HUE054960T2 - Epesav származékok, mint az FXR/TGR5 agonista és annak felhasználási módszerei - Google Patents

Epesav származékok, mint az FXR/TGR5 agonista és annak felhasználási módszerei

Info

Publication number
HUE054960T2
HUE054960T2 HUE16774118A HUE16774118A HUE054960T2 HU E054960 T2 HUE054960 T2 HU E054960T2 HU E16774118 A HUE16774118 A HU E16774118A HU E16774118 A HUE16774118 A HU E16774118A HU E054960 T2 HUE054960 T2 HU E054960T2
Authority
HU
Hungary
Prior art keywords
fxr
methods
acid derivatives
bile acid
tgr5 agonists
Prior art date
Application number
HUE16774118A
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 Pharm 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 Pharm Inc filed Critical Enanta Pharm Inc
Publication of HUE054960T2 publication Critical patent/HUE054960T2/hu

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
    • 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
    • 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
    • C07J41/0055Normal 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
    • 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
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
HUE16774118A 2015-03-31 2016-03-30 Epesav származékok, mint az FXR/TGR5 agonista és annak felhasználási módszerei HUE054960T2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562140927P 2015-03-31 2015-03-31
US201662287267P 2016-01-26 2016-01-26

Publications (1)

Publication Number Publication Date
HUE054960T2 true HUE054960T2 (hu) 2021-10-28

Family

ID=57007583

Family Applications (1)

Application Number Title Priority Date Filing Date
HUE16774118A HUE054960T2 (hu) 2015-03-31 2016-03-30 Epesav származékok, mint az FXR/TGR5 agonista és annak felhasználási módszerei

Country Status (27)

Country Link
US (4) US10457703B2 (hu)
EP (1) EP3277286B1 (hu)
JP (1) JP6785788B2 (hu)
KR (1) KR102681304B1 (hu)
CN (1) CN107427527B (hu)
AU (1) AU2016242861B2 (hu)
CA (1) CA2981503C (hu)
CY (1) CY1124404T1 (hu)
DK (1) DK3277286T3 (hu)
ES (1) ES2886766T3 (hu)
HK (1) HK1250622A1 (hu)
HR (1) HRP20211066T1 (hu)
HU (1) HUE054960T2 (hu)
IL (1) IL254288B (hu)
LT (1) LT3277286T (hu)
MX (1) MX2017012558A (hu)
MY (1) MY192135A (hu)
NZ (1) NZ735126A (hu)
PH (1) PH12017501586B1 (hu)
PL (1) PL3277286T3 (hu)
PT (1) PT3277286T (hu)
RS (1) RS62110B1 (hu)
RU (1) RU2712099C2 (hu)
SG (2) SG11201707263XA (hu)
SI (1) SI3277286T1 (hu)
WO (1) WO2016161003A1 (hu)
ZA (2) ZA201707212B (hu)

Families Citing this family (27)

* 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
EP3215179A4 (en) 2014-11-06 2018-07-25 Enanta Pharmaceuticals, Inc. Bile acid analogs an 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
WO2016086169A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs 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
SG11201707263XA (en) 2015-03-31 2017-10-30 Enanta Pharm Inc Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
NZ745250A (en) * 2016-01-28 2024-08-30 Chia Tai Tianqing Pharmaceutical Group Co Ltd Steroid derivative fxr agonist
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
US10323060B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid 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
CA3045023A1 (en) 2016-11-29 2018-06-07 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
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof
KR102624997B1 (ko) * 2017-04-07 2024-01-12 이난타 파마슈티칼스, 인코포레이티드 술포닐 카바메이트 담즙산 유도체의 제조 방법
IL271343B2 (en) 2017-06-23 2023-12-01 Intercept Pharmaceuticals Inc Methods and intermediates for the preparation of bile acid derivatives
JP7308811B2 (ja) * 2017-07-26 2023-07-14 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド ステロイド系誘導体fxrアゴニストの製造方法
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
WO2021009332A1 (en) 2019-07-18 2021-01-21 Enyo Pharma Method for decreasing adverse-effects of interferon
EP4041722A4 (en) 2019-10-07 2023-12-13 Kallyope, Inc. GPR119 AGONISTS
AU2021207253A1 (en) 2020-01-15 2022-06-09 Centre National De La Recherche Scientifique Use of FXR agonists for treating an infection by hepatitis D virus
IL298306A (en) 2020-05-19 2023-01-01 Kallyope Inc ampk operators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
MX2023008365A (es) 2021-01-14 2023-10-04 Enyo Pharma Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv.
EP4329761A1 (en) 2021-04-28 2024-03-06 ENYO Pharma Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
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
US4917826A (en) 1985-10-18 1990-04-17 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
TW289020B (hu) 1993-05-08 1996-10-21 Hoechst Sktiengesellschaft
TW289757B (hu) 1993-05-08 1996-11-01 Hoechst Ag
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
JP3696884B2 (ja) 1994-03-25 2005-09-21 アイソテクニカ、インコーポレーテッド ジュウテリウム化による薬物の効能の増強
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
US6639078B1 (en) 1998-12-23 2003-10-28 Smithkline Beecham Corporation Assays for ligands for nuclear receptors
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
AU782447C (en) 1999-04-30 2006-07-13 Regents Of The University Of Michigan, The Use of benzodiazepines for treating autoimmune diseases induced by apoptosis
US20020098999A1 (en) * 2000-10-06 2002-07-25 Gallop Mark A. Compounds for sustained release of orally delivered drugs
US6992076B2 (en) * 2000-10-06 2006-01-31 Xenoport, Inc. Bile-acid derived compounds for providing sustained systemic concentrations of drugs after oral administration
ES2248581T3 (es) 2001-03-12 2006-03-16 Intercept Pharmaceuticals, Inc. Esteroides como agonistas de fxr.
EP1285914B1 (en) 2001-08-13 2007-12-19 PheneX Pharmaceuticals AG Nr1h4 nuclear receptor binding compounds
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
US7319109B2 (en) 2002-11-22 2008-01-15 Smith Kline Beecham Corporation Farnesoid X receptor agonists
EP1690538A4 (en) 2003-12-02 2009-02-25 Shionogi & Co ISOXAZOLE DERIVATIVE AGONISTIC ACTION AGAINST PEROXISOM PROLIFERATOR ACTIVATED RECEPTOR
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
ES2609395T5 (es) 2004-03-12 2021-08-06 Intercept Pharmaceuticals Inc Tratamiento de la fibrosis usando ligandos de Fxr
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
WO2007076260A2 (en) 2005-12-19 2007-07-05 Smithkline Beecham Corporation Farnesoid x receptor agonists
BRPI0706747A2 (pt) 2006-01-30 2011-04-05 Exelixis Inc 4-aril-2-amino-pirimidinas ou 4-aril-2-aminoalquil-pirimidinas como moduladores jak-2 e composições farmacêuticas que os contenham
AU2007211279B2 (en) 2006-02-01 2013-02-14 Brigham Young University Cationic steroid antimicrobial compositions and methods of use
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
AU2007215207A1 (en) 2006-02-14 2007-08-23 Intercept Pharmaceuticals, Inc. Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
EP2001897A2 (en) 2006-03-22 2008-12-17 Syndexa Pharmaceuticals Corporation Compounds and methods for treatment of disorders associated with er stress
EP2029547B1 (en) 2006-05-24 2010-04-28 Eli Lilly And Company Fxr agonists
PE20080344A1 (es) 2006-06-27 2008-06-09 Sanofi Aventis Compuestos 8-azabiciclo[3.2.1]oct-8-il-1,2,3,4-tetrahidroquinolina sustituidos como inhibidores 11b-hsd1
AU2007265457C1 (en) 2006-06-27 2012-11-29 Intercept Pharmaceuticals, Inc. Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
WO2008009407A2 (en) 2006-07-17 2008-01-24 Novartis Ag Sulphonylaminocarbonyl derivatives of bile acid amides for use as immunomodulators
KR20140019873A (ko) 2006-08-15 2014-02-17 노파르티스 아게 증가된 지질 수준과 관련된 질환의 치료에 적합한 헤테로시클릭 화합물
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
US20100063697A1 (en) 2006-09-15 2010-03-11 Volvo Lastvagnar Ab Method for adapting an automatic mechanical transmission on a heavy vehicle
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
JP2010513458A (ja) 2006-12-19 2010-04-30 ファイザー・プロダクツ・インク H−pgdsの阻害剤としてのニコチンアミド誘導体、およびプロスタグランジンd2の仲介による疾患を治療するためのその使用
EP1947108A1 (en) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CA2676417C (en) * 2007-01-19 2016-06-28 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
JP2010521463A (ja) 2007-03-15 2010-06-24 シェーリング コーポレイション グルカンシンターゼの阻害剤として有用なピペラジン置換ビリダジノン誘導体
JP2010529996A (ja) 2007-06-13 2010-09-02 グラクソスミスクライン エルエルシー ファルネソイドx受容体アゴニスト
KR20100044810A (ko) 2007-07-02 2010-04-30 글락소스미스클라인 엘엘씨 파네소이드 x 수용체 효능제
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
US9365608B2 (en) 2007-09-06 2016-06-14 Ohr Pharmaceutical, Inc. Method for 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
BRPI0916735B8 (pt) 2008-07-30 2021-05-25 Intercept Pharmaceuticals Inc compostos moduladores de tgr5, composições farmacêuticas compreendendo os mesmos e seus usos
WO2010046445A2 (en) 2008-10-23 2010-04-29 Boehringer Ingelheim International Gmbh Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use
EP2396304A1 (en) 2009-02-12 2011-12-21 Exelixis, Inc. Triazole and imidazole derivatives for use as tgr5 agonists in the treatment of diabetes and obesity
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
ME02356B (me) 2009-11-05 2016-06-20 Glaxosmithkline Llc Inhibitor bromodomena benzodiazepina
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
JP2014500318A (ja) 2010-12-20 2014-01-09 アイアールエム・リミテッド・ライアビリティ・カンパニー ファルネソイドx受容体を調節するための組成物および方法
JP2014500319A (ja) 2010-12-20 2014-01-09 アイアールエム・リミテッド・ライアビリティ・カンパニー ファルネソイドx受容体を調節するための組成物および方法
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
JP2014521699A (ja) 2011-08-04 2014-08-28 ルメナ ファーマシューティカルズ,インク. 膵臓炎の処置用の胆汁酸再利用阻害剤
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
CA2871772A1 (en) 2012-05-01 2013-11-07 Catabasis Pharmaceuticals, Inc. Fatty acid conjugates of statin and fxr agonists; compositions and method of uses
IN2014MN02561A (hu) 2012-06-19 2015-09-04 Intercept Pharmaceuticals Inc
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
WO2014036379A2 (en) 2012-08-31 2014-03-06 Metselex Bile acids prevent or abolish progression of parkinson's and related neurodegenerative diseases
US20140187633A1 (en) 2012-12-31 2014-07-03 Amarin Pharmaceuticals Ireland Limited Methods of treating or preventing nonalcoholic steatohepatitis and/or primary biliary cirrhosis
US9814733B2 (en) 2012-12-31 2017-11-14 A,arin Pharmaceuticals Ireland Limited Compositions comprising EPA and obeticholic acid and methods of use thereof
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
HUE037996T2 (hu) 2013-05-14 2018-09-28 Intercept Pharmaceuticals Inc Epesavak 11 hidroxi-6-helyettesített származékai és ezek aminosav konjugátumai farnezoid X receptor modulátorokként
AU2014296023B2 (en) 2013-08-01 2020-02-06 The Penn State Research Foundation Inhibitors of the farnesoid X receptor and uses in medicine
KR101949251B1 (ko) 2013-09-11 2019-02-18 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) B형간염바이러스 감염의 치료 방법 및 치료용 약학적 조성물
US20150112089A1 (en) 2013-10-22 2015-04-23 Metselex, Inc. Deuterated bile acids
US10407462B2 (en) 2014-05-29 2019-09-10 Bar Pharmaceuticals S.R.L. Cholane derivatives for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases
EP3215179A4 (en) 2014-11-06 2018-07-25 Enanta Pharmaceuticals, Inc. Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
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
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives 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
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
WO2016086169A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs 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
EP3233083A1 (en) 2014-12-18 2017-10-25 Novartis AG Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases
AU2016219266A1 (en) 2015-02-11 2017-08-10 Enanta Pharmaceuticals, Inc. Bile acid analogs as FXR/TGR5 agonists and methods of use thereof
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
SG11201707263XA (en) 2015-03-31 2017-10-30 Enanta Pharm Inc Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
WO2016173493A1 (en) 2015-04-28 2016-11-03 Shanghai De Novo Pharmatech Co. Ltd. Sulfonylaminocarbonyl derivative, pharmaceutical composition and uses thereof
JP2018519246A (ja) 2015-04-28 2018-07-19 ジエンス ハンセン ファーマセウティカル グループ カンパニー リミテッド コール酸誘導体、及びその製造方法及び医薬用途
TW201704251A (zh) 2015-04-29 2017-02-01 正大天晴藥業集團股份有限公司 鵝去氧膽酸衍生物
KR20180043247A (ko) 2015-06-19 2018-04-27 인터셉트 파마슈티컬즈, 인크. Tgr5 조절제 및 이를 사용하는 방법
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
CA2999302A1 (en) 2015-09-24 2017-03-30 Intercept Pharmaceuticals, Inc. Methods and intermediates for the preparation bile acid derivatives
MX2018004186A (es) 2015-10-07 2018-05-17 Intercept Pharmaceuticals Inc Moduladores del receptor x farnesoide.
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
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
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
NZ745250A (en) 2016-01-28 2024-08-30 Chia Tai Tianqing Pharmaceutical Group Co Ltd Steroid derivative fxr agonist
CN108602811B (zh) 2016-02-01 2021-11-16 轩竹生物科技有限公司 Fxr受体激动剂
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
ES2878575T3 (es) 2016-02-22 2021-11-19 Novartis Ag Métodos para usar agonistas del FXR
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
US10323060B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof
SI3426348T1 (sl) 2016-03-11 2021-11-30 Intercept Pharmaceuticals, Inc. Derivat 3-dezoksi in njegovi farmacevtski sestavki
US10080742B2 (en) 2016-04-26 2018-09-25 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
WO2017189663A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
WO2017201152A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
WO2017201155A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. lSOXAZOLE 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
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
ES2921432T3 (es) 2016-06-13 2022-08-25 Gilead Sciences Inc Derivados de azetidina como moduladores de FXR (NR1H4)
AR108711A1 (es) 2016-06-13 2018-09-19 Gilead Sciences Inc Compuestos 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
EP3954684A1 (en) 2016-08-23 2022-02-16 Ardelyx, Inc. Process for the preparation of hormone receptor modulators for treating metabolic conditions and disorders
US10450306B2 (en) 2016-10-04 2019-10-22 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of 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
BE1025121B1 (fr) 2016-11-17 2018-11-05 Glaxosmithkline Biologicals Sa Constructions antigeniques du virus zika
CA3045023A1 (en) 2016-11-29 2018-06-07 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
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof
US20200131129A1 (en) 2017-03-15 2020-04-30 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
KR102624997B1 (ko) 2017-04-07 2024-01-12 이난타 파마슈티칼스, 인코포레이티드 술포닐 카바메이트 담즙산 유도체의 제조 방법
WO2018190643A1 (en) 2017-04-12 2018-10-18 Il Dong Pharmaceutical Co., Ltd. An isoxazole derivatives as nuclear receptor agonists and used thereof
AU2018272359B2 (en) 2017-05-26 2022-03-03 Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. Lactam compound as FXR receptor agonist
MX2020000268A (es) 2017-07-06 2020-07-22 Xuanzhu Biopharmaceutical Co Ltd Agonista de fxr.
US10829486B2 (en) 2018-02-14 2020-11-10 Enanta Pharmacueticals, 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
PH12017501586A1 (en) 2018-02-05
SI3277286T1 (sl) 2021-09-30
CN107427527B (zh) 2021-01-26
KR102681304B1 (ko) 2024-07-03
RU2017134013A3 (hu) 2019-08-08
SG11201707263XA (en) 2017-10-30
CN107427527A (zh) 2017-12-01
WO2016161003A1 (en) 2016-10-06
PL3277286T3 (pl) 2021-11-08
DK3277286T3 (da) 2021-07-05
US20240327452A1 (en) 2024-10-03
HK1250622A1 (zh) 2019-01-11
CA2981503A1 (en) 2016-10-06
RU2712099C2 (ru) 2020-01-24
JP2018510176A (ja) 2018-04-12
IL254288B (en) 2021-04-29
SG10201910670RA (en) 2020-01-30
KR20170131558A (ko) 2017-11-29
ES2886766T3 (es) 2021-12-20
HRP20211066T1 (hr) 2021-10-29
CY1124404T1 (el) 2022-07-22
EP3277286A4 (en) 2018-10-24
ZA202102769B (en) 2022-04-28
PH12017501586B1 (en) 2018-02-05
US20220402966A1 (en) 2022-12-22
LT3277286T (lt) 2021-07-26
CA2981503C (en) 2023-09-19
AU2016242861A1 (en) 2017-09-21
US11958879B2 (en) 2024-04-16
RS62110B1 (sr) 2021-08-31
AU2016242861B2 (en) 2020-08-20
IL254288A0 (en) 2017-10-31
NZ735126A (en) 2022-10-28
MY192135A (en) 2022-07-29
US20160289262A1 (en) 2016-10-06
US20200109164A1 (en) 2020-04-09
RU2017134013A (ru) 2019-04-30
JP6785788B2 (ja) 2020-11-18
EP3277286B1 (en) 2021-04-21
US10457703B2 (en) 2019-10-29
ZA201707212B (en) 2021-08-25
PT3277286T (pt) 2021-07-01
MX2017012558A (es) 2018-04-20
US11040998B2 (en) 2021-06-22
EP3277286A1 (en) 2018-02-07
BR112017020917A2 (pt) 2018-07-10

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
HK1244708A1 (zh) 作爲fxr/tgr5激動劑的胆汁酸類似物及其使用方法
HK1245100A1 (zh) 作為fxr/tgr5激動劑的膽汁酸類似物及其使用方法
HK1243930A1 (zh) 作爲fxr/tgr5激動劑的膽汁酸類似物和其使用方法
ZA201707981B (en) Compositions of obeticholic acid and methods of use
IL252596A0 (en) History of azabicyclooctane as fxr agonists for use in the treatment of liver and gastrointestinal diseases
IL247529B (en) Preparations of choline ester lipoic acid and methods of use
SG11201509738RA (en) Methods of treatment and compositions with xanthine oxidase inhibitors
GB201810520D0 (en) Branched acid emulsifer compositions and methods of use
HK1232209A1 (zh) 製備 -乙酰氧基丙酸及其衍生物的方法