CL2021001877A1 - Compuestos moduladores de fxr (nr1h4) - Google Patents

Compuestos moduladores de fxr (nr1h4)

Info

Publication number
CL2021001877A1
CL2021001877A1 CL2021001877A CL2021001877A CL2021001877A1 CL 2021001877 A1 CL2021001877 A1 CL 2021001877A1 CL 2021001877 A CL2021001877 A CL 2021001877A CL 2021001877 A CL2021001877 A CL 2021001877A CL 2021001877 A1 CL2021001877 A1 CL 2021001877A1
Authority
CL
Chile
Prior art keywords
fxr
nr1h4
compound
modulating compounds
compounds
Prior art date
Application number
CL2021001877A
Other languages
English (en)
Inventor
William J Watkins
Joshua A Kaplan
Peter A Blomgren
Kevin S Currie
Morin Mae Frick
Elizabeth M Horstman
Jeffrey E Kropf
Original Assignee
Gilead Sciences 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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of CL2021001877A1 publication Critical patent/CL2021001877A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La presente descripción se refiere en general a un compuesto de fórmula (I) que se une a FXR y actúa como agonista de FXR. La divulgación se refiere además al uso del compuesto para la preparación de un medicamento para el tratamiento de enfermedades y/o afecciones a través de la unión de dicho receptor nuclear por dichos compuestos y a un proceso para la síntesis de dicho compuesto.
CL2021001877A 2019-01-15 2021-07-14 Compuestos moduladores de fxr (nr1h4) CL2021001877A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201962792714P 2019-01-15 2019-01-15

Publications (1)

Publication Number Publication Date
CL2021001877A1 true CL2021001877A1 (es) 2022-01-07

Family

ID=69740522

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2021001877A CL2021001877A1 (es) 2019-01-15 2021-07-14 Compuestos moduladores de fxr (nr1h4)

Country Status (27)

Country Link
US (2) US11225473B2 (es)
EP (2) EP4360632A2 (es)
JP (2) JP7265635B2 (es)
KR (1) KR20210114457A (es)
CN (1) CN113302190A (es)
AR (1) AR117814A1 (es)
AU (2) AU2020209564B2 (es)
BR (1) BR112021011762A2 (es)
CA (1) CA3124702A1 (es)
CL (1) CL2021001877A1 (es)
CO (1) CO2021009240A2 (es)
CR (1) CR20210385A (es)
DK (1) DK3911647T3 (es)
DO (2) DOP2021000148A (es)
EA (1) EA202191566A1 (es)
FI (1) FI3911647T3 (es)
HR (1) HRP20240265T1 (es)
IL (1) IL284591A (es)
LT (1) LT3911647T (es)
MX (1) MX2021008518A (es)
PE (1) PE20211907A1 (es)
PT (1) PT3911647T (es)
SG (1) SG11202107434PA (es)
SI (1) SI3911647T1 (es)
TW (1) TWI733307B (es)
WO (1) WO2020150136A1 (es)
ZA (1) ZA202104705B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6678779B2 (ja) 2016-06-13 2020-04-08 ギリアード サイエンシーズ, インコーポレイテッド Fxr(nr1h4)調節化合物
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
AU2018243719B2 (en) 2017-03-28 2021-01-21 Gilead Sciences, Inc. Therapeutic combinations for treating liver diseases
US20210393662A1 (en) * 2018-10-18 2021-12-23 Avolynt Use of sglt2 inhibitors to treat primary sclerosing cholangitis
CA3233305A1 (en) 2019-02-19 2020-08-27 Gilead Sciences, Inc. Solid forms of fxr 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
US11478533B2 (en) 2020-04-27 2022-10-25 Novo Nordisk A/S Semaglutide for use in medicine
EP4229043A1 (en) * 2020-10-15 2023-08-23 Eli Lilly and Company Polymorphs of an fxr agonist
WO2022152770A1 (en) 2021-01-14 2022-07-21 Enyo Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
CA3201686A1 (en) 2021-01-14 2022-07-21 Fabiola Terzi Method for treating chronic kidney diseases
WO2022229302A1 (en) 2021-04-28 2022-11-03 Enyo Pharma Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
TW202311256A (zh) 2021-06-18 2023-03-16 美商基利科學股份有限公司 用於治療fxr誘發之搔癢之il-31調節劑

Family Cites Families (199)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ193011A (en) 1979-03-19 1983-03-15 Ici Australia Ltd Diarylamine derivatives intermediates herbicidal compositions
EP0287959B1 (de) 1987-04-21 1993-04-28 BASF Aktiengesellschaft p-Phenoxy-phenoxymethyl-fünfring-heteroaromaten
JP3121061B2 (ja) 1991-10-04 2000-12-25 塩野義製薬株式会社 アルコキシイミノアセトアミド類製造用中間体の製造法およびそれに用いる中間体
DE4137940A1 (de) 1991-11-18 1993-05-19 Basf Ag 3-isoxazolylphenylverbindungen, ihre herstellung und ihre verwendung
US5258551A (en) 1991-12-18 1993-11-02 Shionogi & Co., Ltd. Process for producing α-ketoamide derivative
AU5891494A (en) 1993-01-29 1994-08-15 Nippon Soda Co., Ltd. Heterocyclic derivative
WO1994024095A1 (en) 1993-04-16 1994-10-27 Abbott Laboratories Immunosuppressive agents
IL112721A0 (en) 1994-03-10 1995-05-26 Zeneca Ltd Azole derivatives
EP0804434A1 (en) 1994-08-02 1997-11-05 MERCK SHARP & DOHME LTD. Azetidine, pyrrolidine and piperidine derivatives
GB9501865D0 (en) 1995-01-31 1995-03-22 Merck Sharp & Dohme Therapeutic agents
US5633272A (en) 1995-02-13 1997-05-27 Talley; John J. Substituted isoxazoles for the treatment of inflammation
DE19536811A1 (de) 1995-10-02 1997-04-03 Basf Ag Zwischenprodukte und Verfahren zur Herstellung von substituierten Salicylsäurederivaten als Pflanzenschutzmittel
ES2183140T3 (es) 1996-02-13 2003-03-16 Searle & Co Combinaciones, que tienen efectos inmunosupresores, que contienen un inhibidor de ciclooxigenasa-2 y un inhibidor de leucotrieno a4 hidrolasa.
DE69940958D1 (de) 1998-12-23 2009-07-16 Glaxo Group Ltd Bestimmungsmethode fur liganden der nuklearen rezeptoren
WO2000077011A1 (en) 1999-06-11 2000-12-21 Allergan Sales, Inc. Organosilyl compounds having nuclear hormone receptor modulating activity
US7022725B2 (en) 2000-11-17 2006-04-04 Takeda Pharmaceutical Company Limited Isoxazole derivatives
US20040131670A1 (en) 2001-04-17 2004-07-08 Ping Gao Pellicle-resistant gelatin capsule
US20040105884A1 (en) 2001-04-17 2004-06-03 Ping Gao Pharmaceutical dosage form comprising a sulfite compound
US20040105883A1 (en) 2001-04-17 2004-06-03 Ping Gao Pharmaceutical dosage form capable of maintaining stable dissolution profile upon storage
US20040105885A1 (en) 2001-04-17 2004-06-03 Ping Gao Gelatin capsule exhibiting reduced cross-linking
EP1405636A4 (en) 2001-06-26 2009-04-15 Takeda Pharmaceutical REGULATOR OF RECTINTOR FUNCTION RELATING TO RETINOIDS
US20070010562A1 (en) 2001-08-13 2007-01-11 Ulrike Bauer Nr1h4 nuclear receptor binding compounds
EP1285914B1 (en) 2001-08-13 2007-12-19 PheneX Pharmaceuticals AG Nr1h4 nuclear receptor binding compounds
EP1423113A4 (en) 2001-08-13 2007-04-18 Phenex Pharmaceuticals Ag NR1H4 NUCLEAR RECEPTOR BINDING COMPOUNDS
WO2003080803A2 (en) 2002-03-21 2003-10-02 Smithkline Beecham Corporation Methods of using farnesoid x receptor (fxr) agonists
US7595311B2 (en) 2002-05-24 2009-09-29 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
EP1536790A2 (en) 2002-08-09 2005-06-08 AstraZeneca AB Oxadiazoles as modulators of metabotropic glutamate receptor-5
EP1581525A2 (en) 2002-08-09 2005-10-05 AstraZeneca AB Compounds having an activity at metabotropic glutamate receptors
WO2004014881A2 (en) 2002-08-09 2004-02-19 Astra Zeneca Ab '1,2,4'oxadiazoles as modulators of metabotropic glutamate receptor-5
EP1407774A1 (en) 2002-09-10 2004-04-14 LION Bioscience AG 2-Amino-4-quinazolinones as LXR nuclear receptor binding compounds
WO2004046162A2 (en) 2002-11-14 2004-06-03 The Scripps Research Institute Non-steroidal fxr agonists
US20050143449A1 (en) 2002-11-15 2005-06-30 The Salk Institute For Biological Studies Non-steroidal farnesoid X receptor modulators and methods for the use thereof
EP1562915A1 (en) 2002-11-22 2005-08-17 SmithKline Beecham Corporation Farnesoid x receptor agonists
US20070166710A1 (en) 2003-03-31 2007-07-19 Markus Stoffel Methods for inhibiting adipogenesis and for treating type 2 diabetes
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
US7585881B2 (en) 2004-02-18 2009-09-08 Astrazeneca Ab Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
AU2005245411B2 (en) 2004-05-14 2009-04-23 Irm Llc Compounds and compositions as PPAR modulators
MY144903A (en) 2004-06-17 2011-11-30 Novartis Ag Pyrrolopyridine derivatives and their use as crth2 antagonists
EP1812071A2 (en) 2004-10-13 2007-08-01 PTC Therapeutics, Inc. Compounds for nonsense suppression, use of these compounds for the manufacture of a medicament for treating somatic mutation-related diseases
JP2008137894A (ja) 2005-03-22 2008-06-19 Nippon Kayaku Co Ltd 新規なアセチレン誘導体
WO2006132197A1 (ja) 2005-06-07 2006-12-14 Shionogi & Co., Ltd. I型11βヒドロキシステロイド脱水素酵素阻害活性を有するヘテロ環化合物
WO2007070796A1 (en) 2005-12-15 2007-06-21 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
EP1962838B1 (en) 2005-12-19 2011-09-28 GlaxoSmithKline LLC Farnesoid x receptor agonists
US7560551B2 (en) 2006-01-23 2009-07-14 Amgen Inc. Aurora kinase modulators and method of use
CN101374834B (zh) 2006-02-03 2011-12-14 伊莱利利公司 用于调节fxr的化合物和方法
BRPI0707794A2 (pt) 2006-02-14 2011-05-10 Intercept Pharmaceuticals Inc compostos derivados de Ácido biliar, formulaÇÕes e composiÇÕes farmacÊuticas, bem como uso de ditos compostos
US20070276050A1 (en) 2006-02-27 2007-11-29 Gilead Sciences, Inc. Methods for identifying ASK1 inhibitors useful for preventing and/or treating cardiovascular diseases
WO2007110237A2 (en) 2006-03-28 2007-10-04 Novartis Ag Amide derivatives and their application for the treatment of g protein related diseases
EP2007759A4 (en) 2006-04-17 2010-12-22 Neuromed Pharmaceuticals Ltd ISOXAZOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
PL2029547T3 (pl) 2006-05-24 2010-09-30 Lilly Co Eli Agoniści FXR
JP5225984B2 (ja) 2006-05-24 2013-07-03 イーライ リリー アンド カンパニー Fxrを調節する化合物及び方法
ATE549338T1 (de) 2006-05-24 2012-03-15 Boehringer Ingelheim Int Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
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
US8222256B2 (en) 2006-07-05 2012-07-17 Exelixis, Inc. Methods of using IGFIR and ABL kinase modulators
US20080032990A1 (en) 2006-07-07 2008-02-07 Khalifah Raja G Inhibitors of advanced glycation end products
EA200900072A1 (ru) 2006-07-07 2009-06-30 Бёрингер Ингельхайм Интернациональ Гмбх Фенилзамещенные гетероарильные производные и их применение в качестве противоопухолевых средств
EP1894924A1 (en) 2006-08-29 2008-03-05 Phenex Pharmaceuticals AG Heterocyclic FXR binding compounds
EP1894928A1 (en) 2006-08-29 2008-03-05 PheneX Pharmaceuticals AG Heterocyclic fxr binding compounds
US8193225B2 (en) 2006-10-13 2012-06-05 The Board Of Regents Of The University Of Texas System Isoxazole amides, derivatives and methods of chemical induction of neurogenesis
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,
US8501933B2 (en) 2006-11-09 2013-08-06 Roche Palo Alto Llc Thiazole and oxazole-substituted arylamides as P2X3 and P2X2/3 antagonists
CN101679297B (zh) 2006-12-08 2012-01-11 埃克塞利希斯股份有限公司 Lxr和fxr调节剂
GB0625842D0 (en) 2006-12-22 2007-02-07 Argenta Discovery Ltd Indolizine derivatives
US20090105251A1 (en) 2007-01-25 2009-04-23 Benjamin Jones Renin inhibitors
JP5254999B2 (ja) 2007-02-09 2013-08-07 ダウ アグロサイエンシィズ エルエルシー 特定の置換スルフィルイミン類を殺虫性スルホキシイミン類に酸化する方法
US7511149B2 (en) 2007-02-09 2009-03-31 Dow Agrosciences Llc Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines
AU2008219748B2 (en) 2007-02-26 2012-05-03 Corteva Agriscience Llc Process for the preparation of certain substituted sulfilimines
WO2008157270A1 (en) 2007-06-13 2008-12-24 Smithkline Beecham Corporation Farnesoid x receptor agonists
JP2008308448A (ja) 2007-06-15 2008-12-25 Sankyo Agro Kk (3−硫黄原子置換フェニル)へテロアリール誘導体
WO2008155054A1 (en) 2007-06-20 2008-12-24 F. Hoffmann-La Roche Ag Farnesoid-x-receptor mutants, and crystallisation thereof
WO2009005998A1 (en) 2007-07-02 2009-01-08 Smithkline Beecham Corporation Farnesoid x receptor agonists
EP2176249A2 (en) 2007-07-02 2010-04-21 Boehringer Ingelheim International GmbH New chemical compounds
EA201000051A1 (ru) 2007-07-13 2010-08-30 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Противовирусные соединения, композиции и способы использования
US20090197880A1 (en) 2007-07-13 2009-08-06 Genelabs Technologies, Inc. Anti-viral compounds, compositions, and methods of use
TW200906823A (en) 2007-07-16 2009-02-16 Lilly Co Eli Compounds and methods for modulating FXR
US20100256145A1 (en) 2007-08-01 2010-10-07 H. Lundbeck A/S Use of kcnq potassium channel openers for reducing symptoms of or treating disorders or conditions wherein the dopaminergic system is disrupted
US8188080B2 (en) 2007-10-17 2012-05-29 Sanford-Burnham Medical Research Institute VHR protein tyrosine phosphatase inhibitors, compositions and methods of use
US20090143451A1 (en) 2007-11-14 2009-06-04 Andrews William H Compounds that increase telomerase reverse transcriptase (tert) expression and methods for using the same
AU2008339572B2 (en) 2007-12-21 2012-05-10 Astrazeneca Ab Bicyclic derivatives for use in the treatment of androgen receptor associated conditions
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
CA2724232A1 (en) 2008-05-13 2009-11-19 Boehringer Ingelheim International Gmbh Sulfone compounds which modulate the cb2 receptor
AU2009249180A1 (en) 2008-05-19 2009-11-26 Burnham Institute For Medical Research Intestinal Alkaline Phosphatase modulators and uses thereof
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EP2128158A1 (en) 2008-05-26 2009-12-02 Phenex Pharmaceuticals AG Heterocyclic cyclopropyl-substituted FXR binding compounds
AU2009257635A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. 5H-Pyrrolo [2,3-b] pyrazine derivatives for kinase modulation, and indications therefor
US8822513B2 (en) 2010-03-01 2014-09-02 Gtx, Inc. Compounds for treatment of cancer
KR20110036586A (ko) 2008-06-23 2011-04-07 바스프 에스이 동물 해충의 퇴치를 위한 술폭시민아미드 화합물
WO2010006096A1 (en) 2008-07-11 2010-01-14 Smithkline Beecham Corporation Processes for the preparation of anti-viral compounds and compositions containing them
EP2318381A1 (en) 2008-08-25 2011-05-11 Dow Global Technologies LLC Process for preparing isoxazole compounds
US20120021519A1 (en) 2008-09-19 2012-01-26 Presidents And Fellows Of Harvard College Efficient induction of pluripotent stem cells using small molecule compounds
AU2009296048A1 (en) 2008-09-25 2010-04-01 F. Hoffmann-La Roche Ag 2,3-substituted indazole or 4,5,6,7-tetrahydro-indazoles as FXR modulators against dyslipidemia and related diseases
KR101444988B1 (ko) 2008-09-25 2014-09-26 에프. 호프만-라 로슈 아게 3-아미노-인다졸 또는 3-아미노-4,5,6,7-테트라하이드로-인다졸 유도체
WO2010036362A1 (en) 2008-09-26 2010-04-01 Wyeth 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors
KR20110082145A (ko) 2008-10-21 2011-07-18 메타볼렉스, 인코포레이티드 아릴 gpr120 수용체 작동약 및 이의 용도
CA2744946A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
WO2010093191A2 (en) 2009-02-13 2010-08-19 Lg Life Sciences Ltd. Novel compounds effective as xanthine oxidase inhibitors, method for preparing the same, and pharmaceutical composition containing the same
FR2943059A1 (fr) 2009-03-16 2010-09-17 Sanofi Aventis Derives de n-°6-aza-bicyclo°3.2.1!oct-5-yl)-aryl-methyl!- heterobenzamide,leur preparation et leur application en therapeutique
WO2011003793A1 (en) 2009-07-06 2011-01-13 Basf Se Pyridazine compounds for controlling invertebrate pests
US8883832B2 (en) 2009-07-06 2014-11-11 Aerpio Therapeutics Inc. Compounds, compositions, and methods for preventing metastasis of cancer cells
TWI598347B (zh) 2009-07-13 2017-09-11 基利科學股份有限公司 調節細胞凋亡信號之激酶的抑制劑
BR112012001597A2 (pt) 2009-07-24 2015-09-01 Basf Se Método para controlar e/ou combater pestes de invertebrados, método para a proteção do material de propagação de planta e/ou das plantas que crescem do mesmo, material de propagação de planta e método para tratar ou proteger um animal de infestação ou infecção por parasitas
US9212177B2 (en) 2009-08-05 2015-12-15 Versitech Limited Antiviral compounds and methods of making and using thereof
EP2289883A1 (en) 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
CN102656151A (zh) 2009-09-04 2012-09-05 扎里卡斯药品有限公司 治疗疼痛和癫痫的取代的杂环衍生物
US9095596B2 (en) 2009-10-15 2015-08-04 Southern Research Institute Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
KR20120130777A (ko) 2010-03-01 2012-12-03 유니버시티 오브 테네시 리서치 파운데이션 암 치료용 화합물
WO2011156640A2 (en) 2010-06-09 2011-12-15 Afraxis, Inc. 8-(HETEROARYLMETHYL)PYRIDO[2,3-d]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS
WO2012058531A2 (en) 2010-10-29 2012-05-03 North Carolina State University Modulation of response regulators by imidazole derivatives
TWI408128B (zh) 2010-12-03 2013-09-11 Nat Univ Tsing Hua 間-三聯苯衍生物及其在有機發光二極體之應用
CN103391937A (zh) 2010-12-20 2013-11-13 Irm责任有限公司 用于调控法尼醇x受体的组合物和方法
US20130261108A1 (en) 2010-12-20 2013-10-03 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
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
WO2013037482A1 (en) 2011-09-15 2013-03-21 Phenex Pharmaceuticals Ag Farnesoid x receptor agonists for cancer treatment and prevention
PL2776038T3 (pl) 2011-11-11 2018-06-29 Gilead Apollo, Llc Inhibitory acc i ich zastosowania
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
CA3028207A1 (en) 2012-06-19 2013-12-27 Intercept Pharmaceuticals, Inc. Preparation, uses and solid forms of obeticholic acid
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
EA030942B1 (ru) 2013-05-10 2018-10-31 Джилид Аполло, Ллс Ингибиторы акк и их применение
UA118673C2 (uk) 2013-05-14 2019-02-25 Інтерсепт Фармасутікалз, Інк. Похідні 11-гідроксилу жовчних кислот та їх амінокислотні кон'югати як модулятори фарнезоїдного x-рецептора
CN105593237B (zh) 2013-08-01 2019-06-04 美国卫生和人力服务部 法尼醇x受体的抑制剂和在医学中的用途
BR112016005507B1 (pt) 2013-09-11 2023-02-07 Centre National De La Recherche Scientifique (Cnrs) Uso de um agonista do receptor farnesoide x (fxr)
US20150082981A1 (en) 2013-09-20 2015-03-26 E I Du Pont De Nemours And Company Capture of trifluoromethane using ionic liquids
CN104513213A (zh) 2013-09-28 2015-04-15 山东亨利医药科技有限责任公司 Fxr激动剂
WO2015065983A1 (en) 2013-10-29 2015-05-07 Lumena Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of gastrointestinal infections
TN2016000143A1 (en) 2013-11-05 2017-10-06 Novartis Ag Compositions and methods for modulating farnesoid x receptors.
WO2015116856A2 (en) 2014-01-29 2015-08-06 City Of Hope Farnesoid x receptor antagonists
US10077268B2 (en) 2014-03-13 2018-09-18 Salk Institute For Biological Studies FXR agonists and methods for making and using
CA2942403A1 (en) 2014-03-13 2015-09-17 Salk Institute For Biological Studies Fxr agonists and methods for making and using
EP3116851B1 (en) 2014-03-13 2023-07-26 Salk Institute for Biological Studies Analogs of fexaramine and methods of making and using
JP6673850B2 (ja) 2014-04-14 2020-03-25 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング ヘテロアリール置換されたヘテロシクリルスルホン
WO2015162538A1 (en) 2014-04-21 2015-10-29 Lupin Limited Heterocyclic compounds as calcium sensing receptor modulators for the treatment of hyperparathyroidism, chronic renal failure and chronic kidney disease
WO2015162244A1 (en) 2014-04-25 2015-10-29 Basf Se N-acylamidine compounds
WO2015165960A1 (en) 2014-04-30 2015-11-05 Basf Se N-acylamidine compounds
SI3626725T1 (sl) 2014-05-29 2023-04-28 Bar Pharmaceuticals S.R.L. Derivati holana za uporabo pri zdravljenju in/ali preprečevanju bolezni, posredovanih s FXR in TGR5/GPBAR1
CN104045635A (zh) 2014-06-23 2014-09-17 华东理工大学 3,4,5-三取代异恶唑类化合物及其用途
WO2016054560A1 (en) 2014-10-02 2016-04-07 Flatley Discovery Lab Isoxazole compounds and methods for the treatment of cystic fibrosis
EP3006939A1 (en) 2014-10-06 2016-04-13 Gilead Sciences, Inc. Histidine-rich Glycoprotein as a marker for hepatic Farnesoid X receptor activation
CN106716665B9 (zh) 2014-10-27 2018-12-07 株式会社Lg化学 有机电致发光器件
MX2017005935A (es) 2014-11-06 2018-01-11 Enanta Pharm Inc Análogos de ácido biliar como agonistas fxr/tgr5 y métodos de uso de los mismos.
RU2706007C2 (ru) 2014-11-21 2019-11-13 Акарна Терапьютикс, Лтд. Конденсированные бициклические соединения для лечения заболевания
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
WO2016086134A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
EP3034499A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
EP3034501A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Hydroxy containing FXR (NR1H4) modulating compounds
WO2016097933A1 (en) 2014-12-18 2016-06-23 Novartis Ag Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases
CA2972919A1 (en) 2015-01-09 2016-07-14 Gilead Apollo, Llc Acc inhibitor combination therapy for the treatment of non-alcoholic fatty liver disease
AU2016209321B2 (en) 2015-01-20 2019-05-09 Boehringer Ingelheim Animal Health USA Inc. Anthelmintic compounds, compositions and method of using 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
US10100285B2 (en) 2015-04-03 2018-10-16 Propagenix Inc. Ex vivo proliferation of epithelial cells
CN106146483A (zh) 2015-04-23 2016-11-23 上海迪诺医药科技有限公司 杂环类法尼酯衍生物x受体调节剂
GB201507340D0 (en) 2015-04-29 2015-06-10 Univ St Andrews Light emitting devices and compounds
WO2017011466A1 (en) 2015-07-13 2017-01-19 Zwiebel Laurence J Thermal volatilization of orco agonists
EP3892718A1 (en) 2015-09-11 2021-10-13 Propagenix Inc. Ex vivo proliferation of epithelial cells
MX2018006217A (es) 2015-12-04 2018-08-01 Squibb Bristol Myers Co Agonistas del receptor de apelina y metodos de uso.
WO2017097870A1 (de) 2015-12-11 2017-06-15 Bayer Cropscience Aktiengesellschaft Substituierte malonsäureamide als insektizide
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
EP3190103A1 (en) 2016-01-08 2017-07-12 Rijksuniversiteit Groningen Inhibitors of the pd-1/pd-l1 protein/protein interaction
WO2017117687A1 (en) 2016-01-10 2017-07-13 British Columbia Cancer Agency Branch 18/19f-labelled compounds which target the prostate specific membrane antigen
WO2017122209A2 (en) 2016-01-12 2017-07-20 Yeda Research And Development Co. Ltd. NF-kappaB INHIBITORS
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
CN107021958A (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
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
CN108602811B (zh) 2016-02-01 2021-11-16 轩竹生物科技有限公司 Fxr受体激动剂
TW201741307A (zh) 2016-02-22 2017-12-01 艾洛斯生物製藥公司 Fxr調節劑及其使用方法
CN107224583A (zh) 2016-03-24 2017-10-03 中美华世通生物医药科技(武汉)有限公司 药物组合物及其用途
WO2017189663A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10080742B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10080741B2 (en) 2016-04-26 2018-09-25 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
US10144729B2 (en) 2016-05-18 2018-12-04 Enanta Pharmaceuticals, Inc. Isoxazole analogs 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
US10682344B2 (en) 2016-06-03 2020-06-16 Chemocentryx, Inc. Method of treating liver fibrosis
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
AR108711A1 (es) 2016-06-13 2018-09-19 Gilead Sciences Inc Compuestos moduladores de fxr (nr1h4)
JP6678779B2 (ja) 2016-06-13 2020-04-08 ギリアード サイエンシーズ, インコーポレイテッド Fxr(nr1h4)調節化合物
MA45244A (fr) 2016-06-13 2019-04-17 Cancer Research Tech Ltd Pyridines substituées utilisées en tant qu'inhibiteurs de dnmt1
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
WO2018039384A1 (en) 2016-08-23 2018-03-01 Ardelyx, Inc. Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as fxr activators
CN108430998B (zh) 2016-09-28 2021-07-09 四川科伦博泰生物医药股份有限公司 氮杂双环衍生物及其制备方法和用途
US20200045972A1 (en) 2016-09-29 2020-02-13 Bayer Cropscience Aktiengesellschaft Novel 5-substituted imidazolylmethyl derivatives
KR20190056436A (ko) 2016-10-04 2019-05-24 이난타 파마슈티칼스, 인코포레이티드 Fxr 작용제로서의 이속사졸 유사체 및 그의 사용 방법
ES2924257T3 (es) 2016-10-18 2022-10-05 Madrigal Pharmaceuticals Inc Métodos de tratar trastornos hepáticos o trastornos lipídicos con un agonista de THR-beta
CN107973790A (zh) 2016-10-22 2018-05-01 合帕吉恩治疗公司 杂环fxr调节剂
CN110191724A (zh) 2016-11-10 2019-08-30 盖尔梅德研究与发展有限公司 纤维化的治疗
AU2017356160A1 (en) * 2016-11-11 2019-05-23 Gilead Sciences, Inc. Methods of treating liver disease
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
CN106748922B (zh) 2017-01-12 2019-02-01 中国药科大学 一类新型砜酸衍生物、其制备方法及其作为药物的用途
AU2018243719B2 (en) 2017-03-28 2021-01-21 Gilead Sciences, Inc. Therapeutic combinations for treating liver diseases
JP2020516627A (ja) * 2017-04-12 2020-06-11 ギリアード サイエンシーズ, インコーポレイテッド 肝疾患を処置する方法
WO2018190643A1 (en) 2017-04-12 2018-10-18 Il Dong Pharmaceutical Co., Ltd. An isoxazole derivatives as nuclear receptor agonists and used thereof
CA3233305A1 (en) 2019-02-19 2020-08-27 Gilead Sciences, Inc. Solid forms of fxr agonists
JP2022524398A (ja) 2019-03-11 2022-05-02 ギリアード サイエンシーズ, インコーポレイテッド 化合物の製剤およびそれらの使用

Also Published As

Publication number Publication date
JP2022517108A (ja) 2022-03-04
HRP20240265T1 (hr) 2024-05-10
DOP2021000148A (es) 2021-08-31
CN113302190A (zh) 2021-08-24
EP3911647A1 (en) 2021-11-24
PE20211907A1 (es) 2021-09-28
JP7265635B2 (ja) 2023-04-26
IL284591A (en) 2021-08-31
ZA202104705B (en) 2022-05-25
AR117814A1 (es) 2021-08-25
EP3911647B1 (en) 2023-12-13
EP4360632A2 (en) 2024-05-01
BR112021011762A2 (pt) 2021-11-03
CO2021009240A2 (es) 2021-07-30
LT3911647T (lt) 2024-03-25
AU2020209564B2 (en) 2022-12-01
CR20210385A (es) 2021-09-14
AU2023200994A1 (en) 2023-03-23
JP2023062120A (ja) 2023-05-02
DOP2023000196A (es) 2023-10-31
DK3911647T3 (da) 2024-02-26
FI3911647T3 (fi) 2024-03-01
KR20210114457A (ko) 2021-09-23
TWI733307B (zh) 2021-07-11
MX2021008518A (es) 2021-08-19
AU2020209564A1 (en) 2021-07-15
US20200255418A1 (en) 2020-08-13
SI3911647T1 (sl) 2024-04-30
WO2020150136A1 (en) 2020-07-23
EA202191566A1 (ru) 2021-11-01
US20220204491A1 (en) 2022-06-30
CA3124702A1 (en) 2020-07-23
SG11202107434PA (en) 2021-08-30
US11225473B2 (en) 2022-01-18
TW202043220A (zh) 2020-12-01
PT3911647T (pt) 2024-03-04

Similar Documents

Publication Publication Date Title
CL2021001877A1 (es) Compuestos moduladores de fxr (nr1h4)
ECSP18090693A (es) Compuestos moduladores de fxr (nr1h4)
NZ748641A (en) Fxr (nr1h4) modulating compounds
TR201909093T4 (tr) Hidroksi içeren FXR (NR1H4) modüle edici bileşikleri.
TR201906401T4 (tr) Yeni fxr (nr1h4) modüle edici bileşikler.
MX2019011629A (es) Nuevos compuestos que se unen a fxr (nr1h4) y modulan su actividad.
CU20110052A7 (es) Compuestos orgánicos
UY31863A (es) Combinaciones de drogas que comprenden un inhibidor de dgat y un agonista de ppar
BR112016024936A2 (pt) moduladores de gpr40 à base de pirrolidina para tratamento de doenças como diabetes
ECSP10010032A (es) derivados de azaciclilisoquinolinona e -isoindolinona como antagonistas de la HISTAMINA-3
BR112017008312A2 (pt) novos compostos de piridopirimidinona para modular a atividade catalítica de histona lisina demetilases (kdms)
MX2022000945A (es) Composicion para incrementar la expresion de pgc-1alfa.
CO2021011023A2 (es) Compuesto heterocíclico, composición farmacéutica que lo comprende, método para su preparación, y uso de estos
CL2020002217A1 (es) Uso de alcoxipirazoles como inhibidores de la nitrificación
NZ766972A (en) Compounds having s1p5 receptor agonistic activity
BR112019001153A2 (pt) agonista s1p1 e aplicação do mesmo
BR112018075817A2 (pt) composto de fórmula (i), medicamento e composição farmacêutica
BR112023026538A2 (pt) Pirazóis com pirimidinil substituído como inibidores de cdk2
BR112022001164A2 (pt) Composto, uso de um composto, método para o tratamento ou profilaxia de doenças, composto para uso e composição farmacêutica