ME02434B - Nova jedinjenja koja moduliraju fxr (nr1h4) - Google Patents

Nova jedinjenja koja moduliraju fxr (nr1h4)

Info

Publication number
ME02434B
ME02434B MEP-2016-81A MEP201681A ME02434B ME 02434 B ME02434 B ME 02434B ME P201681 A MEP201681 A ME P201681A ME 02434 B ME02434 B ME 02434B
Authority
ME
Montenegro
Prior art keywords
liver
alkyl
compound according
group
disease
Prior art date
Application number
MEP-2016-81A
Other languages
German (de)
English (en)
French (fr)
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 ME02434B publication Critical patent/ME02434B/me

Links

Classifications

    • 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further 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
    • A61K31/435—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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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

Landscapes

  • 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)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency 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)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (17)

1. Jedinjenje prema sledećoj formuli (1), njegov enantiomer, diastereomer, tautomer ili farmaceutski prihvatljiva so u komeR je izabran iz grupe koja se sastoji od COOR6, CONR7R8, tetrazolil, SO2NR7R8, C1-6 alkil, SO2-C1-6 alkil i H, pri čemu je R6 nezavisno izabran iz grupe koja se sastoji od H ili C1-6alkil, i R7 i R8 međusobno nezavisno su izabrani iz grupe koja se sastoji od H, C1-6alkil, halo-C1-6 alkil, C1-6 alkilen-R9, SO2-C1-6, alkil, gde je R9 izabran iz grupe koja se sastoji od COOH, OH i SO3H;A je izabran iz grupe koja se sastoji od: fenil, piridil, pirimidil, pirazolil, indolil, tienil, benzotienil, indazolil, benzizoksazolil, benzofuranil, benzotriazolil, furanil, benzotiazolil, tiazolil, oksadiazolil, svaki izborno supstituisan sa jednom ili dve grupe nezavisno izabrane iz grupe koja se sastoji od OH, O-C1-6 alkil, O-halo-C1-6 alkil, alkil, halo-C1-6 alkil, C3-6 cikloalkil i halogen;Q je izabran iz grupe koja se sastoji od fenil, piridil, tiazolil, tiofenil, pirimidil, svaka izborno supstituisana sa jednom ili dvegrupe nezavisno izabrane iz grupe koja se sastoji od C1-6alkil, halo-C1-6 alkil, halogen i CF3;Y je izabran od N ili CH;Z je izabran od ili u komeX = CH, N, NO;R1 je izabran iz grupe koja se sastoji od vodonika, C1-3 alkil, C3-6 cikloalkil, C4-5 alkilcikloalkil, gde je C1-3 alkil izborno supstituisan sa 1 do 3 supstituenta nezavisno izabrana od halogena, hidroksi ili C1-6alkoksi;R2 i R3 su nezavisno izabrani iz grupe koja se sastoji od vodonika, C1-3 alkil, C1-3 haloalkil, C1-3 alkoksi, C1-3 haloalkoksi i halogen.
2. Jedinjenje prema patentnom zahtevu 1 naznačeno time što R-A je izabran od ili
3. Jedinjenje prema patentnom zahtevu 1 ili 2 naznačeno time što Q je
4. Jedinjenje prema bilo kom od patentnih zahteva 1 do 3 naznačeno time što Z je
5. Jedinjenje prema bilo kom od patentnih zahteva 1 do 4 izabrano od ili ili njegova farmaceutski prihvatljiva so.
6. Jedinjenje prema bilo kom od patentnih zahteva 1 do 5 koje ima sledeću strukturu ili njegova farmaceutski prihvatljiva so.
7. Jedinjenje prema bilo kom od patentnih zahteva 1 do 5 koje ima sledeću strukturu ili njegova farmaceutski prihvatljiva so.
8. Farmaceutska kompozicija koja sadrži jedinjenje prema bilo kom od patentnih zahteva 1 do 7, ili njegovu farmaceutski prihvatljivu so, i farmaceutski prihvatljiv nosač.
9. Jedinjenje prema bilo kom od patentnih zahteva 1 do 7 za upotrebu kao lek.
10. Jedinjenje prema bilo kom od patentnih zahteva 1 do 7 za upotrebu u profilaksi i/ili lečenju bolesti posredovanih preko FXR.
11. Jedinjenje za upotrebu prema patentnom zahtevu 10 naznačeno time što je bolest izabrana od hroničnog intrahepatičnog ili izvesnih oblika ekstrahepatičnih holestatičkih stanja; fibroze jetre; opstruktivnih ili hroničnih inflamatornih poremećaja jetre; ciroze jetre; steatoze jetre i srodnih sindroma, holestatičkih ili fibrotičkih efekata koji su povezani sa cirozom koja je indukovana alkoholom ili sa virusnim oblicima hepatitisa; insuficijencije jetre ili ishemije jetre posle velike resekcije jetre; steatohepatitisa povezanog sa hemoterapijom (CASH); akutne insuficijencije jetre; i/ili inflamatornih bolesti creva.
12. Jedinjenje za upotrebu prema patentnom zahtevu 10 naznačeno time što je bolest izabrana od poremećaja lipida i lipoproteina; dijabetesa tipa II i kliničkih komplikacija dijabetesa tipa I i tipa II, uključujući dijabetičku nefropatiju, dijabetičku neuropatiju, dijabetičku retinopatiju i druge zabeležene efekte kliničke manifestacije dugotrajnog dijabetesa; stanja i bolesti koja su rezultat hronične masne i fibrotičke degeneracije organa kao posledica pojačane akumulacije lipida i naročito triglicerida i kasnije aktivacije profibrotičkih puteva, kao što je bolest nealkoholne masne jetre (NAFLD) ili nealkoholni steatohepatitis (NASH); gojaznosti ili metaboličkog sindroma (kombinovana stanja dislipidemije, dijabetesa ili abnormalno visokog indeksa telesne mase); i/ili akutnog infarkta miokarda, akutnog šloga ili tromboze koji se javlja kao krajnja tačka hronične opstruktivne ateroskleroze.
13. Jedinjenje za upotrebu prema patentnom zahtevu 10 naznačeno time što je bolest izabrana od nemalignih hiperproliferativnih poremećaja i malignih hiperproliferativnih poremećaja, naročito hepatoćelijskog karcinoma, adenoma debelog creva i polipoza, adenokarcinoma debelog creva, kancera dojke, adenokarcinoma pankreasa, Baretovog jednjaka ili drugih oblika neoplastičnih bolesti gastrointestinalnog trakta i jetre.
14. Upotreba jedinjenja prema bilo kom od patentnih zahteva 1 do 7 za pripremu leka za profilaksu i/ili lečenje bolesti posredovanih preko FXR.
15. Upotreba prema patentnom zahtevu 14 naznačena time što je bolest izabrana od hroničnih intrahepatičnih ili izvesnih oblika ekstrahepatičnih holestatičkih stanja; fibroze jetre; opstruktivnih ili hroničnih inflamatornih poremećaja jetre; ciroze jetre; steatoze jetre i povezanih sindroma, holestatičkih ili fibrotičkih efekata koji su povezani sa cirozom koja je indukovana alkoholom ili sa virusnim oblicima hepatitisa; insuficijencije jetre ili ishemije jetre posle velike resekcije jetre; steatohepatitisa povezanog sa hemoterapijom (CASH); akutne insuficijencije jetre; i/ili inflamatornih bolesti creva.
16. Upotreba prema patentnom zahtevu 14 naznačena time što je bolest izabrana od poremećaja lipida i lipoproteina; dijabetesa tipa II i kliničkih komplikacija dijabetesa tipa I i tipa II, uključujući dijabetičku nefropatiju, dijabetičku neuropatiju, dijabetičku retinopatiju i druge zabeležene efekte kliničke manifestacije dugotrajnog dijabetesa; stanja i bolesti koji su rezultat hronične masne i fibrotičke degeneracije organa kao posledica pojačane akumulacije lipida i naročito triglicerida i kasnije aktivacije profibrotičkih puteva; kao što je bolest nealkoholne masne jetre (NAFLD) ili nealkoholni steatohepatitis (NASH); gojaznosti ili metaboličkog sindroma (kombinovana stanja dislipidemije, dijabetesa ili abnormalno visokog indeksa telesne mase); i/ili akutnog infarkta miokarda, akutnog šloga ili tromboze koja se javlja kao krajnja tačka hronične opstruktivne ateroskleroze.
17. Upotreba prema patentnom zahtevu 14 naznačena time što je bolest izabrana od nemalignih hiperproliferativnih poremećaja i malignih hiperproliferativnih poremećaja, naročito hepatoćelijskog karcinoma, adenoma debelog creva i polipoza, adenokarcinoma debelog creva, kancera dojke, adenokarcinoma pankreasa, Baretovog jednjaka ili drugih oblika neoplastičnih bolesti gastrointestinalnog trakta i jetre.
MEP-2016-81A 2011-07-13 2012-07-12 Nova jedinjenja koja moduliraju fxr (nr1h4) ME02434B (me)

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
EP12735100.5A EP2731676B1 (en) 2011-07-13 2012-07-12 Novel fxr (nr1h4) modulating compounds
PCT/EP2012/002941 WO2013007387A1 (en) 2011-07-13 2012-07-12 Novel fxr (nr1h4) binding and activity modulating compounds

Publications (1)

Publication Number Publication Date
ME02434B true ME02434B (me) 2016-09-20

Family

ID=44513243

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2016-81A ME02434B (me) 2011-07-13 2012-07-12 Nova jedinjenja koja moduliraju fxr (nr1h4)

Country Status (31)

Country Link
US (5) US9139539B2 (me)
EP (6) EP2545964A1 (me)
JP (2) JP5986633B2 (me)
KR (4) KR101766323B1 (me)
CN (2) CN107252424B (me)
AR (1) AR087127A1 (me)
AU (4) AU2012283387C1 (me)
BR (3) BR122019026062B1 (me)
CA (1) CA2839357C (me)
CY (1) CY1117453T1 (me)
DK (2) DK3246070T3 (me)
EA (1) EA024843B1 (me)
ES (3) ES2569718T3 (me)
FI (1) FI3246070T3 (me)
HR (2) HRP20160442T1 (me)
HU (2) HUE066734T2 (me)
IL (1) IL229944A (me)
LT (1) LT3246070T (me)
ME (1) ME02434B (me)
MX (2) MX368371B (me)
MY (1) MY161158A (me)
PH (1) PH12014500124A1 (me)
PL (3) PL3246070T3 (me)
PT (2) PT2987532T (me)
RS (1) RS54786B1 (me)
SI (3) SI3246070T1 (me)
SM (1) SMT201600169B (me)
TW (1) TWI439455B (me)
UY (1) UY34196A (me)
WO (1) WO2013007387A1 (me)
ZA (1) ZA201309521B (me)

Families Citing this family (92)

* 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
MX377523B (es) 2013-09-11 2025-03-10 Inst Nat Sante Rech Med Metodos y composiciones farmaceuticas para el tratamiento de la infeccion por el virus de la hepatitis b.
US10238636B2 (en) 2014-09-24 2019-03-26 Gilead Sciences, Inc. Methods of treating liver disease
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
SG11201704340VA (en) * 2014-12-18 2017-07-28 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
US9586933B2 (en) 2014-12-23 2017-03-07 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
RU2712099C2 (ru) 2015-03-31 2020-01-24 Энанта Фармасьютикалс, Инк. Производные желчных кислот в качестве агонистов fxr/tgr5 и способы их применения
ES2734713T3 (es) 2015-07-06 2019-12-11 Gilead Sciences Inc Moduladores Cot y métodos de utilización de los mismos
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
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
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
JP2019510752A (ja) 2016-03-04 2019-04-18 ギリアード サイエンシーズ， インコーポレイテッド オートタキシン阻害剤の組成物及び合剤
JP2019513737A (ja) 2016-04-08 2019-05-30 ギリアード サイエンシーズ， インコーポレイテッド がん、炎症性疾患および自己免疫疾患を処置するための組成物および方法
US10080742B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10080741B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10080743B2 (en) 2016-04-26 2018-09-25 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
NZ748641A (en) 2016-06-13 2020-04-24 Gilead Sciences Inc Fxr (nr1h4) modulating compounds
AR108711A1 (es) * 2016-06-13 2018-09-19 Gilead Sciences Inc Compuestos moduladores de fxr (nr1h4)
CA2968836C (en) * 2016-06-13 2025-09-02 Gilead Sciences, Inc. FXR MODULATING COMPOUNDS (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
CA3039124A1 (en) 2016-10-04 2018-04-12 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
WO2018081285A1 (en) * 2016-10-26 2018-05-03 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
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
JP7618384B2 (ja) 2017-02-21 2025-01-21 ジェンフィ Ｐｐａｒアゴニストとｆｘｒアゴニストとの組合せ
WO2018169742A1 (en) 2017-03-14 2018-09-20 Gilead Sciences, Inc. Apoptosis signal-regulating kinase inhibtor
ES2982801T3 (es) * 2017-03-28 2024-10-17 Gilead Sciences Inc Combinaciones terapéuticas para el tratamiento de las enfermedades hepáticas
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
MX388300B (es) 2017-04-07 2025-03-19 Enanta Pharm Inc Proceso para la preparación de derivados de ácidos biliares de sulfonil carbamato
RU2741306C1 (ru) 2017-04-12 2021-01-25 Ил Дон Фармасьютикал Ко., Лтд. Производные изоксазола в качестве агонистов ядерных рецепторов и их применение
EP3609496A1 (en) * 2017-04-12 2020-02-19 Gilead Sciences, Inc. Methods of treating liver disease
WO2018231851A1 (en) 2017-06-13 2018-12-20 Gilead Sciences, Inc. Methods of treating liver fibrosis
CN111182904A (zh) 2017-10-06 2020-05-19 吉利德科学公司 包含acc抑制剂的组合治疗
KR102731925B1 (ko) 2017-11-01 2024-11-18 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서의 멀티시클릭 화합물
US11286252B2 (en) 2017-11-01 2022-03-29 Bristol-Myers Squibb Company Alkene spirocyclic 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
US11168079B2 (en) 2017-11-01 2021-11-09 Bristol-Myers Squibb Company Alkene compounds as farnesoid x receptor modulators
JP7212693B2 (ja) 2017-11-01 2023-01-25 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架橋二環化合物
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
AU2019319750A1 (en) 2018-08-08 2021-03-04 Inorbit Therapeutics Ab Compounds useful in modulating the farnesoid X receptor and methods of making and using the same
EP3852748B1 (en) 2018-09-18 2025-09-03 Eli Lilly and Company Farnesoid x receptor agonists and uses thereof
HU231223B1 (hu) 2018-09-28 2022-01-28 Richter Gedeon Nyrt. GABAA A5 receptor modulátor hatású biciklusos vegyületek
KR102692309B1 (ko) 2019-01-15 2024-08-07 길리애드 사이언시즈, 인코포레이티드 Fxr (nr1h4) 조정 화합물
US12479816B2 (en) 2019-02-08 2025-11-25 University of Pittsburgh—of the Commonwealth System of Higher Education 20-HETE formation inhibitors
JP7465883B2 (ja) 2019-02-15 2024-04-11 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としての置換二環式化合物
US12319676B2 (en) 2019-02-15 2025-06-03 Bristol-Myers Squibb Company Substituted amide compounds useful as farnesoid X receptor modulators
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
JP7449300B2 (ja) 2019-02-15 2024-03-13 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として有用な置換アミド化合物
WO2020172075A1 (en) 2019-02-19 2020-08-27 Gilead Sciences, Inc. Solid forms of fxr agonists
JP7697885B2 (ja) 2019-03-11 2025-06-24 ギリアード サイエンシーズ， インコーポレイテッド 化合物の製剤およびそれらの使用
WO2020231917A1 (en) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
TWI915558B (zh) 2019-06-14 2026-02-21 美商基利科學股份有限公司 Cot 調節劑及其使用方法
WO2021009332A1 (en) 2019-07-18 2021-01-21 Enyo Pharma Method for decreasing adverse-effects of interferon
US20230105984A1 (en) 2019-12-23 2023-04-06 Svetlana Marukian Compositions and methods for the treatment of liver diseases and disorders
IL293892A (en) 2020-01-15 2022-08-01 Inserm Institut National De La Sant? Et De La Rech M?Dicale Use of fxr agonists for treating an infection by hepatitis d virus
CN120227340A (zh) 2020-03-18 2025-07-01 伊莱利利公司 法尼醇x受体激动剂的制剂
KR20220154801A (ko) * 2020-03-18 2022-11-22 메타크린, 인크. 질환의 치료를 위한 파르네소이드 x 수용체 작용제
JP7664278B2 (ja) 2020-03-18 2025-04-17 オルガノボ，インク． ファルネソイドｘ受容体アゴニストの結晶質形態
US12649738B2 (en) 2020-03-26 2026-06-09 Richter Gedeon Nyrt. 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine derivatives as GABAA α5 receptor modulators
TWI901650B (zh) 2020-03-26 2025-10-21 匈牙利商羅特格登公司 啶及吡啶并〔３，４－ｃ〕嗒衍生物
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
EP4126862B1 (en) 2020-04-02 2025-05-21 Gilead Sciences, Inc. Process for preparing a cot inhibitor compound
US11478533B2 (en) 2020-04-27 2022-10-25 Novo Nordisk A/S Semaglutide for use in medicine
CN114656460B (zh) 2020-12-22 2025-01-10 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.
EP4304711A1 (en) 2021-03-11 2024-01-17 Gilead Sciences, Inc. Glp-1r modulating compounds
ES3061522T3 (en) 2021-03-29 2026-04-06 Gilead Sciences Inc Khk inhibitors
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
TW202345826A (zh) 2021-06-04 2023-12-01 美商基利科學股份有限公司 治療nash之方法
KR20240021883A (ko) 2021-06-16 2024-02-19 셀진 코포레이션 신경변성 질환의 치료를 위한 카르복실산 기를 포함하는 아제티디닐 화합물
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
EP4608506A1 (en) 2022-10-25 2025-09-03 Assia Chemical Industries Ltd. Solid state forms of cilofexor salts
US20260207538A1 (en) 2024-12-20 2026-07-23 Gilead Sciences, Inc. Combinations for liver disease

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
ES2054725T3 (es) 1987-04-21 1994-08-16 Basf Ag Heteroaromatos anulares de cinco miembros de p-fenoxi-fenoximetilo.
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 (fr) 1993-01-29 1994-08-04 Nippon Soda Co., Ltd. Derive heterocyclique
WO1994024095A1 (en) 1993-04-16 1994-10-27 Abbott Laboratories Immunosuppressive agents
IL112721A0 (en) 1994-03-10 1995-05-26 Zeneca Ltd Azole derivatives
EP0804434A1 (en) 1994-08-02 1997-11-05 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
AU1952597A (en) 1996-02-13 1997-09-02 G.D. Searle & Co. Combinations, having immunosuppressive effects, containing cyclooxygenase-2 inhibitor and a leukotriene a4 hydrolase inhibitor
ES2326850T3 (es) 1998-12-23 2009-10-20 Glaxo Group Limited Ensayos para ligandos de receptores nucleares.
ATE283860T1 (de) 1999-06-11 2004-12-15 Allergan Inc Organosiliciumvebindungen mit der fähigkeit zur modulation von im zellkern lokalisierten hormonrezeptoren
US7022725B2 (en) 2000-11-17 2006-04-04 Takeda Pharmaceutical Company Limited Isoxazole derivatives
US20040105885A1 (en) 2001-04-17 2004-06-03 Ping Gao Gelatin capsule exhibiting reduced cross-linking
US20040105883A1 (en) 2001-04-17 2004-06-03 Ping Gao Pharmaceutical dosage form capable of maintaining stable dissolution profile upon storage
US20040131670A1 (en) 2001-04-17 2004-07-08 Ping Gao Pellicle-resistant gelatin capsule
US20040105884A1 (en) 2001-04-17 2004-06-03 Ping Gao Pharmaceutical dosage form comprising a sulfite compound
EP1405636A4 (en) 2001-06-26 2009-04-15 Takeda Pharmaceutical FUNCTIONAL REGULATOR FOR RETINOID RELATIVE RECEPTOR
US20070010562A1 (en) 2001-08-13 2007-01-11 Ulrike Bauer Nr1h4 nuclear receptor binding compounds
DE60131967D1 (de) 2001-08-13 2008-01-31 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
WO2003015777A1 (en) 2001-08-13 2003-02-27 Lion Bioscience Ag Nr1h4 nuclear receptor binding compounds
WO2003080803A2 (en) 2002-03-21 2003-10-02 Smithkline Beecham Corporation Methods of using farnesoid x receptor (fxr) agonists
US7595311B2 (en) 2002-05-24 2009-09-29 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
WO2004014881A2 (en) 2002-08-09 2004-02-19 Astra Zeneca Ab '1,2,4'oxadiazoles as modulators of metabotropic glutamate receptor-5
AU2003264018A1 (en) 2002-08-09 2004-02-25 Astrazeneca Ab Compounds having an activity at metabotropic glutamate receptors
CN1691944A (zh) 2002-08-09 2005-11-02 阿斯利康(瑞典)有限公司 作为代谢型谷氨酸受体－5调节剂的噁二唑
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
JP2006515838A (ja) 2002-11-22 2006-06-08 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
WO2004087076A2 (en) 2003-03-31 2004-10-14 The Rockefeller University 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
CA2564429A1 (en) 2004-05-14 2005-12-01 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
JP2008515992A (ja) 2004-10-13 2008-05-15 ピーティーシー セラピューティクス，インコーポレーテッド 体細胞変異に起因する疾患の阻止／治療用医薬を製造するための規定化合物の使用
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
WO2007070796A1 (en) 2005-12-15 2007-06-21 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
ATE526318T1 (de) 2005-12-19 2011-10-15 Glaxosmithkline Llc Farnesoid-x-rezeptor-agonisten
US7560551B2 (en) 2006-01-23 2009-07-14 Amgen Inc. Aurora kinase modulators and method of use
ES2452031T3 (es) 2006-02-03 2014-03-31 Eli Lilly & Company Compuestos y procedimientos para modular receptores FX
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
EP2007759A4 (en) 2006-04-17 2010-12-22 Neuromed Pharmaceuticals Ltd ISOXAZOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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
WO2007135027A1 (de) 2006-05-24 2007-11-29 Boehringer Ingelheim International Gmbh Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
ES2340221T3 (es) * 2006-05-24 2010-05-31 Eli Lilly And Company Compuestos y procedimientos para modular fxr.
DK2029547T3 (da) 2006-05-24 2010-07-26 Lilly Co Eli FXR-agonister
DK2040713T3 (da) 2006-06-27 2014-09-29 Intercept Pharmaceuticals Inc Galdesyrederivater som fxr-ligander til forebyggelsen eller behandlingen af fxr-medierede sygdomme eller tilstande
AU2007269540B2 (en) 2006-07-05 2013-06-27 Exelixis, Inc. Methods of using IGF1R and Abl kinase modulators
PE20080401A1 (es) 2006-07-07 2008-06-23 Boehringer Ingelheim Int DERIVADOS DE HETEROARIL-FENIL SUSTITUIDOS COMO INHIBIDORES DE B-Raf-QUINASAS
WO2008013660A2 (en) 2006-07-07 2008-01-31 Biostratum, Inc. 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
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
CN101605760B (zh) 2007-02-09 2012-06-20 陶氏益农公司 将某些取代的硫亚胺氧化为杀虫性磺基肟的方法
US7511149B2 (en) 2007-02-09 2009-03-31 Dow Agrosciences Llc Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines
ZA200905012B (en) 2007-02-26 2010-10-27 Dow Agrosciences Llc Process for the preparation of certain substituted sulfimines
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
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
CA2692379A1 (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
EA201000051A1 (ru) 2007-07-13 2010-08-30 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Противовирусные соединения, композиции и способы использования
TW200906823A (en) 2007-07-16 2009-02-16 Lilly Co Eli Compounds and methods for modulating FXR
CN101790374A (zh) 2007-08-01 2010-07-28 H.隆德贝克有限公司 Kcnq钾通道开放剂用于减轻多巴胺能系统受到干扰的障碍或病症的症状或治疗这种障碍或病症的用途
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
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2009143150A2 (en) 2008-05-19 2009-11-26 Burnham Institute For Medical Research Intestinal alkaline phosphatase modulators and uses thereof
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
US8252939B2 (en) 2008-06-23 2012-08-28 Basf Se Sulfoximinamide compounds for combating animal pests
WO2010006096A1 (en) 2008-07-11 2010-01-14 Smithkline Beecham Corporation Processes for the preparation of anti-viral compounds and compositions containing them
JP2012500848A (ja) 2008-08-25 2012-01-12 ダウ グローバル テクノロジーズ エルエルシー イソオキサゾール化合物の製造方法
WO2010033906A2 (en) 2008-09-19 2010-03-25 President And Fellows Of Harvard College Efficient induction of pluripotent stem cells using small molecule compounds
EP2344459B1 (en) 2008-09-25 2013-12-25 F. Hoffmann-La Roche AG 2,3-substituted indazole or 4,5,6,7-tetrahydro-indazoles as fxr modulators against dyslipidemia and related diseases
MX2011002793A (es) 2008-09-25 2011-04-05 Hoffmann La Roche Derivados de 3-amino-indazol o de 3-amino-4,5,6,7-tetrahidro-indaz ol.
JP2012503654A (ja) 2008-09-26 2012-02-09 ワイス・エルエルシー １，２，３，６−テトラヒドロアゼピノ［４，５−ｂ］インドール−５−カルボキシレート核内受容体阻害剤
EA022417B1 (ru) 2008-10-21 2015-12-30 Саймабэй Терапевтикс, Инк. Арильные агонисты рецептора gpr120 и их применение
JP5679997B2 (ja) 2009-02-04 2015-03-04 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 １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
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
US8883832B2 (en) 2009-07-06 2014-11-11 Aerpio Therapeutics Inc. Compounds, compositions, and methods for preventing metastasis of cancer cells
ES2461618T3 (es) 2009-07-06 2014-05-20 Basf Se Compuestos de piridacina para el control de plagas de invertebrados
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
KR20120081119A (ko) 2009-09-04 2012-07-18 잘리커스 파마슈티컬즈 리미티드 통증 및 간질 치료를 위한 치환된 헤테로고리 유도체
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
CA2791738C (en) 2010-03-01 2020-06-09 Gtx, Inc. Aryl imidazolyl compounds for the treatment of cancer
US20130231348A1 (en) 2010-06-09 2013-09-05 Afraxis, Inc. 8-(HETEROARYLMETHYL)PYRIDO[2,3-d]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS
WO2012058531A2 (en) 2010-10-29 2012-05-03 North Carolina State University Modulation of response regulators by imidazole derivatives
TWI408128B (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
JP2014500319A (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
WO2012087520A1 (en) 2010-12-20 2012-06-28 Irm Llc 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
ES2822375T3 (es) 2012-06-19 2021-04-30 Intercept Pharmaceuticals Inc Preparación de la forma no cristalina del ácido obeticólico
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
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
MX377523B (es) 2013-09-11 2025-03-10 Inst Nat Sante Rech Med Metodos y composiciones farmaceuticas para el tratamiento de la infeccion por el virus de la hepatitis b.
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
SG11201603026PA (en) 2013-11-05 2016-05-30 Novartis Ag Compositions and methods for modulating farnesoid x receptors
WO2015116856A2 (en) 2014-01-29 2015-08-06 City Of Hope Farnesoid x receptor antagonists
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
CA2942403A1 (en) 2014-03-13 2015-09-17 Salk Institute For Biological Studies Fxr agonists and methods for making and using
US9879000B2 (en) 2014-04-14 2018-01-30 Grünenthal GmbH Heteroaryl substituted heterocyclyl sulfones
WO2015162538A1 (en) 2014-04-21 2015-10-29 Lupin Limited Heterocyclic compounds as calcium sensing receptor modulators for the treatment of hyperparathyroidism, chronic renal failure and chronic kidney disease
WO2015162244A1 (en) 2014-04-25 2015-10-29 Basf Se N-acylamidine compounds
WO2015165960A1 (en) 2014-04-30 2015-11-05 Basf Se N-acylamidine compounds
SI3626725T1 (sl) 2014-05-29 2023-04-28 Bar Pharmaceuticals S.R.L. Derivati holana za uporabo pri zdravljenju in/ali preprečevanju bolezni, posredovanih s FXR in TGR5/GPBAR1
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
BR112017009657A2 (pt) 2014-11-06 2018-01-23 Enanta Pharmaceuticals, Inc análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos
CA2968434A1 (en) 2014-11-21 2016-05-26 Akarna Therapeutics, Ltd. Fused bicyclic compounds for the treatment of disease
WO2016086115A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof
RU2017121457A (ru) 2014-11-26 2018-12-26 Энанта Фармасьютикалс, Инк. Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения
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
EP3034501A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Hydroxy containing FXR (NR1H4) modulating compounds
EP3034499A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
SG11201704340VA (en) 2014-12-18 2017-07-28 Novartis Ag Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases
MX2017008844A (es) 2015-01-09 2018-03-14 Gilead Apollo Llc Terapia de combinacion con inhibidor de acetil-coa carboxilasa (acc) para el tratamiento de enfermedad de higado graso no alcoholico.
ES2907461T3 (es) 2015-01-20 2022-04-25 Boehringer Ingelheim Animal Health Usa Inc Compuestos antihelmínticos, composiciones y procedimientos de uso de los mismos
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
WO2017011466A1 (en) 2015-07-13 2017-01-19 Zwiebel Laurence J Thermal volatilization of orco agonists
JP6869231B2 (ja) 2015-09-11 2021-05-12 プロパジェニクス インコーポレイテッド ｅｘ ｖｉｖｏでの上皮細胞の増殖
AR106948A1 (es) 2015-12-04 2018-03-07 Bristol Myers Squibb Co Agonistas del receptor de apelina y método 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
US10080743B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10080742B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10080741B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
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
US10144729B2 (en) 2016-05-18 2018-12-04 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
KR102444366B1 (ko) 2016-06-03 2022-09-19 케모센트릭스, 인크. 간 섬유화 치료 방법
NZ748641A (en) 2016-06-13 2020-04-24 Gilead Sciences Inc Fxr (nr1h4) modulating compounds
CA2968836C (en) 2016-06-13 2025-09-02 Gilead Sciences, Inc. FXR MODULATING COMPOUNDS (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
CN116854681B (zh) 2016-08-23 2026-05-26 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
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
WO2018060075A1 (en) 2016-09-29 2018-04-05 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
CA3039124A1 (en) 2016-10-04 2018-04-12 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
CA3152584C (en) 2016-11-10 2024-02-13 Galmed Research And Development Ltd. Treatment for fibrosis
CA3042398A1 (en) 2016-11-11 2018-05-17 Gilead Sciences, Inc. Methods of treating liver disease
CN106588804B (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

Also Published As

Publication number Publication date
EA201391674A1 (ru) 2014-08-29
EP2731676B1 (en) 2016-02-03
AU2012283387B2 (en) 2016-09-08
CN107252424A (zh) 2017-10-17
TWI439455B (zh) 2014-06-01
EP3246070B1 (en) 2024-03-20
EP4400503B1 (en) 2026-05-20
EP3246070A1 (en) 2017-11-22
PL2731676T3 (pl) 2016-08-31
US9820979B2 (en) 2017-11-21
CA2839357A1 (en) 2013-01-17
ES2978166T3 (es) 2024-09-06
WO2013007387A1 (en) 2013-01-17
KR101722410B1 (ko) 2017-04-03
TW201302719A (zh) 2013-01-16
EP4400503C0 (en) 2026-05-20
US10220027B2 (en) 2019-03-05
ES2632492T3 (es) 2017-09-13
KR101934335B1 (ko) 2019-01-02
DK3246070T3 (da) 2024-04-02
PL2987532T3 (pl) 2017-10-31
US20150342930A1 (en) 2015-12-03
AU2012283387A1 (en) 2014-01-09
UY34196A (es) 2013-01-31
SMT201600169B (it) 2016-07-01
CY1117453T1 (el) 2017-04-26
HRP20160442T1 (hr) 2016-05-20
EP4400503A2 (en) 2024-07-17
AU2018203613A1 (en) 2018-06-14
EP4400503A3 (en) 2024-10-23
AU2019261667B2 (en) 2021-03-11
AU2016265993A1 (en) 2016-12-15
DK2731676T3 (en) 2016-05-02
EP2545964A1 (en) 2013-01-16
CN107252424B (zh) 2020-03-27
CN103702719A (zh) 2014-04-02
ES2569718T3 (es) 2016-05-12
US20190142814A1 (en) 2019-05-16
KR101859533B1 (ko) 2018-05-18
PH12014500124A1 (en) 2015-09-23
AU2018203613B2 (en) 2019-08-08
HK1221680A1 (en) 2017-06-09
EA024843B1 (ru) 2016-10-31
AU2012283387C1 (en) 2020-03-12
PT2987532T (pt) 2017-07-13
US20180200243A1 (en) 2018-07-19
CA2839357C (en) 2017-10-24
NZ620177A (en) 2015-10-30
LT3246070T (lt) 2024-04-25
MX368371B (es) 2019-09-30
IL229944A (en) 2017-07-31
KR20170007543A (ko) 2017-01-18
HUE066734T2 (hu) 2024-09-28
MX2019011629A (es) 2019-12-05
NZ710770A (en) 2017-02-24
BR112014000260A2 (pt) 2017-03-01
US10485795B2 (en) 2019-11-26
RS54786B1 (sr) 2016-10-31
JP2017014249A (ja) 2017-01-19
MX2014000534A (es) 2014-05-13
AU2019261667A1 (en) 2019-11-28
AR087127A1 (es) 2014-02-12
US9139539B2 (en) 2015-09-22
KR20140051932A (ko) 2014-05-02
BR112014000260B1 (pt) 2020-08-11
SI2731676T1 (sl) 2016-06-30
EP2731676A1 (en) 2014-05-21
US20170143684A1 (en) 2017-05-25
BR122019026062B1 (pt) 2020-12-15
MY161158A (en) 2017-04-14
JP5986633B2 (ja) 2016-09-06
KR20180053771A (ko) 2018-05-23
HK1192181A1 (zh) 2014-08-15
PL3246070T3 (pl) 2024-08-05
SI3246070T1 (sl) 2024-05-31
EP2987532B1 (en) 2017-04-12
SI2987532T1 (sl) 2017-07-31
PT3246070T (pt) 2024-05-15
FI3246070T3 (fi) 2024-04-18
BR122020008872B1 (pt) 2022-04-12
US20140221659A1 (en) 2014-08-07
US9539244B2 (en) 2017-01-10
KR101766323B1 (ko) 2017-08-08
EP2987532A1 (en) 2016-02-24
AU2016265993B2 (en) 2018-03-15
ZA201309521B (en) 2014-08-27
CN103702719B (zh) 2017-09-08
KR20170093258A (ko) 2017-08-14
JP6321097B2 (ja) 2018-05-09
HRP20240422T1 (hr) 2024-06-21
HUE027931T2 (en) 2016-11-28
EP4793273A2 (en) 2026-08-19
JP2014520823A (ja) 2014-08-25

Similar Documents

Publication Publication Date Title
HRP20160442T1 (hr) Novi spojevi koji moduliraju fxr (nr1h4)
JP2014520823A5 (me)
ME02047B (me) Nova jedinjenja koja se vezuju za fxr (nr1 h4) i moduliraju njegovu aktivnost
HRP20191561T1 (hr) Spojevi za modulaciju fxr (nr1h4)
HRP20240265T1 (hr) Spoj izoksazola kao fxr agonist i farmaceutski pripravci koji ga sadrže
JP6452821B2 (ja) 新規なｆｘｒ（ｎｒ１ｈ４）モジュレート化合物
CN114728168A (zh) 三唑氨基甲酸酯吡啶基磺酰胺作为lpa受体拮抗剂及其用途
ES2538655T3 (es) 3-Amino-piridinas como agonistas de GPBAR1
JP2023538408A5 (me)
HRP20241656T1 (hr) Derivat nitrila koji djeluje kao inhibitor dipeptidil peptidaze 1 i njegova upotreba
HRP20171258T1 (hr) Acilamino-supstituirani kondenzirani derivati ciklopentankarboksilne kiseline i njihova upotreba kao farmaceutski proizvodi
CN112955448A (zh) 芳环或芳杂环类化合物及其制备方法和医药用途
CA2637768C (en) Benzamide and heteroarene derivatives
AU2017284160A1 (en) FXR (NR1H4) modulating compounds
CA2716352A1 (en) Conformationally constrained carboxylic acid derivatives useful for treating metabolic disorders
JP2019521977A (ja) Ｆｘｒ（ｎｒ１ｈ４）調節化合物
JP2016517432A5 (me)
JP2015517579A5 (me)
KR102796877B1 (ko) 신규 ep4 길항제의 합성 및 암과 염증에서의 이의 용도
JP2013501031A5 (me)
WO2013040790A1 (en) Substituted pyrimidines
KR20220068224A (ko) Perk 억제 화합물
KR20190112009A (ko) Ror감마 조절제 및 이의 용도
WO2013043624A1 (en) Substituted pyrimidines
CN116615193A (zh) 作为选择性fabp5抑制剂的吐昔酸单酯衍生物和药物组合物及其用途