DK3911647T3 - Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan - Google Patents

Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan Download PDF

Info

Publication number
DK3911647T3
DK3911647T3 DK20708721.4T DK20708721T DK3911647T3 DK 3911647 T3 DK3911647 T3 DK 3911647T3 DK 20708721 T DK20708721 T DK 20708721T DK 3911647 T3 DK3911647 T3 DK 3911647T3
Authority
DK
Denmark
Prior art keywords
pharmaceutical compositions
fxr agonist
isoxazole compound
isoxazole
compound
Prior art date
Application number
DK20708721.4T
Other languages
English (en)
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
Application granted granted Critical
Publication of DK3911647T3 publication Critical patent/DK3911647T3/da

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)
DK20708721.4T 2019-01-15 2020-01-13 Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan DK3911647T3 (da)

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
DK3911647T3 true DK3911647T3 (da) 2024-02-26

Family

ID=69740522

Family Applications (1)

Application Number Title Priority Date Filing Date
DK20708721.4T DK3911647T3 (da) 2019-01-15 2020-01-13 Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan

Country Status (30)

Country Link
US (2) US11225473B2 (da)
EP (2) EP4360632A3 (da)
JP (2) JP7265635B2 (da)
KR (1) KR20210114457A (da)
CN (1) CN113302190A (da)
AR (1) AR117814A1 (da)
AU (2) AU2020209564B2 (da)
BR (1) BR112021011762A2 (da)
CA (1) CA3124702A1 (da)
CL (1) CL2021001877A1 (da)
CO (1) CO2021009240A2 (da)
CR (1) CR20210385A (da)
DK (1) DK3911647T3 (da)
DO (2) DOP2021000148A (da)
EA (1) EA202191566A1 (da)
ES (1) ES2973500T3 (da)
FI (1) FI3911647T3 (da)
HR (1) HRP20240265T1 (da)
HU (1) HUE065889T2 (da)
IL (1) IL284591A (da)
LT (1) LT3911647T (da)
MX (1) MX2021008518A (da)
PE (1) PE20211907A1 (da)
PL (1) PL3911647T3 (da)
PT (1) PT3911647T (da)
SG (1) SG11202107434PA (da)
SI (1) SI3911647T1 (da)
TW (1) TWI733307B (da)
WO (1) WO2020150136A1 (da)
ZA (1) ZA202104705B (da)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2018015443A (es) 2016-06-13 2019-04-11 Gilead Sciences Inc Compuestos moduladores de fxr (nr1h4).
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
JP6906626B2 (ja) 2017-03-28 2021-07-21 ギリアード サイエンシーズ, インコーポレイテッド 肝疾患を処置するための治療的組み合わせ
WO2020081766A1 (en) * 2018-10-18 2020-04-23 Avolynt Use of sglt2 inhibitors to treat primary sclerosing cholangitis
AU2020225225B2 (en) 2019-02-19 2022-12-22 Gilead Sciences, Inc. Solid forms of FXR agonists
JP2023510274A (ja) 2020-01-15 2023-03-13 アンセルム(アンスティチュート・ナシオナル・ドゥ・ラ・サンテ・エ・ドゥ・ラ・ルシェルシュ・メディカル) D型肝炎ウイルスによる感染を処置するためのfxrアゴニストの使用
US11478533B2 (en) 2020-04-27 2022-10-25 Novo Nordisk A/S Semaglutide for use in medicine
US20220135540A1 (en) * 2020-10-15 2022-05-05 Eli Lilly And Company Polymorphs of an fxr agonist
EP4277630A1 (en) 2021-01-14 2023-11-22 ENYO Pharma Method for treating chronic kidney diseases
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.
CA3213217A1 (en) 2021-04-28 2022-11-03 Raphael Darteil 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
DE3880544D1 (de) 1987-04-21 1993-06-03 Basf Ag P-phenoxy-phenoxymethyl-fuenfring-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
CA2195107A1 (en) 1994-08-02 1996-02-15 Richard Alexander Jelley 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
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
US6639078B1 (en) 1998-12-23 2003-10-28 Smithkline Beecham Corporation Assays for ligands for nuclear receptors
BR0011741A (pt) 1999-06-11 2002-03-19 Allergan Sales Inc Compostos de organossilila tendo atividade de modulação do receptor de hormÈnio nuclear
US7022725B2 (en) 2000-11-17 2006-04-04 Takeda Pharmaceutical Company Limited Isoxazole derivatives
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
US20040105884A1 (en) 2001-04-17 2004-06-03 Ping Gao Pharmaceutical dosage form comprising a sulfite compound
US20040131670A1 (en) 2001-04-17 2004-07-08 Ping Gao Pellicle-resistant gelatin capsule
WO2003000249A1 (fr) 2001-06-26 2003-01-03 Takeda Chemical Industries, Ltd. Regulateur de la fonction du recepteur relatif aux retinoides
EP1423113A4 (en) 2001-08-13 2007-04-18 Phenex Pharmaceuticals Ag NR1H4 NUCLEAR RECEPTOR BINDING COMPOUNDS
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
AU2003225903A1 (en) 2002-03-21 2003-10-08 Curagen Corporation Methods of using farnesoid x receptor (fxr) agonists
US7595311B2 (en) 2002-05-24 2009-09-29 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
US20040132726A1 (en) 2002-08-09 2004-07-08 Astrazeneca Ab And Nps Pharmaceuticals, Inc. New compounds
TWI341314B (en) 2002-08-09 2011-05-01 Astrazeneca Ab New compounds
US7074809B2 (en) 2002-08-09 2006-07-11 Astrazeneca Ab Compounds
EP1407774A1 (en) 2002-09-10 2004-04-14 LION Bioscience AG 2-Amino-4-quinazolinones as LXR nuclear receptor binding compounds
AU2003290796A1 (en) 2002-11-14 2004-06-15 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
US7319109B2 (en) 2002-11-22 2008-01-15 Smith Kline 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
RU2408589C2 (ru) 2004-05-14 2011-01-10 Айрм Ллк Соединения и композиции в качестве модуляторов ppar-рецепторов, активируемых пролифератором пероксисом
MY144903A (en) 2004-06-17 2011-11-30 Novartis Ag Pyrrolopyridine derivatives and their use as crth2 antagonists
MX2007004484A (es) 2004-10-13 2007-06-25 Ptc Therapeutics Inc Compuestos de pirazol o triazol y su uso para la fabricacion de un medicamento para tratar las enfermedades relacionadas con la mutacion somatica.
JP2008137894A (ja) 2005-03-22 2008-06-19 Nippon Kayaku Co Ltd 新規なアセチレン誘導体
TW200716576A (en) 2005-06-07 2007-05-01 Shionogi & Co Heterocyclic derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
AU2006325815B2 (en) 2005-12-15 2012-07-05 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
JP5081161B2 (ja) 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 ファルネソイドx受容体アゴニスト
US7560551B2 (en) 2006-01-23 2009-07-14 Amgen Inc. Aurora kinase modulators and method of use
CA2640476A1 (en) 2006-02-03 2007-08-16 Eli Lilly And Company Compounds and methods for modulating fx-receptors
CA2642220A1 (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
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
CA2651373A1 (en) 2006-05-24 2007-12-06 Eli Lilly And Company Compounds and methods for modulating fxr
EP2029600B1 (de) 2006-05-24 2012-03-14 Boehringer Ingelheim International GmbH Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
MX2008014854A (es) 2006-05-24 2008-12-05 Lilly Co Eli Antagonistas de fxr.
ES2523591T3 (es) 2006-06-27 2014-11-27 Intercept Pharmaceuticals Inc. Derivados de ácidos biliares como ligandos de FXR para la prevención o el tratamiento de enfermedades o estados mediados por FXR
CA2656290A1 (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
JP5153773B2 (ja) 2006-07-07 2013-02-27 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング フェニル置換ヘテロアリール誘導体及び抗癌剤としてのその使用
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
EP2121621B1 (en) 2006-12-08 2014-05-07 Exelixis Patent Company LLC 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
CA2676700C (en) 2007-02-09 2013-12-17 Dow Agrosciences Llc Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines
US7511149B2 (en) 2007-02-09 2009-03-31 Dow Agrosciences Llc Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines
CA2678028C (en) 2007-02-26 2015-02-03 Dow Agrosciences Llc Process for the preparation of certain substituted sulfilimines
CA2689980A1 (en) 2007-06-13 2008-12-24 Glaxosmithkline Llc 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
AU2008270784A1 (en) 2007-07-02 2009-01-08 Glaxosmithkline Llc Farnesoid X receptor agonists
JP2010531850A (ja) 2007-07-02 2010-09-30 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規化合物
TW200920372A (en) 2007-07-13 2009-05-16 Genelabs Tech Inc 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 (es) 2007-08-01 2010-03-01 Lundbeck & Co As H Uso de abridores de canales de potasio kcnq para reducir los sintomas o tratar desordenes o afecciones en las cuales se encuentra anulado el sistema dopaminergico.
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
BRPI0821676A2 (pt) 2007-12-21 2015-06-16 Astrazeneca Ab Composto, composição farmacêutica, e, processo para a preparação dos compostos.
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
US20120015988A1 (en) 2008-05-13 2012-01-19 Boehringer Ingelheim International Gmbh Sulfone Compounds Which Modulate The CB2 Receptor
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
JP2011521916A (ja) 2008-05-19 2011-07-28 バーナム インスティテュート フォー メディカル リサーチ 腸アルカリホスファターゼモジュレーターおよびそれの使用
EP2128158A1 (en) 2008-05-26 2009-12-02 Phenex Pharmaceuticals AG Heterocyclic cyclopropyl-substituted FXR binding compounds
CN104530052A (zh) 2008-06-10 2015-04-22 普莱希科公司 用于激酶调节的5h-吡咯[2,3-b]吡嗪衍生物和其适应症
US8822513B2 (en) 2010-03-01 2014-09-02 Gtx, Inc. Compounds for treatment of cancer
WO2009156336A1 (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
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
WO2010034649A1 (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
ES2443947T3 (es) 2008-09-25 2014-02-21 F. Hoffmann-La Roche Ag Derivados de 3-amino-indazol o de 3-amino-4,5,6,7-tetrahidro-indazol
WO2010036362A1 (en) 2008-09-26 2010-04-01 Wyeth 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors
JP2012506386A (ja) 2008-10-21 2012-03-15 メタボレックス, インコーポレイテッド アリールgpr120受容体アゴニストおよびその使用
WO2010089303A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh CYCLIC INHIBITORS OF 11 β-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
JP2012532175A (ja) 2009-07-06 2012-12-13 ビーエーエスエフ ソシエタス・ヨーロピア 無脊椎動物系害虫防除用ピリダジン化合物
US8883832B2 (en) 2009-07-06 2014-11-11 Aerpio Therapeutics Inc. Compounds, compositions, and methods for preventing metastasis of cancer cells
TWI625121B (zh) 2009-07-13 2018-06-01 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
JP2013500246A (ja) 2009-07-24 2013-01-07 ビーエーエスエフ ソシエタス・ヨーロピア 無脊椎動物系害虫防除用ピリジン誘導体化合物
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
AU2010291834A1 (en) 2009-09-04 2012-03-15 Zalicus Pharmaceuticals Ltd. Substituted heterocyclic derivatives for the treatment of pain and epilepsy
WO2011047129A1 (en) 2009-10-15 2011-04-21 Southern Research Institute Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
WO2011109059A1 (en) 2010-03-01 2011-09-09 Gtx, Inc. Compounds for treatment of cancer
EP2580213A4 (en) 2010-06-09 2013-12-25 Afraxis Holdings 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
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
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
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
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
UA123760C2 (uk) 2011-11-11 2021-06-02 Гіліад Аполло, Ллс Сполука (варіанти) та композиція, що містить сполуку
UY34573A (es) 2012-01-27 2013-06-28 Gilead Sciences Inc Inhibidor de la quinasa que regula la señal de la apoptosis
NZ734451A (en) 2012-06-19 2018-12-21 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
CN105358154A (zh) 2013-05-10 2016-02-24 尼普斯阿波罗有限公司 Acc抑制剂和其用途
SI3360882T1 (sl) 2013-05-14 2021-06-30 Intercept Pharmaceuticals, Inc. 11-hidroksil-6-substituirani derivati žolčnih kislin in aminokislinski konjugati le-teh kot modulatorji receptorja farnezoid X
NZ716568A (en) 2013-08-01 2021-07-30 Us Health Inhibitors of the farnesoid x receptor and uses in medicine
JP6366721B2 (ja) 2013-09-11 2018-08-01 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル B型肝炎ウイルス感染症を処置するための方法及び医薬組成物
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
UY35818A (es) 2013-11-05 2015-05-29 Irm Llc Composiciones y métodos para modular los receptores x farnesoides
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
JP2017511304A (ja) 2014-03-13 2017-04-20 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 フェキサラミン類似体ならびに作製方法および使用方法
EP3116878A4 (en) 2014-03-13 2018-02-14 Salk Institute for Biological Studies Fxr agonists and methods for making and using
PE20161366A1 (es) 2014-04-14 2017-01-15 Gruenenthal Chemie Heterociclil-sulfonas sustituidas con heteroarilo
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
DK3626725T3 (da) 2014-05-29 2023-02-27 Bar Pharmaceuticals S R L Cholan-derivater til anvendelse ved behandlingen og/eller forebyggelsen af fxr- og tgr5/gpbar1-medierede sygdomme
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
TWI577070B (zh) 2014-10-27 2017-04-01 Lg 化學股份有限公司 有機電致發光元件
AU2015343025A1 (en) 2014-11-06 2017-06-08 Enanta Pharmaceuticals, Inc. Bile acid analogs an FXR/TGR5 agonists and methods of use thereof
AU2015349687B2 (en) 2014-11-21 2020-07-09 Akarna Therapeutics, Ltd. Fused bicyclic compounds for the treatment of disease
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
WO2016086134A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
JP2017535570A (ja) 2014-11-26 2017-11-30 エナンタ ファーマシューティカルズ インコーポレイテッド Fxr/tgr5アゴニストとしての胆汁酸類似体およびその使用方法
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
AU2015365481B2 (en) 2014-12-18 2018-08-09 Novartis Ag Azabicyclooctane derivatives as FXR agonists for use in the treatment of liver and gastrointestinal diseases
EA201892625A1 (ru) 2015-01-09 2019-07-31 Джилид Аполло, Ллс КОМБИНИРОВАННАЯ ТЕРАПИЯ С ПРИМЕНЕНИЕМ ИНГИБИТОРА АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ (ACC) ДЛЯ ЛЕЧЕНИЯ НЕАЛКОГОЛЬНОЙ ЖИРОВОЙ БОЛЕЗНИ ПЕЧЕНИ
US10597364B2 (en) 2015-01-20 2020-03-24 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
CN107920523A (zh) 2015-07-13 2018-04-17 范德比尔特大学 Orco激动剂的热挥发
DK3347450T3 (da) 2015-09-11 2021-05-31 Propagenix Inc Ex vivo-proliferation af epithelceller
AR106948A1 (es) 2015-12-04 2018-03-07 Bristol Myers Squibb Co Agonistas del receptor de apelina y método de uso
TW201734002A (zh) 2015-12-11 2017-10-01 拜耳作物科學股份有限公司 作為殺蟲劑之經取代的丙二醯胺類
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
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 (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
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
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
WO2017133521A1 (zh) 2016-02-01 2017-08-10 山东轩竹医药科技有限公司 Fxr受体激动剂
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
WO2017189652A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10080743B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017189651A1 (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
CN115154467A (zh) 2016-06-03 2022-10-11 坎莫森特里克斯公司 治疗肝纤维化的方法
MX2018015483A (es) 2016-06-13 2019-03-18 Glaxosmithkline Ip Dev Ltd Piridinas sustituidas como inhibidores de adn metiltransferasa-1 (dnmt1).
MX2018015443A (es) * 2016-06-13 2019-04-11 Gilead Sciences Inc Compuestos moduladores de fxr (nr1h4).
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)
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
MA46052A (fr) 2016-08-23 2021-03-17 Ardelyx Inc Modulateurs du récepteur hormonal pour le traitement d'états et de troubles métaboliques
US11091482B2 (en) 2016-08-23 2021-08-17 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
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
US10450306B2 (en) 2016-10-04 2019-10-22 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
KR20190109387A (ko) * 2016-10-18 2019-09-25 마드리갈 파마슈티칼스, 인크. Thr-베타 아고니스트로 간 질환 또는 지질 질환을 치료하는 방법
CN107973790A (zh) 2016-10-22 2018-05-01 合帕吉恩治疗公司 杂环fxr调节剂
KR20190083659A (ko) 2016-11-10 2019-07-12 갈메드 리서치 앤드 디벨롭먼트 리미티드 섬유증에 대한 치료
CA3042398A1 (en) * 2016-11-11 2018-05-17 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
JP6906626B2 (ja) 2017-03-28 2021-07-21 ギリアード サイエンシーズ, インコーポレイテッド 肝疾患を処置するための治療的組み合わせ
TW201902478A (zh) 2017-04-12 2019-01-16 美商基利科學股份有限公司 治療肝臟疾病之方法
WO2018190643A1 (en) 2017-04-12 2018-10-18 Il Dong Pharmaceutical Co., Ltd. An isoxazole derivatives as nuclear receptor agonists and used thereof
AU2020225225B2 (en) 2019-02-19 2022-12-22 Gilead Sciences, Inc. Solid forms of FXR agonists
WO2020185686A1 (en) 2019-03-11 2020-09-17 Gilead Sciences, Inc. Formulations of a compound and uses thereof

Also Published As

Publication number Publication date
AU2023200994A1 (en) 2023-03-23
HUE065889T2 (hu) 2024-06-28
US11225473B2 (en) 2022-01-18
SG11202107434PA (en) 2021-08-30
TW202043220A (zh) 2020-12-01
EP4360632A2 (en) 2024-05-01
KR20210114457A (ko) 2021-09-23
JP2023062120A (ja) 2023-05-02
CO2021009240A2 (es) 2021-07-30
HRP20240265T1 (hr) 2024-05-10
DOP2021000148A (es) 2021-08-31
US20220204491A1 (en) 2022-06-30
US20200255418A1 (en) 2020-08-13
CL2021001877A1 (es) 2022-01-07
WO2020150136A1 (en) 2020-07-23
EA202191566A1 (ru) 2021-11-01
CN113302190A (zh) 2021-08-24
AU2020209564A1 (en) 2021-07-15
BR112021011762A2 (pt) 2021-11-03
CR20210385A (es) 2021-09-14
IL284591A (en) 2021-08-31
FI3911647T3 (fi) 2024-03-01
EP3911647A1 (en) 2021-11-24
JP2022517108A (ja) 2022-03-04
PT3911647T (pt) 2024-03-04
AU2020209564B2 (en) 2022-12-01
ZA202104705B (en) 2022-05-25
EP4360632A3 (en) 2024-06-19
PE20211907A1 (es) 2021-09-28
SI3911647T1 (sl) 2024-04-30
DOP2023000196A (es) 2023-10-31
MX2021008518A (es) 2021-08-19
JP7265635B2 (ja) 2023-04-26
ES2973500T3 (es) 2024-06-20
CA3124702A1 (en) 2020-07-23
EP3911647B1 (en) 2023-12-13
PL3911647T3 (pl) 2024-05-20
LT3911647T (lt) 2024-03-25
AR117814A1 (es) 2021-08-25
TWI733307B (zh) 2021-07-11

Similar Documents

Publication Publication Date Title
DK3911647T3 (da) Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan
DK3442973T3 (da) Hidtil ukendte forbindelser som autotaxinhæmmere og farmaceutiske sammensætninger omfattende samme
DK3328843T3 (da) 1,3,4-oxadiazolsulfonamidderivat-forbindelser som histon- deacetylase-6-inhibitor, og den farmaceutske sammensætning
DK3331864T3 (da) 1,3,4-Oxadiazolderivat-forbindelser som histon-deacetylase-6-hæmmer, og den farmaceutiske sammensætning omfattende disse
DK3775091T3 (da) Stabiliserede fluorolefinsammensætninger og fremgangsmåder til fremstilling, oplagring og anvendelse deraf
DK3330259T3 (da) 1,3,4-oxadiazolamidderivativ-forbindelse som histondeacetylase-6-inhibitor og farmaceutisk sammensætning indeholdende denne
DK3362445T3 (da) Oxadiazolaminderivatforbindelser som histondeacetylase 6-inhibitor, og den farmaceutiske sammensætning dermed
DK3328844T3 (da) 1,3,4-oxadiazolsulfamidderivater som histondeacetylase-6-inhibitor og farmaceutisk sammensætning omfattende samme
DK3768674T3 (da) Aminopyrimidinderivater som ctps1-hæmmere
DK3986890T3 (da) Benzisoxazol-sulfonamid-derivater
DK3810201T5 (da) GIP/GLP1-agonist-sammensætninger
DK3956324T3 (da) 1,3,4-oxadiazol-derivater som histondeacetylase-inhibitorer
DK3634468T3 (da) Fast sammensætning til oral indgivelse
DK3762368T3 (da) Aminopyrazindiolforbindelser som pi3k-y-inhibitorer
DK3681885T3 (da) Tetrahydro-imidazo-quinolinsammensætninger som cbp/p300-inhibitorer
DK3797107T3 (da) Heterokondenserede pyridonforbindelser og anvendelse deraf som idh- hæmmere
DK3612520T3 (da) Isoxazolderivater som kernereceptoragonister og anvendelser deraf
CY1122287T1 (el) Ενωσεις χρησιμες για την αναστολη toy ror-γαμμα-τ
DK3707128T3 (da) Injicerbare, farmaceutiske isoxazolinsammensætninger og anvendelse deraf mod parasitangreb
DK3844161T3 (da) Heteroaromatiske forbindelser som vanininhibitorer.
DK3297992T3 (da) Heterocykliske alkylderivatforbindelser som selektive histondeacetylase-inhibitorer og farmaceutiske sammensætninger omfattende samme
UY37560A (es) Combinación de un inhibidor de mcl-1 y un compuesto taxano, usos y composiciones farmacéuticas de ésta
DK3568396T3 (da) Hidtil ukendte amino-imidazopyridinderivater som janus kinase-inhibitorer og farmaceutisk anvendelse deraf
DK3837256T3 (da) Ureaforbindelser og sammensætninger som smarca2/brm-atpase-hæmmere
DK3455216T3 (da) Pyridinylderivater, farmaceutiske sammensætninger og anvendelser deraf som aoc3-inhibitorer