MX2021008518A - Compuestos que modulan fxr(nr1h4). - Google Patents

Compuestos que modulan fxr(nr1h4).

Info

Publication number
MX2021008518A
MX2021008518A MX2021008518A MX2021008518A MX2021008518A MX 2021008518 A MX2021008518 A MX 2021008518A MX 2021008518 A MX2021008518 A MX 2021008518A MX 2021008518 A MX2021008518 A MX 2021008518A MX 2021008518 A MX2021008518 A MX 2021008518A
Authority
MX
Mexico
Prior art keywords
fxr
nr1h4
compound
modulating compounds
compounds
Prior art date
Application number
MX2021008518A
Other languages
English (en)
Inventor
Jeffrey E Kropf
Peter A Blomgren
William J Watkins
Kevin S Currie
Joshua A Kaplan
Morin Mae Frick
Elizabeth M Horstman
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 MX2021008518A publication Critical patent/MX2021008518A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline 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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

La presente divulgación se refiere de manera general a compuestos de fórmula (I) que se unen a FXR y actúan como agonistas de FXR. La divulgación se refiere además al uso de los compuestos para la preparación de un medicamento para el tratamiento de enfermedades y/o condiciones a través de la unión de dicho receptor nuclear por dichos compuestos y a un proceso para la síntesis de dichos compuestos.
MX2021008518A 2019-01-15 2020-01-13 Compuestos que modulan fxr(nr1h4). MX2021008518A (es)

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
MX2021008518A true MX2021008518A (es) 2021-08-19

Family

ID=69740522

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2021008518A MX2021008518A (es) 2019-01-15 2020-01-13 Compuestos que modulan fxr(nr1h4).

Country Status (31)

Country Link
US (2) US11225473B2 (es)
EP (2) EP4360632A3 (es)
JP (2) JP7265635B2 (es)
KR (1) KR102692309B1 (es)
CN (1) CN113302190B (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)
ES (1) ES2973500T3 (es)
FI (1) FI3911647T3 (es)
HR (1) HRP20240265T1 (es)
HU (1) HUE065889T2 (es)
IL (1) IL284591A (es)
LT (1) LT3911647T (es)
MX (1) MX2021008518A (es)
NZ (1) NZ777524A (es)
PE (1) PE20211907A1 (es)
PL (1) PL3911647T3 (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
PT3730487T (pt) 2016-06-13 2022-07-22 Gilead Sciences Inc Derivados de azetidina como moduladores de fxr (nr1h4)
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
US20180280394A1 (en) 2017-03-28 2018-10-04 Gilead Sciences, Inc. Methods of treating liver disease
US20210393662A1 (en) * 2018-10-18 2021-12-23 Avolynt Use of sglt2 inhibitors to treat primary sclerosing cholangitis
CA3129949C (en) 2019-02-19 2024-04-30 Gilead Sciences, Inc. Solid forms of fxr agonists
MX2022008062A (es) 2020-01-15 2022-07-27 Inst Nat Sante Rech Med Uso del agonista fxr para el tratamiento de una infeccion por el virus de la hepatitis d.
US11478533B2 (en) 2020-04-27 2022-10-25 Novo Nordisk A/S Semaglutide for use in medicine
IL302099A (en) * 2020-10-15 2023-06-01 Lilly Co Eli FXR agonist polymorphs
AU2022208190A1 (en) 2021-01-14 2023-07-06 Enyo Pharma Method for treating chronic kidney diseases
JP2024502673A (ja) 2021-01-14 2024-01-22 ウエヌイグレックオ・ファーマ Ｈｂｖ感染の処置のためのｆｘｒアゴニストとｉｆｎの相乗効果
TW202308629A (zh) 2021-04-28 2023-03-01 法商Ｅｎｙｏ製藥公司 使用fxr激動劑作為組合治療以增強tlr3激動劑之療效
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 (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 (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
WO1994017059A1 (en) 1993-01-29 1994-08-04 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 (de) 1995-10-02 1997-04-03 Basf Ag Zwischenprodukte und Verfahren zur Herstellung von substituierten Salicylsäurederivaten als Pflanzenschutzmittel
WO1997029774A1 (en) 1996-02-13 1997-08-21 G.D. Searle & Co. Combinations, having immunosuppressive effects, containing a cyclooxygenase-2 inhibitor and a leukotriene a4 hydrolase inhibitor
JP2002532729A (ja) 1998-12-23 2002-10-02 グラクソ グループ リミテッド 核内受容体のリガンドのアッセイ
EP1185539B1 (en) 1999-06-11 2004-12-01 Allergan, Inc. Organosilyl compounds having nuclear hormone receptor modulating activity
US7022725B2 (en) 2000-11-17 2006-04-04 Takeda Pharmaceutical Company Limited Isoxazole derivatives
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
US20040131670A1 (en) 2001-04-17 2004-07-08 Ping Gao Pellicle-resistant gelatin capsule
US7223791B2 (en) 2001-06-26 2007-05-29 Takeda Pharmaceutical Company Limited Function regulator for retinoid relative receptor
EP1423113A4 (en) 2001-08-13 2007-04-18 Phenex Pharmaceuticals Ag NR1H4 NUCLEAR RECEPTOR BINDING COMPOUNDS
EP1285914B1 (en) 2001-08-13 2007-12-19 PheneX Pharmaceuticals AG Nr1h4 nuclear receptor binding compounds
US20070010562A1 (en) 2001-08-13 2007-01-11 Ulrike Bauer 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
MXPA05001592A (es) 2002-08-09 2005-05-05 Astrazeneca Ab Oxadiazoles como moduladores de receptor-5 de glutamato metabotropico.
WO2004014881A2 (en) 2002-08-09 2004-02-19 Astra Zeneca Ab '1,2,4'oxadiazoles as modulators of metabotropic glutamate receptor-5
CA2495179A1 (en) 2002-08-09 2004-02-19 Astrazeneca Ab Compounds having an activity at metabotropic glutamate receptors
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
WO2004048349A1 (en) 2002-11-22 2004-06-10 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
EP1815206B1 (en) 2004-10-13 2016-04-06 PTC Therapeutics, Inc. Compounds for nonsense suppression, and methods for their use
JP2008137894A (ja) 2005-03-22 2008-06-19 Nippon Kayaku Co Ltd 新規なアセチレン誘導体
EP1894919B1 (en) 2005-06-07 2012-03-28 Shionogi & Co., Ltd. Heterocyclic compound having type i 11 beta hydroxysteroid dehydrogenase inhibitory activity
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
CN101395170A (zh) 2006-02-14 2009-03-25 英特塞普特药品公司 用于预防或治疗fxr介导的疾病或状态的作为fxr配体的胆汁酸衍生物
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 (ja) 2006-03-28 2009-09-03 ノバルティス アクチエンゲゼルシャフト アミド誘導体およびｇタンパク質関連疾患の処置のためのそれらの使用
US20090286806A1 (en) 2006-04-17 2009-11-19 Hassan Pajouhesh Isoxazole derivatives as calcium channel blockers
US7846960B2 (en) 2006-05-24 2010-12-07 Eli Lilly And Company FXR agonists
BRPI0711875A2 (pt) 2006-05-24 2012-01-10 Lilly Co Eli compostos e métodos para modular os fxr
ATE549338T1 (de) 2006-05-24 2012-03-15 Boehringer Ingelheim Int Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
CN101522703B (zh) 2006-06-27 2013-04-17 英特塞普特医药品公司 胆酸派生物及其在制备预防或治疗fxr介导的疾病或状况的药物中的应用
EP2043651A2 (en) 2006-07-05 2009-04-08 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
CA2654898A1 (en) 2006-07-07 2008-10-01 Boehringer Ingelheim International Gmbh New chemical compounds
US20080032990A1 (en) 2006-07-07 2008-02-07 Khalifah Raja G Inhibitors of advanced glycation end products
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
KR20090094125A (ko) 2006-12-08 2009-09-03 엑셀리시스, 인코포레이티드 Ｌｘｒ 및 ｆｘｒ 조절자
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
PL2114885T3 (pl) 2007-02-09 2016-07-29 Dow Agrosciences Llc Sposób utleniania niektórych podstawionych sulfiloimin do owadobójczych sulfoksyimin
BRPI0807702B8 (pt) 2007-02-26 2022-06-28 Dow Agrosciences Llc Processo para a preparação de certas sulfiliminas substituídas
KR20100038102A (ko) 2007-06-13 2010-04-12 글락소스미스클라인 엘엘씨 파네소이드 ｘ 수용체 작용제
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
BRPI0812851A2 (pt) 2007-07-02 2014-09-30 Glaxosmithkline Llc Composto, composição farmacêutica, métodos para o tratamento de uma doença e de uma condição em um indivíduo, processo para preparar um composto, e, uso de um composto
WO2009003998A2 (en) 2007-07-02 2009-01-08 Boehringer Ingelheim International Gmbh Antiproliferative compounds based on 5-membered heterocycles
US20090197880A1 (en) 2007-07-13 2009-08-06 Genelabs Technologies, Inc. Anti-viral compounds, compositions, and methods of use
TW200920372A (en) 2007-07-13 2009-05-16 Genelabs Tech 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
EA201070189A1 (ru) 2007-08-01 2010-08-30 Х. Лундбекк А/С Применение соединений, открывающих калиевые каналы kcnq, для подавления симптомов или лечения расстройств или состояний, при которых нарушается дофаминергическая система
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
US8003649B2 (en) 2007-12-21 2011-08-23 Astrazeneca Ab Bicyclic derivatives for use in the treatment of androgen receptor associated conditions-155
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
EP2283001A2 (en) 2008-05-13 2011-02-16 Boehringer Ingelheim International GmbH Sulfone compounds which modulate the cb2 receptor
WO2009143018A2 (en) 2008-05-19 2009-11-26 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
CN102112478A (zh) 2008-06-10 2011-06-29 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
US8252939B2 (en) 2008-06-23 2012-08-28 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
WO2010025035A1 (en) 2008-08-25 2010-03-04 Dow Global Technologies Inc. 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
CA2736434A1 (en) 2008-09-25 2010-04-01 F. Hoffmann-La Roche Ag 3-amino-indazole or 3-amino-4,5,6,7-tetrahydro-indazole derivatives
CA2736880A1 (en) 2008-09-26 2010-04-01 Wyeth Llc 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors
MX2011004125A (es) 2008-10-21 2011-05-19 Metabolex Inc Agonistas del receptor gpr120 de arilo y usos de los mismos.
WO2010089303A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh CYCLIC INHIBITORS OF 11 β-HYDROXYSTEROID DEHYDROGENASE 1
KR20100092909A (ko) 2009-02-13 2010-08-23 주식회사 엘지생명과학 잔틴 옥시다제 저해제로서 효과적인 신규 화합물, 그 제조방법 및 그를 함유하는 약제학적 조성물
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
US8883832B2 (en) 2009-07-06 2014-11-11 Aerpio Therapeutics Inc. Compounds, compositions, and methods for preventing metastasis of cancer cells
WO2011003793A1 (en) 2009-07-06 2011-01-13 Basf Se Pyridazine compounds for controlling invertebrate pests
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
CN102469785A (zh) 2009-07-24 2012-05-23 巴斯夫欧洲公司 防治无脊椎动物害虫的吡啶衍生物
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
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
CN102883607B (zh) 2010-03-01 2015-07-22 Gtx公司 用于治疗癌的化合物
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
EP2655368A1 (en) 2010-12-20 2013-10-30 Irm Llc Compositions and methods for modulating farnesoid x receptors
US20140039007A1 (en) 2010-12-20 2014-02-06 David C. Tully 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
PL3628320T3 (pl) 2011-11-11 2022-07-25 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
KR101881245B1 (ko) 2012-06-19 2018-07-23 인터셉트 파마슈티컬즈, 인크. 오베티콜산의 제조법, 용도 및 고체 형태
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
EP2994139B1 (en) 2013-05-10 2019-04-10 Gilead Apollo, LLC Acc inhibitors and uses thereof
CN105377870B (zh) 2013-05-14 2018-04-03 英特塞普特医药品公司 作为法尼醇x受体调节剂的胆汁酸的11‑羟基衍生物及其氨基酸共轭物
BR112016002268B1 (pt) 2013-08-01 2022-11-01 The Penn State Research Foundation Uso de inibidores do receptor x farnesoide
EP3711762A1 (en) 2013-09-11 2020-09-23 INSERM (Institut National de la Santé et de la Recherche Médicale) A farnesoid x receptor agonsits foruse and pharmaceutical compositions for the treatment of chronic 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 (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
US20150119345A1 (en) 2013-10-29 2015-04-30 Lumena Pharmaceuticals, Inc. Bile acid recycling inhibitors for treatment of gastrointestinal infections
CN105682656B (zh) 2013-11-05 2019-11-05 诺华股份有限公司 调节法尼醇x受体的组合物和方法
WO2015116856A2 (en) 2014-01-29 2015-08-06 City Of Hope Farnesoid x receptor antagonists
KR20160132111A (ko) 2014-03-13 2016-11-16 더 솔크 인스티튜트 포 바이올로지칼 스터디즈 Fxr 작용제와 제조방법 및 용도
US10077268B2 (en) 2014-03-13 2018-09-18 Salk Institute For Biological Studies FXR agonists and methods for making and using
WO2015138969A1 (en) 2014-03-13 2015-09-17 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
HUE048351T2 (hu) 2014-05-29 2020-07-28 Bar Pharmaceuticals S R L Kolán-származékok alkalmazása FXR és TGR5/GPBAR1 mediált betegségek kezelésére és/vagy prevenciójára
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
JP2017533923A (ja) 2014-11-06 2017-11-16 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
MX370480B (es) 2014-11-21 2019-12-16 Akarna Therapeutics Ltd Compuestos bicíclicos fusionados para el tratamiento de enfermedades.
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
MX2017006833A (es) 2014-11-26 2018-02-13 Enanta Pharm Inc Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos.
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
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
CN107106555A (zh) 2014-12-18 2017-08-29 诺华股份有限公司 氮杂双环辛烷衍生物作为fxr激动剂在治疗肝脏和胃肠疾病中的应用
EP3597271A1 (en) 2015-01-09 2020-01-22 Gilead Apollo, LLC Acc inhibitor combination therapy for the treatment of non-alcoholic fatty liver disease
BR112017015273A2 (pt) 2015-01-20 2018-01-09 Merial Inc. compostos e composições antihelmínticos e método de utilizações dos mesmos
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
EP3892718A1 (en) 2015-09-11 2021-10-13 Propagenix Inc. Ex vivo proliferation of epithelial cells
PE20181269A1 (es) 2015-12-04 2018-08-03 Bristol Myers Squibb 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
EP3400229B1 (en) 2016-01-10 2024-03-06 Provincial Health Services Authority 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
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
WO2017189651A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
WO2017189652A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10144729B2 (en) 2016-05-18 2018-12-04 Enanta Pharmaceuticals, Inc. Isoxazole analogs 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
US10149835B2 (en) 2016-05-18 2018-12-11 Elmore Patent Law Group, P.C. Isoxazole derivatives as FXR agonists and methods of use thereof
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
AU2017274521B2 (en) 2016-06-03 2021-08-19 Chemocentryx, Inc. Method of treating liver fibrosis
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
PT3730487T (pt) 2016-06-13 2022-07-22 Gilead Sciences Inc Derivados de azetidina como moduladores de fxr (nr1h4)
PE20190971A1 (es) 2016-06-13 2019-07-09 Glaxosmithkline Ip Dev Ltd Compuestos quimicos
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
WO2018039384A1 (en) 2016-08-23 2018-03-01 Ardelyx, Inc. Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as fxr activators
CN110177783B (zh) 2016-08-23 2023-06-06 阿德利克斯股份有限公司 用于治疗代谢病状和病症的激素受体调节剂
WO2018059314A1 (zh) 2016-09-28 2018-04-05 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
CN109906223A (zh) 2016-10-04 2019-06-18 英安塔制药有限公司 异噁唑类似物作为fxr激动剂及其使用方法
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
IL266530B2 (en) 2016-11-10 2024-09-01 Galmed Res And Development Ltd Use of Amcol for the treatment of fibrosis
EP3538097A1 (en) * 2016-11-11 2019-09-18 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
US20180280394A1 (en) 2017-03-28 2018-10-04 Gilead Sciences, Inc. Methods of treating 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
KR20190132515A (ko) 2017-04-12 2019-11-27 길리애드 사이언시즈, 인코포레이티드 간 질환을 치료하는 방법
CA3129949C (en) 2019-02-19 2024-04-30 Gilead Sciences, Inc. Solid forms of fxr agonists
KR20240135055A (ko) 2019-03-11 2024-09-10 길리애드 사이언시즈, 인코포레이티드 화합물의 제제 및 그의 용도

Also Published As

Publication number Publication date
US20220204491A1 (en) 2022-06-30
US20200255418A1 (en) 2020-08-13
EP4360632A2 (en) 2024-05-01
TWI733307B (zh) 2021-07-11
CN113302190A (zh) 2021-08-24
EP3911647A1 (en) 2021-11-24
ES2973500T3 (es) 2024-06-20
DOP2021000148A (es) 2021-08-31
CL2021001877A1 (es) 2022-01-07
CO2021009240A2 (es) 2021-07-30
LT3911647T (lt) 2024-03-25
CR20210385A (es) 2021-09-14
NZ777524A (en) 2024-07-26
FI3911647T3 (fi) 2024-03-01
US11225473B2 (en) 2022-01-18
CA3124702A1 (en) 2020-07-23
HUE065889T2 (hu) 2024-06-28
JP2023062120A (ja) 2023-05-02
AR117814A1 (es) 2021-08-25
WO2020150136A1 (en) 2020-07-23
KR102692309B1 (ko) 2024-08-07
JP2022517108A (ja) 2022-03-04
JP7265635B2 (ja) 2023-04-26
AU2020209564A1 (en) 2021-07-15
EP3911647B1 (en) 2023-12-13
AU2023200994A1 (en) 2023-03-23
EA202191566A1 (ru) 2021-11-01
PL3911647T3 (pl) 2024-05-20
EP4360632A3 (en) 2024-06-19
BR112021011762A2 (pt) 2021-11-03
HRP20240265T1 (hr) 2024-05-10
CN113302190B (zh) 2024-10-18
DOP2023000196A (es) 2023-10-31
SI3911647T1 (sl) 2024-04-30
ZA202104705B (en) 2022-05-25
DK3911647T3 (da) 2024-02-26
TW202043220A (zh) 2020-12-01
PT3911647T (pt) 2024-03-04
IL284591A (en) 2021-08-31
AU2020209564B2 (en) 2022-12-01
SG11202107434PA (en) 2021-08-30
KR20210114457A (ko) 2021-09-23
PE20211907A1 (es) 2021-09-28

Similar Documents

Publication Publication Date Title
NZ777524A (en) Fxr (nr1h4) modulating compounds
NZ748641A (en) Fxr (nr1h4) modulating compounds
PH12020551959A1 (en) Fxr (nr1h4) modulating compounds
MX2019011629A (es) Nuevos compuestos que se unen a fxr (nr1h4) y modulan su actividad.
NZ732210A (en) Novel fxr (nr1h4) modulating compounds
TR201909093T4 (tr) Hidroksi içeren FXR (NR1H4) modüle edici bileşikleri.
MX2021001752A (es) Compuestos de pirrolo-dipiridina.
MY163109A (en) Novel fxr (nr1h4) binding and activity modulating compounds
MX2009002274A (es) Compuestos de enlace fxr heterociclicos.
SA521431279B1 (ar) D1 مشتق تتراهيدرو إيزوكينولين بديل كمعدِّل تفارغي إيجابي
MX2021009971A (es) Compuesto heterociclico, composicion farmaceutica que lo comprende, metodo para su preparacion, y uso de estos.
MX2021001804A (es) Compuestos de urea y composiciones como inhibidores de atpasa de smarca2/brm.
MX2021009188A (es) Uso de composición que contiene inhibidor de quinasa dependiente de ciclina 4/6 en combinación con anastrozol en la preparación de medicamentos para el tratamiento de enfermedades tumorales.