HK1245786B - 新的fxr(nr1h4)調節化合物 - Google Patents

新的fxr(nr1h4)調節化合物

Info

Publication number
HK1245786B
HK1245786B HK18105262.0A HK18105262A HK1245786B HK 1245786 B HK1245786 B HK 1245786B HK 18105262 A HK18105262 A HK 18105262A HK 1245786 B HK1245786 B HK 1245786B
Authority
HK
Hong Kong
Prior art keywords
nr1h4
modulating compounds
novel fxr
fxr
novel
Prior art date
Application number
HK18105262.0A
Other languages
English (en)
Inventor
Olaf Kinzel
Claus Kremoser
Peter A Blomgren
Kevin S Currie
Jeffrey E Kropf
Aaron Schmitt
William J Watkins
Jianjun Xu
Christian Gege
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 HK1245786B publication Critical patent/HK1245786B/zh

Links

Classifications

    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic 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
    • C07D261/08—Heterocyclic 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
HK18105262.0A 2014-12-17 2018-04-23 新的fxr(nr1h4)調節化合物 HK1245786B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14004260.7A EP3034499A1 (en) 2014-12-17 2014-12-17 Novel FXR (NR1H4) modulating compounds
PCT/EP2015/002512 WO2016096116A1 (en) 2014-12-17 2015-12-14 Novel fxr (nr1h4) modulating compounds

Publications (1)

Publication Number Publication Date
HK1245786B true HK1245786B (zh) 2019-11-08

Family

ID=52338777

Family Applications (1)

Application Number Title Priority Date Filing Date
HK18105262.0A HK1245786B (zh) 2014-12-17 2018-04-23 新的fxr(nr1h4)調節化合物

Country Status (23)

Country Link
US (1) US9938278B2 (zh)
EP (2) EP3034499A1 (zh)
JP (2) JP6452821B2 (zh)
KR (1) KR101955840B1 (zh)
CN (1) CN107108595B (zh)
AR (1) AR103064A1 (zh)
AU (1) AU2015365945B2 (zh)
BR (1) BR102015031497A2 (zh)
CA (1) CA2971241C (zh)
EA (1) EA033642B1 (zh)
ES (1) ES2719902T3 (zh)
HK (1) HK1245786B (zh)
IL (1) IL252496A0 (zh)
MX (1) MX2017007522A (zh)
NZ (1) NZ732210A (zh)
PL (1) PL3233831T3 (zh)
PT (1) PT3233831T (zh)
SG (1) SG11201704539TA (zh)
SI (1) SI3233831T1 (zh)
TR (1) TR201906401T4 (zh)
TW (1) TWI598345B (zh)
UY (1) UY36452A (zh)
WO (1) WO2016096116A1 (zh)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI491606B (zh) 2009-07-13 2015-07-11 Gilead Sciences Inc 調節細胞凋亡信號之激酶的抑制劑
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
EP3034499A1 (en) * 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
BR112017013858A2 (pt) 2014-12-26 2018-02-27 Univ Emory n4-hidroxicitidina e derivados e usos antivirais relacionados aos 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
CN107427527B (zh) 2015-03-31 2021-01-26 英安塔制药有限公司 作为fxr/tgr5激动剂的胆汁酸衍生物及其使用方法
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
US10080743B2 (en) 2016-04-26 2018-09-25 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
WO2017189651A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10149835B2 (en) 2016-05-18 2018-12-11 Elmore Patent Law Group, P.C. Isoxazole derivatives as FXR agonists and methods of use thereof
US10144729B2 (en) 2016-05-18 2018-12-04 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
WO2017201152A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
JP6678779B2 (ja) 2016-06-13 2020-04-08 ギリアード サイエンシーズ， インコーポレイテッド Ｆｘｒ（ｎｒ１ｈ４）調節化合物
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
KR20190056436A (ko) 2016-10-04 2019-05-24 이난타 파마슈티칼스, 인코포레이티드 Fxr 작용제로서의 이속사졸 유사체 및 그의 사용 방법
CN107973790A (zh) * 2016-10-22 2018-05-01 合帕吉恩治疗公司 杂环fxr调节剂
WO2018081285A1 (en) 2016-10-26 2018-05-03 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as fxr agonists and methods of use thereof
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
CN109071468B (zh) * 2017-01-20 2022-09-02 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
CN110461328A (zh) 2017-03-28 2019-11-15 吉利德科学公司 治疗肝疾病的治疗组合
KR102168543B1 (ko) 2017-04-12 2020-10-21 일동제약(주) 핵 수용체의 효능제인 아이속사졸 유도체 및 이의 용도
WO2018215070A1 (en) * 2017-05-24 2018-11-29 Johann Wolfgang Goethe-Universität Frankfurt am Main Dual modulators of farnesoid x receptor and soluble epoxide hydrolase
WO2019089672A1 (en) 2017-11-01 2019-05-09 Bristol-Myers Squibb Company Spirocyclic compounds as farnesoid x receptor modulators
CN111295382B (zh) 2017-11-01 2024-02-02 百时美施贵宝公司 作为法尼酯x受体调节剂的桥联双环化合物
WO2019089665A1 (en) * 2017-11-01 2019-05-09 Bristol-Myers Squibb Company Alkene spirocyclic compounds as farnesoid x receptor modulators
KR20200081435A (ko) 2017-11-01 2020-07-07 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서의 멀티시클릭 화합물
KR20200081436A (ko) * 2017-11-01 2020-07-07 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서의 알켄 화합물
MX2020005392A (es) 2017-12-07 2020-12-07 Univ Emory N4-hidroxicitidina y derivados y usos antivirales relacionados con los mismos.
WO2019118571A1 (en) 2017-12-12 2019-06-20 Enanta Pharmaceuticals, Inc. Isoxazole analogs as fxr agonists and methods of use thereof
JP7243959B2 (ja) * 2017-12-22 2023-03-22 シチュアン ケルン－バイオテック バイオファーマシューティカル カンパニー リミテッド イソオキサゾール誘導体、その製造方法、及びその使用
CN108129348B (zh) * 2018-01-12 2019-11-01 南开大学 叠氮三氟甲氧基化合物及其合成方法
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
JP7457020B2 (ja) * 2018-08-08 2024-03-27 インオルビット セラピューティクス エイビー ファルネソイドｘ受容体の調節に有用な化合物並びに当該化合物の製造方法及び使用方法
CN112585532B (zh) 2018-08-31 2022-08-30 索尼公司 照明装置和显示设备
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
KR20210114457A (ko) 2019-01-15 2021-09-23 길리애드 사이언시즈, 인코포레이티드 Fxr (nr1h4) 조정 화합물
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
US11524005B2 (en) 2019-02-19 2022-12-13 Gilead Sciences, Inc. Solid forms of FXR agonists
CN110144349A (zh) * 2019-04-21 2019-08-20 吉林省农业科学院 一种大豆叶特异启动子GmNR1(Glyma14g33480)及其分离方法和应用
WO2020231917A1 (en) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US20220241376A1 (en) 2019-07-18 2022-08-04 Enyo Pharma Method for decreasing adverse-effects of interferon
AU2020319052A1 (en) 2019-07-23 2022-01-27 Novartis Ag Combination treatment of liver diseases using FXR agonists
US20220265614A1 (en) 2019-07-23 2022-08-25 Novartis Ag Treatment comprising fxr agonists
US20220340668A1 (en) 2019-09-03 2022-10-27 Novartis Ag Treatment of liver disease or disorder comprising actrii receptor antagonists
JP2022548617A (ja) 2019-09-19 2022-11-21 ノバルティス アーゲー Ｆｘｒアゴニストを含む処置
WO2021064575A1 (en) 2019-09-30 2021-04-08 Novartis Ag Treatment comprising the use of fxr agonists
CN114929218A (zh) 2019-12-20 2022-08-19 诺华股份有限公司 使用整联蛋白抑制剂组合治疗肝脏疾病
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
WO2022101853A1 (en) 2020-11-16 2022-05-19 Novartis Ag Method of determining liver fibrosis
KR20230154806A (ko) 2021-01-14 2023-11-09 엔요 파마 Hbv 감염 치료를 위한 fxr 작용제 및 ifn의 상승작용효과
EP4329761A1 (en) 2021-04-28 2024-03-06 ENYO Pharma Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
IL310708A (en) * 2021-08-12 2024-04-01 Shanghai Simr Biotechnology Co Ltd The history of converted triazole, a method for its preparation, its pharmaceutical preparation and its use
CN113876789B (zh) * 2021-10-28 2022-05-20 兰州大学第一医院 Licraside用于制备治疗胆汁淤积药物的用途
CN117430574B (zh) * 2023-12-20 2024-03-22 潍坊医学院 一种苯并呋喃衍生物及其制备方法、用途

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE433106T1 (de) 1998-12-23 2009-06-15 Glaxo Group Ltd Bestimmungsmethode fur liganden der nuklearen rezeptoren
ATE381542T1 (de) 2001-08-13 2008-01-15 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
WO2003080803A2 (en) 2002-03-21 2003-10-02 Smithkline Beecham Corporation Methods of using farnesoid x receptor (fxr) agonists
EP1562915A1 (en) 2002-11-22 2005-08-17 SmithKline Beecham Corporation Farnesoid x receptor agonists
WO2004087076A2 (en) 2003-03-31 2004-10-14 The Rockefeller University Methods for inhibiting adipogenesis and for treating type 2 diabetes
EP1962838B1 (en) 2005-12-19 2011-09-28 GlaxoSmithKline LLC Farnesoid x receptor agonists
CN101374834B (zh) 2006-02-03 2011-12-14 伊莱利利公司 用于调节fxr的化合物和方法
ATE465996T1 (de) 2006-05-24 2010-05-15 Lilly Co Eli Fxr-agonisten
MX2008014959A (es) 2006-05-24 2008-12-09 Lilly Co Eli Compuestos y metodos para modular fxr.
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
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,
KR20090094125A (ko) * 2006-12-08 2009-09-03 엑셀리시스, 인코포레이티드 Ｌｘｒ 및 ｆｘｒ 조절자
BRPI0812521A2 (pt) 2007-06-13 2015-06-23 Glaxosmithkline Llc Composto, composição farmacêutica, método para o tratamento de doença em um mamífero, processo para a preparação de um composto, e, uso de um composto
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
TW200906823A (en) 2007-07-16 2009-02-16 Lilly Co Eli Compounds and methods for modulating FXR
AU2008339572B2 (en) * 2007-12-21 2012-05-10 Astrazeneca Ab Bicyclic derivatives for use in the treatment of androgen receptor associated conditions
EP2289883A1 (en) 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
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
EP3034499A1 (en) * 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
MA41252A (fr) * 2014-12-23 2017-10-31 Gilead Sciences Inc Formes solides d'un inhibiteur d'ask 1

Also Published As

Publication number Publication date
AU2015365945A1 (en) 2017-06-15
TWI598345B (zh) 2017-09-11
EP3233831B1 (en) 2019-02-20
TR201906401T4 (tr) 2019-05-21
EA201791002A1 (ru) 2018-06-29
JP2018162309A (ja) 2018-10-18
EA033642B1 (ru) 2019-11-12
EP3233831A1 (en) 2017-10-25
AU2015365945B2 (en) 2018-09-27
CA2971241C (en) 2021-06-22
US20170298068A1 (en) 2017-10-19
SI3233831T1 (sl) 2019-05-31
AR103064A1 (es) 2017-04-12
PL3233831T3 (pl) 2019-08-30
IL252496A0 (en) 2017-07-31
EP3034499A1 (en) 2016-06-22
CA2971241A1 (en) 2016-06-23
MX2017007522A (es) 2017-08-22
KR101955840B1 (ko) 2019-03-07
NZ732210A (en) 2018-11-30
UY36452A (es) 2016-07-29
CN107108595B (zh) 2021-04-06
WO2016096116A1 (en) 2016-06-23
TW201627292A (zh) 2016-08-01
ES2719902T3 (es) 2019-07-16
JP2018500305A (ja) 2018-01-11
KR20170093969A (ko) 2017-08-16
US9938278B2 (en) 2018-04-10
JP6452821B2 (ja) 2019-01-16
CN107108595A (zh) 2017-08-29
PT3233831T (pt) 2019-05-09
SG11201704539TA (en) 2017-07-28
BR102015031497A2 (pt) 2016-06-21

Similar Documents

Publication Publication Date Title
HK1245786B (zh) 新的fxr(nr1h4)調節化合物
IL263495A (en) Modulating compounds (fxr (nr1h4
HK1251552A1 (zh) 含羥基的fxr(nr1h4)調節化合物
IL263493B (en) Modulating compounds (fxr (nr1h4
GB201416754D0 (en) Novel compounds
GB201417011D0 (en) Novel compounds
GB201417094D0 (en) Novel compounds
GB201417018D0 (en) Novel compounds
AP2016009432A0 (en) Novel compounds
GB201405991D0 (en) Novel compounds
GB201411236D0 (en) Novel compounds
GB201411239D0 (en) Novel compounds
GB201404002D0 (en) Novel compounds
GB201419102D0 (en) Novel compounds
HK1226059A1 (zh) 新的fxr(nr1h4)調節化合物
GB201421784D0 (en) Novel compounds
GB201417041D0 (en) Novel compounds
GB201417021D0 (en) Novel compounds
GB201417043D0 (en) Novel compounds
GB201414614D0 (en) Novel compounds
GB201413451D0 (en) Novel compounds
GB201413260D0 (en) Novel compounds
GB201412689D0 (en) Novel compounds
GB201409911D0 (en) Novel compounds
GB201409221D0 (en) Novel Compounds