados de azetidina como moduladores de FXR (NR1H4)
TW201808283A (zh) 2016-08-05 2018-03-16 廣東東陽光藥業有限公司 含氮三環化合物及其在藥物中的應用
WO2018039386A1 (en) 2016-08-23 2018-03-01 Ardelyx, Inc. Hormone receptor modulators for treating metabolic conditions and disorders
EP3523298A4 (en) 2016-10-04 2020-06-24 Enanta Pharmaceuticals, Inc. ISOXAZOLANALOGA AS FXR AGONISTS AND METHOD FOR USE THEREOF
CN107973790A (zh) 2016-10-22 2018-05-01 合帕吉恩治疗公司 杂环fxr调节剂
US10597391B2 (en) 2016-10-26 2020-03-24 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof
CN108017636A (zh) 2016-11-04 2018-05-11 合帕吉恩治疗公司 作为fxr调节剂的含氮杂环化合物
WO2018091540A1 (en) 2016-11-17 2018-05-24 Glaxosmithkline Biologicals Sa Zika viral antigen constructs
US10584145B2 (en) 2016-11-29 2020-03-10 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonylurea bile acid derivatives
CN106588804B (zh) 2016-12-09 2018-11-09 都创(上海)医药科技有限公司 一种作为类法尼醇x受体(fxr)的化合物的制备方法
CN106632294A (zh) 2016-12-15 2017-05-10 宁波百纳西药业有限公司 一种螺环化合物及其药物用途
WO2018133730A1 (zh) 2017-01-20 2018-07-26 四川科伦博泰生物医药股份有限公司 一种杂环化合物及其制备方法和用途
CN108341822B (zh) 2017-01-23 2021-04-16 广州市恒诺康医药科技有限公司 Fxr受体调节剂及其制备方法和应用
WO2018152171A1 (en) 2017-02-14 2018-08-23 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr agonists and methods of use thereof
WO2018170173A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
ES2971092T3 (es) 2017-04-07 2024-06-03 Enanta Pharm Inc Procedimiento para la preparación de derivados de ácidos biliares de carbamato de sulfonilo
WO2018190643A1 (en) 2017-04-12 2018-10-18 Il Dong Pharmaceutical Co., Ltd. An isoxazole derivatives as nuclear receptor agonists and used thereof
EP3632910B1 (en) 2017-05-26 2024-07-17 CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. 3,4-dihydroquinolinones as fxr receptor agonists
EP3650449B1 (en) 2017-07-06 2023-08-23 Xuanzhu Biopharmaceutical Co., Ltd. Fxr receptor agonist
WO2019160813A1 (en) 2018-02-14 2019-08-22 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
CN109053751A (zh) 2018-08-30 2018-12-21 成都海博锐药业有限公司 具有螺环结构的fxr调节剂

Also Published As

Publication number Publication date
CY1124404T1 (el) 2022-07-22
PH12017501586A1 (en) 2018-02-05
US20200109164A1 (en) 2020-04-09
ZA201707212B (en) 2021-08-25
US10457703B2 (en) 2019-10-29
WO2016161003A1 (en) 2016-10-06
US11040998B2 (en) 2021-06-22
NZ735126A (en) 2022-10-28
HRP20211066T1 (hr) 2021-10-29
EP3277286A1 (en) 2018-02-07
PT3277286T (pt) 2021-07-01
JP2018510176A (ja) 2018-04-12
MX379579B (es) 2025-03-11
EP3277286B1 (en) 2021-04-21
AU2016242861A1 (en) 2017-09-21
US20240327452A1 (en) 2024-10-03
CN107427527A (zh) 2017-12-01
BR112017020917A2 (pt) 2018-07-10
KR20170131558A (ko) 2017-11-29
IL254288B (en) 2021-04-29
JP6785788B2 (ja) 2020-11-18
RU2712099C2 (ru) 2020-01-24
IL254288A0 (en) 2017-10-31
MX2017012558A (es) 2018-04-20
LT3277286T (lt) 2021-07-26
ES2886766T3 (es) 2021-12-20
RU2017134013A (ru) 2019-04-30
RS62110B1 (sr) 2021-08-31
DK3277286T3 (da) 2021-07-05
HK1250622A1 (zh) 2019-01-11
EP3277286A4 (en) 2018-10-24
SMT202100593T1 (it) 2021-11-12
MY192135A (en) 2022-07-29
PH12017501586B1 (en) 2018-02-05
US20220402966A1 (en) 2022-12-22
RU2017134013A3 (pl) 2019-08-08
US11958879B2 (en) 2024-04-16
ZA202102769B (en) 2022-04-28
US20160289262A1 (en) 2016-10-06
HUE054960T2 (hu) 2021-10-28
SG10201910670RA (en) 2020-01-30
CN107427527B (zh) 2021-01-26
SI3277286T1 (sl) 2021-09-30
KR102681304B1 (ko) 2024-07-03
AU2016242861B2 (en) 2020-08-20
SG11201707263XA (en) 2017-10-30
CA2981503A1 (en) 2016-10-06
CA2981503C (en) 2023-09-19

Similar Documents

Publication Publication Date Title
ZA202102769B (en) Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
ZA201908293B (en) Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
ZA201703759B (en) Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
SG11201703997XA (en) Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
SG11201706089RA (en) Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
ZA201707981B (en) Compositions of obeticholic acid and methods of use
IL257235A (en) Methods for preparation of bile acids and derivatives thereof
IL252596A0 (en) History of azabicyclooctane as fxr agonists for use in the treatment of liver and gastrointestinal diseases
IL258922A (en) Methods for the preparation of obeticholic acid and derivatives thereof
SG11201610228RA (en) Methods and compositions of bile acids and salts for reduction of fat
IL256971A (en) Methods for preparation of bile acids and derivatives thereof
IL274796A (en) Oxoacridinyl acetic acid derivatives and methods of use
IL247529B (en) Preparations of choline ester lipoic acid and methods of use
SG10201709955PA (en) Methods of treatment and compositions with xanthine oxidase inhibitors
GB201810520D0 (en) Branched acid emulsifer compositions and methods of use
IL249463A0 (en) Production method for (s)-2-acetyloxypropionic acid and their derivatives
HK1244707B (en) Bile acid derivatives as fxr/tgr5 agonists