PL2987532T3 - Nowe związki wiążące i modulujące aktywność FXR (NR1H4) - Google Patents

Nowe związki wiążące i modulujące aktywność FXR (NR1H4)

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Publication number
PL2987532T3
PL2987532T3 PL15002478T PL15002478T PL2987532T3 PL 2987532 T3 PL2987532 T3 PL 2987532T3 PL 15002478 T PL15002478 T PL 15002478T PL 15002478 T PL15002478 T PL 15002478T PL 2987532 T3 PL2987532 T3 PL 2987532T3
Authority
PL
Poland
Prior art keywords
nr1h4
binding
modulating compounds
activity modulating
novel fxr
Prior art date
Application number
PL15002478T
Other languages
English (en)
Inventor
Olaf Kinzel
Christoph Steeneck
Claus Kremoser
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 PL2987532T3 publication Critical patent/PL2987532T3/pl

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    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further 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
    • A61K31/435Heterocyclic 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicinal Preparation (AREA)
PL15002478T 2011-07-13 2012-07-12 Nowe związki wiążące i modulujące aktywność FXR (NR1H4) PL2987532T3 (pl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161507153P 2011-07-13 2011-07-13
EP11005722A EP2545964A1 (en) 2011-07-13 2011-07-13 Novel FXR (NR1H4) binding and activity modulating compounds
EP15002478.4A EP2987532B1 (en) 2011-07-13 2012-07-12 Novel fxr (nr1h4) binding and activity modulating compounds
EP12735100.5A EP2731676B1 (en) 2011-07-13 2012-07-12 Novel fxr (nr1h4) modulating compounds

Publications (1)

Publication Number Publication Date
PL2987532T3 true PL2987532T3 (pl) 2017-10-31

Family

ID=44513243

Family Applications (2)

Application Number Title Priority Date Filing Date
PL12735100T PL2731676T3 (pl) 2011-07-13 2012-07-12 Nowe związki modulujące FXR (NR1H4)
PL15002478T PL2987532T3 (pl) 2011-07-13 2012-07-12 Nowe związki wiążące i modulujące aktywność FXR (NR1H4)

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PL12735100T PL2731676T3 (pl) 2011-07-13 2012-07-12 Nowe związki modulujące FXR (NR1H4)

Country Status (31)

Country Link
US (5) US9139539B2 (pl)
EP (5) EP2545964A1 (pl)
JP (2) JP5986633B2 (pl)
KR (4) KR101766323B1 (pl)
CN (2) CN107252424B (pl)
AR (1) AR087127A1 (pl)
AU (4) AU2012283387C1 (pl)
BR (3) BR112014000260B1 (pl)
CA (1) CA2839357C (pl)
CY (1) CY1117453T1 (pl)
DK (2) DK3246070T3 (pl)
EA (1) EA024843B1 (pl)
ES (2) ES2632492T3 (pl)
FI (1) FI3246070T3 (pl)
HK (2) HK1192181A1 (pl)
HR (2) HRP20240422T1 (pl)
HU (1) HUE027931T2 (pl)
IL (1) IL229944A (pl)
LT (1) LT3246070T (pl)
ME (1) ME02434B (pl)
MX (2) MX368371B (pl)
MY (1) MY161158A (pl)
PL (2) PL2731676T3 (pl)
PT (2) PT3246070T (pl)
RS (1) RS54786B1 (pl)
SI (3) SI2987532T1 (pl)
SM (1) SMT201600169B (pl)
TW (1) TWI439455B (pl)
UY (1) UY34196A (pl)
WO (1) WO2013007387A1 (pl)
ZA (1) ZA201309521B (pl)

Families Citing this family (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
IL253437A0 (en) * 2011-07-13 2017-09-28 Gilead Sciences Inc New compounds modulate fxr (nr1h4) activity and bind
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
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
CA2962572A1 (en) 2014-09-24 2016-03-31 Gilead Sciences, Inc. Methods of treating liver disease with a combination of an ask1 inhibitor and a fxr agonist
EP3006939A1 (en) 2014-10-06 2016-04-13 Gilead Sciences, Inc. Histidine-rich Glycoprotein as a marker for hepatic Farnesoid X receptor activation
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
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
MA41252A (fr) * 2014-12-23 2017-10-31 Gilead Sciences Inc Formes solides d'un inhibiteur d'ask 1
EP3693366B8 (en) 2014-12-23 2023-08-09 Gilead Sciences, Inc. Processes for preparing ask1 inhibitors
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
EP3277286B1 (en) 2015-03-31 2021-04-21 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
PT3456717T (pt) 2015-07-06 2021-05-26 Gilead Sciences Inc Derivado de 4,6-diamino-quinolina-3-carbonitrilo como modulador do cancro da tiróide de osaka (cot) para o tratamento de doenças inflamatórias
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
CN106995416A (zh) * 2016-01-26 2017-08-01 上海翰森生物医药科技有限公司 Fxr激动剂及其制备方法和应用
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
WO2017152062A1 (en) 2016-03-04 2017-09-08 Gilead Sciences, Inc. Compositions and combinations of autotaxin inhibitors
US20170306050A1 (en) 2016-04-08 2017-10-26 Gilead Sciences, Inc. Compositions and methods for treating cancer, inflammatory diseases and autoimmune diseases
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
US10080743B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017201152A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
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
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
CN106237332A (zh) * 2016-08-11 2016-12-21 河南大学 核受体fxr在肝癌干细胞靶向治疗中的应用
US10450306B2 (en) 2016-10-04 2019-10-22 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
CN107973790A (zh) * 2016-10-22 2018-05-01 合帕吉恩治疗公司 杂环fxr调节剂
US10597391B2 (en) 2016-10-26 2020-03-24 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof
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
CN108218852A (zh) * 2016-12-15 2018-06-29 宁波百纳西药业有限公司 一种螺环化合物、其制备方法、组合物及用途
WO2018133730A1 (zh) * 2017-01-20 2018-07-26 四川科伦博泰生物医药股份有限公司 一种杂环化合物及其制备方法和用途
WO2018153933A1 (en) 2017-02-21 2018-08-30 Genfit Combination of a ppar agonist with a fxr agonist
JOP20180017A1 (ar) 2017-03-14 2019-01-30 Gilead Sciences Inc مثبط كيناز منظم لإشارة تلاشي خلايا
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
JP2020515564A (ja) 2017-03-30 2020-05-28 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 エピソーマルウイルスの持続性及び発現を低下させるための方法及び医薬組成物
US10676500B2 (en) 2017-04-07 2020-06-09 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonyl carbamate bile acid derivatives
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
SI3612520T1 (sl) 2017-04-12 2022-01-31 Il Dong Pharmaceutical Co., Ltd. Izoksazolni derivati kot agonisti nuklearnega receptorja in njihove uporabe
JP7029583B2 (ja) 2017-05-31 2022-03-04 パナソニックIpマネジメント株式会社 洗濯機
WO2018231851A1 (en) 2017-06-13 2018-12-20 Gilead Sciences, Inc. Methods of treating liver fibrosis
EP3691648A1 (en) 2017-10-06 2020-08-12 Gilead Sciences, Inc. Combination therapy comprising an acc inhibitor
AU2018360577A1 (en) 2017-11-01 2020-06-18 Bristol-Myers Squibb Company Bridged bicyclic compounds as farnesoid X receptor modulators
CN111278821B (zh) 2017-11-01 2023-10-03 百时美施贵宝公司 作为法尼醇x受体调节剂的螺环化合物
JP7264906B2 (ja) 2017-11-01 2023-04-25 ブリストル-マイヤーズ スクイブ カンパニー ファルネソイドx受容体モジュレーターとしてのアルケン化合物
ES2963652T3 (es) 2017-11-01 2024-04-01 Bristol Myers Squibb Co Compuestos espirocíclicos de alquenos como moduladores del receptor x farnesoide
EP3704107B1 (en) 2017-11-01 2023-04-12 Bristol-Myers Squibb Company Multicyclic compounds as farnesoid x receptor modulators
US20200340060A1 (en) 2017-11-13 2020-10-29 Gilead Sciences, Inc. Compositions and methods for identifying and treating liver diseases and monitoring treatment outcomes
US10689391B2 (en) 2017-12-12 2020-06-23 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
CN110128432B (zh) 2018-02-02 2021-03-02 广东东阳光药业有限公司 含氮三环化合物及其在药物中的应用
WO2019160813A1 (en) 2018-02-14 2019-08-22 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
WO2020029908A1 (zh) * 2018-08-08 2020-02-13 广州市恒诺康医药科技有限公司 螺桥环化合物、其药物组合物及其用途
CN112638473B (zh) * 2018-08-08 2022-06-07 因奥必治疗有限公司 用于调节类法尼醇x受体的化合物以及制备和使用所述化合物的方法
CN113056271A (zh) 2018-09-18 2021-06-29 梅塔科林公司 法尼醇x受体激动剂及其用途
HU231223B1 (hu) 2018-09-28 2022-01-28 Richter Gedeon Nyrt. GABAA A5 receptor modulátor hatású biciklusos vegyületek
BR112021011762A2 (pt) 2019-01-15 2021-11-03 Gilead Sciences Inc Compostos para modulação de fxr (nr1h4)
KR20210129119A (ko) 2019-02-15 2021-10-27 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서 유용한 치환된 아미드 화합물
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
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
US11555032B2 (en) 2019-05-13 2023-01-17 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
TW202235416A (zh) 2019-06-14 2022-09-16 美商基利科學股份有限公司 Cot 調節劑及其使用方法
JP2022540699A (ja) 2019-07-18 2022-09-16 ウエヌイグレックオ・ファーマ インターフェロンの有害作用を減少させる方法
US20230105984A1 (en) 2019-12-23 2023-04-06 Svetlana Marukian Compositions and methods for the treatment of liver diseases and disorders
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
CN115666559A (zh) * 2020-03-18 2023-01-31 梅塔科林公司 用于治疗疾病的法尼醇x受体激动剂
US20240043418A1 (en) 2020-03-26 2024-02-08 Richter Gedeon Nyrt. 1,3-dihydro-2h-pyrrolo[3,4-c]pyridine derivatives as gabaa a5 receptor modulators
CA3175541A1 (en) 2020-03-30 2021-10-07 Gilead Sciences, Inc. Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound
KR20220160645A (ko) 2020-04-02 2022-12-06 길리애드 사이언시즈, 인코포레이티드 Cot 저해제 화합물의 제조 방법
US11478533B2 (en) 2020-04-27 2022-10-25 Novo Nordisk A/S Semaglutide for use in medicine
CN114656460A (zh) * 2020-12-22 2022-06-24 江苏天士力帝益药业有限公司 一种新型吡嗪结构fxr激动剂、制备方法及应用
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.
WO2022192428A1 (en) 2021-03-11 2022-09-15 Gilead Sciences, Inc. Glp-1r modulating compounds
CN117120429A (zh) 2021-03-29 2023-11-24 吉利德科学公司 Khk抑制剂
CA3213217A1 (en) 2021-04-28 2022-11-03 Raphael Darteil Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
TW202304435A (zh) 2021-06-04 2023-02-01 美商基利科學股份有限公司 治療nash之方法
IL308122A (en) 2021-06-16 2023-12-01 Celgene Corp Azetidinyl compounds consisting of a carboxylic acid group for the treatment of neurodegenerative diseases
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
WO2023125904A1 (zh) * 2021-12-30 2023-07-06 苏州晶云药物科技股份有限公司 氮杂环丁基烟酸类化合物的晶型及其制备方法
WO2024089582A1 (en) 2022-10-25 2024-05-02 Assia Chemical Industries Ltd. Solid state forms of cilofexor salts

Family Cites Families (186)

* 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
US20040105884A1 (en) 2001-04-17 2004-06-03 Ping Gao Pharmaceutical dosage form comprising a sulfite compound
US20040105883A1 (en) 2001-04-17 2004-06-03 Ping Gao Pharmaceutical dosage form capable of maintaining stable dissolution profile upon storage
US20040131670A1 (en) 2001-04-17 2004-07-08 Ping Gao Pellicle-resistant gelatin capsule
US20040105885A1 (en) 2001-04-17 2004-06-03 Ping Gao Gelatin capsule exhibiting reduced cross-linking
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
US7074809B2 (en) 2002-08-09 2006-07-11 Astrazeneca Ab Compounds
TWI341314B (en) 2002-08-09 2011-05-01 Astrazeneca Ab New 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
EP2007759A4 (en) 2006-04-17 2010-12-22 Neuromed Pharmaceuticals Ltd ISOXAZOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
MX2008014854A (es) 2006-05-24 2008-12-05 Lilly Co Eli Antagonistas de fxr.
CA2651373A1 (en) 2006-05-24 2007-12-06 Eli Lilly And Company Compounds and methods for modulating fxr
CN101448798A (zh) * 2006-05-24 2009-06-03 伊莱利利公司 用于调节fxr的化合物和方法
EP2029600B1 (de) 2006-05-24 2012-03-14 Boehringer Ingelheim International GmbH Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
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
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
WO2008013660A2 (en) 2006-07-07 2008-01-31 Biostratum, Inc. Inhibitors of advanced glycation end products
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 (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
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
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
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
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
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
EP2128158A1 (en) 2008-05-26 2009-12-02 Phenex Pharmaceuticals AG Heterocyclic cyclopropyl-substituted FXR binding compounds
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
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
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
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
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
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
CU24152B1 (es) 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
JP2014500318A (ja) 2010-12-20 2014-01-09 アイアールエム・リミテッド・ライアビリティ・カンパニー ファルネソイドx受容体を調節するための組成物および方法
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
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
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
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives 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
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
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
ES2550374B1 (es) * 2015-06-30 2016-09-08 Universidad De La Rioja Compuestos fotoprotectores análogos de MAA, procedimiento de síntesis y composición que comprende los mismos
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
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
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
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
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
WO2017189652A1 (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
US10144729B2 (en) 2016-05-18 2018-12-04 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
WO2017201155A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. lSOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF
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
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
MX2018015443A (es) 2016-06-13 2019-04-11 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
US11091482B2 (en) 2016-08-23 2021-08-17 Ardelyx, Inc. Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as FXR activators
MA46052A (fr) 2016-08-23 2021-03-17 Ardelyx Inc Modulateurs du récepteur hormonal pour le traitement d'états et de troubles métaboliques
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
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

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