SG11202107434PA - Fxr (nr1h4) modulating compounds - Google Patents

Fxr (nr1h4) modulating compounds

Info

Publication number
SG11202107434PA
SG11202107434PA SG11202107434PA SG11202107434PA SG11202107434PA SG 11202107434P A SG11202107434P A SG 11202107434PA SG 11202107434P A SG11202107434P A SG 11202107434PA SG 11202107434P A SG11202107434P A SG 11202107434PA SG 11202107434P A SG11202107434P A SG 11202107434PA
Authority
SG
Singapore
Prior art keywords
nr1h4
fxr
modulating compounds
modulating
compounds
Prior art date
Application number
SG11202107434PA
Inventor
Peter A Blomgren
Kevin S Currie
Morin Mae Frick
Elizabeth M Horstman
Joshua A Kaplan
Jeffrey E Kropf
William J Watkins
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 SG11202107434PA publication Critical patent/SG11202107434PA/en

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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
SG11202107434PA 2019-01-15 2020-01-13 Fxr (nr1h4) modulating compounds SG11202107434PA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962792714P 2019-01-15 2019-01-15
PCT/US2020/013319 WO2020150136A1 (en) 2019-01-15 2020-01-13 Fxr (nr1h4) modulating compounds

Publications (1)

Publication Number Publication Date
SG11202107434PA true SG11202107434PA (en) 2021-08-30

Family

ID=69740522

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202107434PA SG11202107434PA (en) 2019-01-15 2020-01-13 Fxr (nr1h4) modulating compounds

Country Status (30)

Country Link
US (2) US11225473B2 (en)
EP (2) EP4360632A3 (en)
JP (2) JP7265635B2 (en)
KR (1) KR102692309B1 (en)
CN (1) CN113302190A (en)
AR (1) AR117814A1 (en)
AU (2) AU2020209564B2 (en)
BR (1) BR112021011762A2 (en)
CA (1) CA3124702A1 (en)
CL (1) CL2021001877A1 (en)
CO (1) CO2021009240A2 (en)
CR (1) CR20210385A (en)
DK (1) DK3911647T3 (en)
DO (2) DOP2021000148A (en)
EA (1) EA202191566A1 (en)
ES (1) ES2973500T3 (en)
FI (1) FI3911647T3 (en)
HR (1) HRP20240265T1 (en)
HU (1) HUE065889T2 (en)
IL (1) IL284591A (en)
LT (1) LT3911647T (en)
MX (1) MX2021008518A (en)
PE (1) PE20211907A1 (en)
PL (1) PL3911647T3 (en)
PT (1) PT3911647T (en)
SG (1) SG11202107434PA (en)
SI (1) SI3911647T1 (en)
TW (1) TWI733307B (en)
WO (1) WO2020150136A1 (en)
ZA (1) ZA202104705B (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3730487T3 (en) 2016-06-13 2022-08-16 Gilead Sciences, Inc. Azetidine derivatives as fxr (nr1h4) modulators
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
CN110461328A (en) 2017-03-28 2019-11-15 吉利德科学公司 The therapeutic combination for treating liver disease
CN113226295A (en) * 2018-10-18 2021-08-06 阿沃林特有限公司 Use of SGLT2 inhibitor in treatment of primary sclerosing cholangitis
CN118388474A (en) 2019-02-19 2024-07-26 吉利德科学公司 Solid forms of FXR agonists
EP4090327A1 (en) 2020-01-15 2022-11-23 Institut National de la Santé et de la Recherche Médicale (INSERM) 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
AU2021359895A1 (en) * 2020-10-15 2023-06-15 Eli Lilly And Company Polymorphs of an fxr agonist
JP2024503861A (en) 2021-01-14 2024-01-29 ウエヌイグレックオ・ファーマ How to treat chronic kidney disease
CA3204800A1 (en) 2021-01-14 2022-07-21 Raphael Darteil Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
WO2022229302A1 (en) 2021-04-28 2022-11-03 Enyo Pharma Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
TW202311256A (en) 2021-06-18 2023-03-16 美商基利科學股份有限公司 Il-31 modulators for treating fxr-induced pruritis

Family Cites Families (200)

* 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
DE3880544D1 (en) 1987-04-21 1993-06-03 Basf Ag P-PHENOXY-PHENOXYMETHYL-FUENFRING-HETEROAROMAT.
JP3121061B2 (en) 1991-10-04 2000-12-25 塩野義製薬株式会社 Method for producing intermediate for producing alkoxyiminoacetamides and intermediate used therein
DE4137940A1 (en) 1991-11-18 1993-05-19 Basf Ag 3-ISOXAZOLYLPHENYL COMPOUNDS, THEIR PRODUCTION AND THEIR USE
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
US5854268A (en) 1994-08-02 1998-12-29 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 (en) 1995-10-02 1997-04-03 Basf Ag Intermediates and processes for the production of substituted salicylic acid derivatives as crop protection agents
EP0880363B1 (en) 1996-02-13 2002-09-11 G.D. SEARLE & CO. Combinations, having immunosuppressive effects, containing a cyclooxygenase-2 inhibitor and a leukotriene a 4 hydrolase inhibitor
EP1140079B1 (en) 1998-12-23 2009-06-03 Glaxo Group Limited Assays for ligands for nuclear receptors
CN1368975A (en) 1999-06-11 2002-09-11 阿勒根销售公司 Organosilyl compounds having nuclear hormone receptor modulating activity
WO2002040458A1 (en) 2000-11-17 2002-05-23 Takeda Chemical Industries, Ltd. 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
US20040105885A1 (en) 2001-04-17 2004-06-03 Ping Gao Gelatin capsule exhibiting reduced cross-linking
US20040105883A1 (en) 2001-04-17 2004-06-03 Ping Gao Pharmaceutical dosage form capable of maintaining stable dissolution profile upon storage
US7223791B2 (en) 2001-06-26 2007-05-29 Takeda Pharmaceutical Company Limited Function regulator for retinoid relative receptor
ATE381542T1 (en) 2001-08-13 2008-01-15 Phenex Pharmaceuticals Ag NR1H4 CORE RECEPTOR BINDING COMPOUNDS
WO2003015777A1 (en) 2001-08-13 2003-02-27 Lion Bioscience Ag Nr1h4 nuclear receptor binding compounds
US20070010562A1 (en) 2001-08-13 2007-01-11 Ulrike Bauer Nr1h4 nuclear receptor binding compounds
US20050107475A1 (en) 2002-03-21 2005-05-19 Jones Stacey A. Methods of using farnesoid x receptor (frx) agonists
US7595311B2 (en) 2002-05-24 2009-09-29 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
JP2006502134A (en) 2002-08-09 2006-01-19 アストラゼネカ アクチボラグ Compounds having activity at metabotropic glutamate receptors
JP2006506340A (en) 2002-08-09 2006-02-23 アストラゼネカ アクチボラグ Oxadiazole as a modulator of metabotropic glutamate receptor 5
CN1894241A (en) 2002-08-09 2007-01-10 阿斯利康(瑞典)有限公司 '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
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
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
CA2583177A1 (en) 2004-10-13 2006-04-27 Ptc Therapeutics, Inc. Compounds for nonsense suppression, and methods for their use
JP2008137894A (en) 2005-03-22 2008-06-19 Nippon Kayaku Co Ltd New acetylene derivative
US8952176B2 (en) 2005-06-07 2015-02-10 Shionogi & Co., Ltd. Heterocyclic compound having type I 11 β hydroxysteroid dehydrogenase inhibitory activity
EP1963331A1 (en) 2005-12-15 2008-09-03 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
JP5081161B2 (en) 2005-12-19 2012-11-21 スミスクライン ビーチャム コーポレーション Farnesoid X receptor agonist
US7560551B2 (en) 2006-01-23 2009-07-14 Amgen Inc. Aurora kinase modulators and method of use
JP5301286B2 (en) 2006-02-03 2013-09-25 イーライ リリー アンド カンパニー Compounds and methods for modulating FX receptors
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
US20070276050A1 (en) 2006-02-27 2007-11-29 Gilead Sciences, Inc. Methods for identifying ASK1 inhibitors useful for preventing and/or treating cardiovascular diseases
JP2009531364A (en) 2006-03-28 2009-09-03 ノバルティス アクチエンゲゼルシャフト Amide derivatives and their use for the treatment of G protein related diseases
US20090286806A1 (en) 2006-04-17 2009-11-19 Hassan Pajouhesh Isoxazole derivatives as calcium channel blockers
DK2029547T3 (en) 2006-05-24 2010-07-26 Lilly Co Eli FXR agonists
BRPI0711875A2 (en) 2006-05-24 2012-01-10 Lilly Co Eli compounds and methods for modulating fxr
EP2029600B1 (en) 2006-05-24 2012-03-14 Boehringer Ingelheim International GmbH Substituted pteridines substituted with a four-membered heterocycle
WO2008002573A2 (en) 2006-06-27 2008-01-03 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated deseases or conditions
WO2008005538A2 (en) 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
WO2008013660A2 (en) 2006-07-07 2008-01-31 Biostratum, Inc. Inhibitors of advanced glycation end products
CN101501023A (en) 2006-07-07 2009-08-05 贝林格尔.英格海姆国际有限公司 Phenyl substituted heteroaryl-derivatives and use thereof as anti-tumor agents
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
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 (en) 2006-10-24 2008-05-16 Smithkline Beechman Corp COMPOUNDS DERIVED FROM ISOXAZOL REPLACED, FARNESOID X RECEIVER AGONISTS; PREPARATION PROCEDURE; PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS IT; AND USE OF THE COMPOUND IN THE TREATMENT OF OBESITY, DIABETES MELLITUS, FIBROSIS IN ORGANS,
US8501933B2 (en) 2006-11-09 2013-08-06 Roche Palo Alto Llc Thiazole and oxazole-substituted arylamides as P2X3 and P2X2/3 antagonists
CN101679297B (en) 2006-12-08 2012-01-11 埃克塞利希斯股份有限公司 LXR and FXR modulators
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
US7511149B2 (en) 2007-02-09 2009-03-31 Dow Agrosciences Llc Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines
MX2009008421A (en) 2007-02-09 2009-11-02 Dow Agrosciences Llc Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines.
BRPI0807702B8 (en) 2007-02-26 2022-06-28 Dow Agrosciences Llc PROCESS FOR THE PREPARATION OF CERTAIN SUBSTITUTED SULPHILIMINES
US20100249179A1 (en) 2007-06-13 2010-09-30 Smithkline Beecham Corporation Farnesoid X Receptor Agonists
JP2008308448A (en) 2007-06-15 2008-12-25 Sankyo Agro Kk (3-sulfur atom-substituted phenyl)heteroaryl derivative
WO2008155054A1 (en) 2007-06-20 2008-12-24 F. Hoffmann-La Roche Ag Farnesoid-x-receptor mutants, and crystallisation thereof
MX2009013946A (en) 2007-07-02 2010-03-10 Glaxosmithkline Llc Farnesoid x receptor agonists.
US20100240657A1 (en) 2007-07-02 2010-09-23 Boehringer Ingelheim International Gmbh Chemical compounds
KR20100056462A (en) 2007-07-13 2010-05-27 글락소스미스클라인 엘엘씨 Anti-viral compounds, compositions, and methods of use
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
MX2010001171A (en) 2007-08-01 2010-03-01 Lundbeck & Co As H Use of kncq 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
PE20091157A1 (en) 2007-12-21 2009-09-03 Astrazeneca Ab BICYCLE DERIVATIVES TO USE IN THE TREATMENT OF CONDITIONS ASSOCIATED WITH THE ANDROGEN RECEPTOR - 155
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
EP2418207A1 (en) 2008-05-13 2012-02-15 Boehringer Ingelheim International GmbH Sulfone compounds which modulate the CB2 receptor
WO2009143150A2 (en) 2008-05-19 2009-11-26 Burnham Institute For Medical Research Intestinal alkaline phosphatase modulators and uses thereof
WO2009143018A2 (en) 2008-05-19 2009-11-26 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
CA2727078A1 (en) 2008-06-23 2009-12-30 Basf Se Sulfoximinamide compounds for combating animal pests
US20100029655A1 (en) 2008-07-11 2010-02-04 Martin Robert Leivers Processes For The Preparation Of Anti-Viral Compounds And Compositions Containing Them
US8044214B2 (en) 2008-08-25 2011-10-25 Angus Chemical Company Process for preparing isoxazole compounds
WO2010033906A2 (en) 2008-09-19 2010-03-25 President And Fellows Of Harvard College Efficient induction of pluripotent stem cells using small molecule compounds
KR101444988B1 (en) 2008-09-25 2014-09-26 에프. 호프만-라 로슈 아게 3-amino-indazole or 3-amino-4,5,6,7-tetrahydro-indazole derivatives
JP5425911B2 (en) 2008-09-25 2014-02-26 エフ.ホフマン−ラ ロシュ アーゲー 2,3-substituted indazoles or 4,5,6,7-tetrahydro-indazoles as FXR modulators for dyslipidemia and related diseases
EP2334681A1 (en) 2008-09-26 2011-06-22 Wyeth LLC 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors
NZ592603A (en) 2008-10-21 2013-02-22 Metabolex Inc Aryl gpr120 receptor agonists and uses thereof
WO2010089303A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh CYCLIC INHIBITORS OF 11 β-HYDROXYSTEROID DEHYDROGENASE 1
KR20100092909A (en) 2009-02-13 2010-08-23 주식회사 엘지생명과학 Novel compounds effective as xanthine oxidase inhibitors, method for preparing the same, and pharmaceutical composition containing the same
FR2943059A1 (en) 2009-03-16 2010-09-17 Sanofi Aventis N-6-AZA-BICYCLO® 3.2.1.0-OCT-5-YL) -ARYL-METHYL-HETEROBENZAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
US8883832B2 (en) 2009-07-06 2014-11-11 Aerpio Therapeutics Inc. Compounds, compositions, and methods for preventing metastasis of cancer cells
US8710056B2 (en) 2009-07-06 2014-04-29 Basf Se Pyridazine compounds for controlling invertebrate pests
TWI598347B (en) 2009-07-13 2017-09-11 基利科學股份有限公司 Apoptosis signal-regulating kinase inhibitors
CN102469785A (en) 2009-07-24 2012-05-23 巴斯夫欧洲公司 Pyridine derivatives compounds for controlling invertebrate pests
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
CA2771592A1 (en) 2009-09-04 2011-03-10 Zalicus Pharmaceuticals Ltd. Substituted heterocyclic derivatives for the treatment of pain and epilepsy
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
RU2581367C2 (en) 2010-03-01 2016-04-20 Джи Ти Икс, ИНК. Compounds for treating cancer
US20130231348A1 (en) 2010-06-09 2013-09-05 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 (en) 2010-12-03 2013-09-11 Nat Univ Tsing Hua M-terphenyl compound derivatives and application for organic light emitting diode
EP2655369A1 (en) 2010-12-20 2013-10-30 Irm Llc Compositions and methods for modulating farnesoid x receptors
JP2014500318A (en) 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 Compositions and methods for modulating farnesoid X receptor
CU24152B1 (en) 2010-12-20 2016-02-29 Irm Llc 1,2 OXAZOL-8-AZABICICLO [3,2,1] OCTANO 8 IL AS FXR MODULATORS
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
CA2855372C (en) 2011-11-11 2022-03-22 Nimbus Apollo, Inc. 2,4-dioxo-thieno[2,3-d]pyrimidinyl derivatives and pharmaceutical compositions thereof used as acc inhibitors
UY34573A (en) 2012-01-27 2013-06-28 Gilead Sciences Inc QUINASE INHIBITOR REGULATING THE APOPTOSIS SIGNAL
AU2013277429B2 (en) 2012-06-19 2016-01-14 Intercept Pharmaceuticals, Inc. Preparation, uses and solid forms of obeticholic acid
TWI621618B (en) 2013-03-13 2018-04-21 比利時商健生藥品公司 Substituted 2-azabicycles and their use as orexin receptor modulators
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
BR112015028152A2 (en) 2013-05-10 2017-07-25 Nimbus Apollo Inc acc inhibitors and uses thereof
BR112015028399B1 (en) 2013-05-14 2021-11-16 Intercept Pharmaceuticals, Inc 11-HYDROXYL DERIVATIVES OF BILIARY ACIDS AND AMINO ACID CONJUGATES THEREOF AS FARNESOID X RECEPTOR MODULATORS, PHARMACEUTICAL COMPOSITION AND USE OF REFERRED TO DERIVATIVES
AU2014296023B2 (en) 2013-08-01 2020-02-06 The Penn State Research Foundation Inhibitors of the farnesoid X receptor and uses in medicine
DK3043865T3 (en) 2013-09-11 2021-02-01 Univ Claude Bernard Lyon PROCEDURES AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF HEPATITIS B VIRUS INFECTION
US20150082981A1 (en) 2013-09-20 2015-03-26 E I Du Pont De Nemours And Company Capture of trifluoromethane using ionic liquids
CN104513213A (en) 2013-09-28 2015-04-15 山东亨利医药科技有限责任公司 Fxr agonist
WO2015065983A1 (en) 2013-10-29 2015-05-07 Lumena Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of gastrointestinal infections
RS57179B1 (en) 2013-11-05 2018-07-31 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
JP2017510572A (en) 2014-03-13 2017-04-13 ソーク インスティチュート フォー バイオロジカル スタディーズ FXR agonists and methods for making and using
AU2015229055B2 (en) 2014-03-13 2019-09-12 Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
US10077268B2 (en) 2014-03-13 2018-09-18 Salk Institute For Biological Studies FXR agonists and methods for making and using
TW201620899A (en) 2014-04-14 2016-06-16 歌林達有限公司 Heteroaryl substituted heterocyclyl sulfones
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 (en) 2014-05-29 2023-04-28 Bar Pharmaceuticals S.R.L. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
CN104045635A (en) 2014-06-23 2014-09-17 华东理工大学 3,4,5-tri-substituted isoxazole compounds and applications thereof
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
JP6457069B2 (en) 2014-10-27 2019-01-23 エルジー・ケム・リミテッド Organic electroluminescence device
MX2017005935A (en) 2014-11-06 2018-01-11 Enanta Pharm Inc Bile acid analogs an fxr/tgr5 agonists and methods of use thereof.
WO2016081918A1 (en) 2014-11-21 2016-05-26 Akarna Therapeutics, Ltd. Fused bicyclic compounds for the treatment of disease
US11578097B2 (en) 2014-11-26 2023-02-14 Enanta Pharmaceuticals, Inc. Tetrazole derivatives of bile acids 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
AU2015353473A1 (en) 2014-11-26 2017-06-08 Enanta Pharmaceuticals, Inc. Bile acid analogs 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
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
RU2017125365A (en) 2014-12-18 2019-01-21 Новартис Аг Derivatives of azabicyclohexane as FXR agonists for use in the treatment of liver diseases and gastrointestinal diseases
US20180021341A1 (en) 2015-01-09 2018-01-25 Gilead Apollo, Llc Acc inhibitor combination therapy for the treatment of non-alcoholic fatty liver disease
CN107257793A (en) 2015-01-20 2017-10-17 梅里亚股份有限公司 Anti- worm compound, composition and its application method
TWI698430B (en) 2015-02-13 2020-07-11 南北兄弟藥業投資有限公司 Tricyclic compounds and uses thereof in medicine
US10100285B2 (en) 2015-04-03 2018-10-16 Propagenix Inc. Ex vivo proliferation of epithelial cells
CN106146483A (en) 2015-04-23 2016-11-23 上海迪诺医药科技有限公司 Heterocyclic method Buddhist nun's ester derivant X receptor modulators
GB201507340D0 (en) 2015-04-29 2015-06-10 Univ St Andrews Light emitting devices and compounds
US20180192651A1 (en) 2015-07-13 2018-07-12 Vanderbilt University Thermal volatilization of orco agonists
US10066201B2 (en) 2015-09-11 2018-09-04 Propagenix Inc. Ex vivo proliferation of epithelial cells
ES2858312T3 (en) 2015-12-04 2021-09-30 Bristol Myers Squibb Co Apelin receptor agonists and methods of use
TW201734002A (en) 2015-12-11 2017-10-01 拜耳作物科學股份有限公司 Substituted malonamides as insecticides
CN106946867B (en) 2016-01-06 2019-11-12 广州市恒诺康医药科技有限公司 FXR receptor modulators and its preparation method and application
EP3190103A1 (en) 2016-01-08 2017-07-12 Rijksuniversiteit Groningen Inhibitors of the pd-1/pd-l1 protein/protein interaction
US10882871B2 (en) 2016-01-10 2021-01-05 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 (en) 2016-01-26 2017-08-03 江苏豪森药业集团有限公司 Fxr agonist and preparation method and use thereof
CN107021957A (en) 2016-02-01 2017-08-08 山东轩竹医药科技有限公司 FXR receptor stimulating agents
CN107021958A (en) 2016-02-01 2017-08-08 山东轩竹医药科技有限公司 FXR receptor stimulating agents
WO2017133521A1 (en) 2016-02-01 2017-08-10 山东轩竹医药科技有限公司 Fxr receptor agonist
TW201741307A (en) 2016-02-22 2017-12-01 艾洛斯生物製藥公司 FXR modulators and methods of their use
CN107224583A (en) 2016-03-24 2017-10-03 中美华世通生物医药科技(武汉)有限公司 Medical composition and its use
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
US10080741B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
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
US10138228B2 (en) 2016-05-18 2018-11-27 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use therof
WO2017203367A2 (en) 2016-05-22 2017-11-30 Volant Holdings Gmbh Diagnostics and methods for treatment of non-alcoholic hepatic steatosis and hepatic steatohepatitis, and prevention of complications thereof
RU2740902C2 (en) 2016-06-03 2021-01-21 Хемоцентрикс, Инк. Method of treating hepatic fibroses
PL3730487T3 (en) * 2016-06-13 2022-08-16 Gilead Sciences, Inc. Azetidine derivatives as fxr (nr1h4) modulators
SG11201809559UA (en) 2016-06-13 2018-12-28 Glaxosmithkline Ip Dev Ltd Substituted pyridines as inhibitors of dnmt1
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
AR108711A1 (en) 2016-06-13 2018-09-19 Gilead Sciences Inc FXR MODULATING COMPOUNDS (NR1H4)
TW201808283A (en) 2016-08-05 2018-03-16 廣東東陽光藥業有限公司 Nitrogen-containing tricyclic compounds and uses thereof in medicine
CN116854681A (en) 2016-08-23 2023-10-10 阿德利克斯股份有限公司 Hormone receptor modulators for the treatment of metabolic conditions and disorders
US11091482B2 (en) 2016-08-23 2021-08-17 Ardelyx, Inc. Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as FXR activators
CN108430998B (en) 2016-09-28 2021-07-09 四川科伦博泰生物医药股份有限公司 Azabicyclo derivatives, preparation method and application thereof
EP3519408A1 (en) 2016-09-29 2019-08-07 Bayer CropScience Aktiengesellschaft 1 -[2-(1 -chlorocyclopropyl)-2-hydroxy-3-(3-phenyl-1,2-oxazol-5-yl)propyl]-1h-imidazole-5-carbonitrile derivatives and related compounds as fungicides for crop protection
RU2019113066A (en) 2016-10-04 2020-11-09 Энанта Фармасьютикалс, Инк. ISOXAZOLE ANALOGUES AS FXR AGONISTS AND METHODS OF THEIR APPLICATION
WO2018075650A1 (en) * 2016-10-18 2018-04-26 Madrigal Pharmaceuticals, Inc. Methods of treating liver disorders or lipid disorders with a thr-beta agonist
CN107973790A (en) 2016-10-22 2018-05-01 合帕吉恩治疗公司 Heterocyclic FXR conditioning agent
WO2018087599A1 (en) 2016-11-10 2018-05-17 Galmed Research And Development Ltd. Treatment for fibrosis
CA3042398A1 (en) * 2016-11-11 2018-05-17 Gilead Sciences, Inc. Methods of treating liver disease
CN106588804B (en) 2016-12-09 2018-11-09 都创(上海)医药科技有限公司 A kind of preparation method of compound as Farnesoid X receptor (FXR)
CN106632294A (en) 2016-12-15 2017-05-10 宁波百纳西药业有限公司 Spiro compound and medicinal use thereof
CN106748922B (en) 2017-01-12 2019-02-01 中国药科大学 A kind of novel sulfone acid derivative, preparation method and its purposes as drug
CN110461328A (en) 2017-03-28 2019-11-15 吉利德科学公司 The therapeutic combination for treating liver disease
KR20190132515A (en) 2017-04-12 2019-11-27 길리애드 사이언시즈, 인코포레이티드 How to treat liver disease
WO2018190643A1 (en) 2017-04-12 2018-10-18 Il Dong Pharmaceutical Co., Ltd. An isoxazole derivatives as nuclear receptor agonists and used thereof
CN118388474A (en) 2019-02-19 2024-07-26 吉利德科学公司 Solid forms of FXR agonists
CN113573700A (en) 2019-03-11 2021-10-29 吉利德科学公司 Formulations of compounds and uses thereof

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