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
Links
- 150000001875 compounds Chemical class 0.000 title claims 15
- 102100038495 Bile acid receptor Human genes 0.000 title claims 4
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 title claims 4
- 230000000694 effects Effects 0.000 title claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 18
- 201000010099 disease Diseases 0.000 claims 12
- 210000004185 liver Anatomy 0.000 claims 8
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 230000001684 chronic effect Effects 0.000 claims 6
- 208000019425 cirrhosis of liver Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 230000001587 cholestatic effect Effects 0.000 claims 4
- 206010012601 diabetes mellitus Diseases 0.000 claims 4
- 230000003176 fibrotic effect Effects 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 230000003463 hyperproliferative effect Effects 0.000 claims 4
- 150000002632 lipids Chemical group 0.000 claims 4
- 230000003211 malignant effect Effects 0.000 claims 4
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 4
- 230000000414 obstructive effect Effects 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 208000007788 Acute Liver Failure Diseases 0.000 claims 2
- 206010000804 Acute hepatic failure Diseases 0.000 claims 2
- 206010052747 Adenocarcinoma pancreas Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000023514 Barrett esophagus Diseases 0.000 claims 2
- 208000023665 Barrett oesophagus Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010048832 Colon adenoma Diseases 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 208000004930 Fatty Liver Diseases 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 206010019663 Hepatic failure Diseases 0.000 claims 2
- 206010019708 Hepatic steatosis Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 102000004895 Lipoproteins Human genes 0.000 claims 2
- 108090001030 Lipoproteins Proteins 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 238000009825 accumulation Methods 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 231100000836 acute liver failure Toxicity 0.000 claims 2
- 206010000891 acute myocardial infarction Diseases 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 208000037976 chronic inflammation Diseases 0.000 claims 2
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 2
- 230000007882 cirrhosis Effects 0.000 claims 2
- 201000010897 colon adenocarcinoma Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 2
- 208000006454 hepatitis Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 208000028867 ischemia Diseases 0.000 claims 2
- 231100000835 liver failure Toxicity 0.000 claims 2
- 208000007903 liver failure Diseases 0.000 claims 2
- 230000007774 longterm Effects 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 230000001613 neoplastic effect Effects 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000015768 polyposis Diseases 0.000 claims 2
- 230000002206 pro-fibrotic effect Effects 0.000 claims 2
- 238000011321 prophylaxis Methods 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 238000002271 resection Methods 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 150000003626 triacylglycerols Chemical class 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- -1 SO2NR7R8 Chemical group 0.000 claims 1
- 229910006069 SO3H Inorganic materials 0.000 claims 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (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)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (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.
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| EP12735100.5A EP2731676B1 (en) | 2011-07-13 | 2012-07-12 | Novel fxr (nr1h4) modulating compounds |
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Families Citing this family (90)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI598347B (zh) | 2009-07-13 | 2017-09-11 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| 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 |
| BR112016005507B1 (pt) | 2013-09-11 | 2023-02-07 | Centre National De La Recherche Scientifique (Cnrs) | Uso de um agonista do receptor farnesoide x (fxr) |
| KR20190035960A (ko) | 2014-09-24 | 2019-04-03 | 길리애드 사이언시즈, 인코포레이티드 | 간 질환의 치료 방법 |
| 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 |
| JP2017537960A (ja) * | 2014-12-18 | 2017-12-21 | ノバルティス アーゲー | 肝疾患および胃腸疾患の治療に使用するためのｆｘｒアゴニストとしてのアザビシクロオクタン誘導体 |
| TWI749934B (zh) | 2014-12-23 | 2021-12-11 | 美商基利科學股份有限公司 | 製備2-氟-4-甲基-5-(4-環丙基-1h-咪唑-1-基)苯甲酸之方法 |
| MA41252A (fr) * | 2014-12-23 | 2017-10-31 | Gilead Sciences Inc | Formes solides d'un inhibiteur d'ask 1 |
| 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 |
| SMT202100593T1 (it) | 2015-03-31 | 2021-11-12 | Enanta Pharm Inc | Derivati degli acidi biliari come agonisti di fxr/tgr5 e metodi per il loro uso |
| HRP20190853T1 (hr) | 2015-07-06 | 2019-06-28 | Gilead Sciences, Inc. | Cot modulatori i postupci za njihovu upotrebu |
| 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 |
| CA3016081A1 (en) | 2016-03-04 | 2017-09-08 | Gilead Sciences, Inc. | Compositions and combinations of autotaxin inhibitors |
| CA3019003A1 (en) | 2016-04-08 | 2017-10-12 | Gilead Sciences, Inc. | Compositions and methods for treating cancer, inflammatory diseases and autoimmune diseases |
| US10080742B2 (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 |
| WO2017189663A1 (en) * | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| WO2017201150A1 (en) * | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| US10138228B2 (en) | 2016-05-18 | 2018-11-27 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use therof |
| US10149835B2 (en) | 2016-05-18 | 2018-12-11 | Elmore Patent Law Group, P.C. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| CA2968836C (en) * | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| AR108711A1 (es) * | 2016-06-13 | 2018-09-19 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4) |
| SG11201810600WA (en) * | 2016-06-13 | 2018-12-28 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| 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 |
| 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 |
| US10597391B2 (en) | 2016-10-26 | 2020-03-24 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof |
| AU2017356160A1 (en) * | 2016-11-11 | 2019-05-23 | 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 |
| NZ756329A (en) | 2017-02-21 | 2025-09-26 | 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 |
| EP4122464B1 (en) * | 2017-03-28 | 2024-05-15 | Gilead Sciences, Inc. | Therapeutic combinations for treating liver diseases |
| CN110944635A (zh) | 2017-03-30 | 2020-03-31 | 国家医疗保健研究所 | 用于减少附加体病毒的持久性和表达的方法和药物组合物 |
| AU2018249950B2 (en) | 2017-04-07 | 2023-09-21 | Enanta Pharmaceuticals, Inc. | Process for preparation of sulfonyl carbamate bile acid derivatives |
| US10988449B2 (en) | 2017-04-12 | 2021-04-27 | Il Dong Pharmaceutical Co., Ltd. | Isoxazole derivatives as nuclear receptor agonists and uses thereof |
| AU2018250614A1 (en) * | 2017-04-12 | 2019-10-17 | Gilead Sciences, Inc. | Methods of treating liver disease |
| WO2018231851A1 (en) | 2017-06-13 | 2018-12-20 | Gilead Sciences, Inc. | Methods of treating liver fibrosis |
| TWI814744B (zh) | 2017-10-06 | 2023-09-11 | 美商基利科學股份有限公司 | 包含acc抑制劑之組合療法 |
| ES2944657T3 (es) | 2017-11-01 | 2023-06-23 | Bristol Myers Squibb Co | Compuestos de alqueno como moduladores del receptor farnesoide X |
| AR113820A1 (es) | 2017-11-01 | 2020-06-17 | Bristol Myers Squibb Co | Compuestos bicíclicos en puente como moduladores del receptor farnesoide x |
| BR112020008157A2 (pt) | 2017-11-01 | 2020-10-06 | Bristol-Myers Squibb Company | compostos espirocíclicos como moduladores do receptor farnesoide x |
| EA202091084A1 (ru) | 2017-11-01 | 2020-08-13 | Бристол-Маерс Сквибб Компани | Алкеновые спироциклические соединения как модуляторы фарнезоидных x-рецепторов |
| JP7264905B2 (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多環化合物 |
| ES2986647T3 (es) | 2017-11-13 | 2024-11-12 | Gilead Sciences Inc | Método de estadificación de la fibrosis hepática en pacientes con EHNA |
| 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 |
| PL3833434T3 (pl) * | 2018-08-08 | 2022-03-07 | Inorbit Therapeutics Ab | Związki przydatne w modulowaniu receptora farnezoidalnego x oraz sposoby jego wytwarzania i stosowania |
| 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 |
| PL3852748T3 (pl) | 2018-09-18 | 2025-12-01 | Eli Lilly And Company | Agoniści receptora farnezoidowego x i ich zastosowanie |
| 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) |
| US12479816B2 (en) | 2019-02-08 | 2025-11-25 | University of Pittsburgh—of the Commonwealth System of Higher Education | 20-HETE formation inhibitors |
| SG11202108798XA (en) | 2019-02-15 | 2021-09-29 | Bristol Myers Squibb Co | 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 |
| JP7550777B2 (ja) | 2019-02-15 | 2024-09-13 | 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 |
| KR102905880B1 (ko) | 2019-02-15 | 2025-12-29 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 치환된 비시클릭 화합물 |
| WO2020172075A1 (en) * | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| EP3937908A1 (en) * | 2019-03-11 | 2022-01-19 | Gilead Sciences, Inc. | Formulations of a compound and uses thereof |
| WO2020231917A1 (en) | 2019-05-13 | 2020-11-19 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| TWI770527B (zh) | 2019-06-14 | 2022-07-11 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| EP3999101A1 (en) | 2019-07-18 | 2022-05-25 | 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 |
| 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 |
| AU2021240001A1 (en) * | 2020-03-18 | 2022-10-13 | Eli Lilly And Company | Farnesoid X receptor agonists for the treatment of disease |
| US12545660B2 (en) | 2020-03-18 | 2026-02-10 | Eli Lilly And Company | Crystalline forms of a farnesoid X receptor agonist |
| CN120938936A (zh) | 2020-03-18 | 2025-11-14 | 伊莱利利公司 | 法尼醇x受体激动剂的制剂 |
| EP4126858A1 (en) | 2020-03-26 | 2023-02-08 | Richter Gedeon Nyrt. | Dihydro-2-pyrrolo[3,4-c]pyridine derivatives as gabaa a5 receptor modulators |
| US11655237B2 (en) | 2020-03-30 | 2023-05-23 | Gilead Sciences, Inc. | Solid forms of a Cot inhibitor compound |
| AU2021245924B2 (en) | 2020-04-02 | 2024-02-29 | 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 |
| CN117202905A (zh) | 2021-01-14 | 2023-12-08 | 埃尼奥制药公司 | Fxr激动剂和ifn用于治疗hbv感染的协同效果 |
| WO2022192428A1 (en) | 2021-03-11 | 2022-09-15 | Gilead Sciences, Inc. | Glp-1r modulating compounds |
| EP4313967B1 (en) | 2021-03-29 | 2025-11-12 | Gilead Sciences, Inc. | Khk inhibitors |
| US20240216364A1 (en) | 2021-04-28 | 2024-07-04 | Enyo Pharma | Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment |
| 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 |
| BR112023023420A2 (pt) | 2021-06-16 | 2024-01-30 | Celgene Corp | Compostos de azetidinila compreendendo um grupo ácido carboxílico para o tratamento de doenças neurodegenerativas |
| 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)
| 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 |
| JPH10503768A (ja) | 1994-08-02 | 1998-04-07 | メルク シヤープ エンド ドーム リミテツド | アゼチジン、ピロリジンおよびピペリジン誘導体 |
| 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 |
| ATE223732T1 (de) | 1996-02-13 | 2002-09-15 | Searle & Co | Arzneimittelkombinationen mit immunosuppressiven wirkungen welche cyclooxygenase-2 inhibitoren und leukotrien lta4 hydrase-inhibitoren enthalten |
| WO2000037077A1 (en) | 1998-12-23 | 2000-06-29 | Glaxo Group Limited | Assays for ligands for nuclear receptors |
| AU774538B2 (en) | 1999-06-11 | 2004-07-01 | Allergan, Inc. | Organosilyl compounds having nuclear hormone receptor modulating activity |
| EP1340749A4 (en) | 2000-11-17 | 2007-09-05 | Takeda Pharmaceutical | ISOXAZOLE DERIVATIVES |
| US20040105883A1 (en) | 2001-04-17 | 2004-06-03 | Ping Gao | Pharmaceutical dosage form capable of maintaining stable dissolution profile upon storage |
| US20040105884A1 (en) | 2001-04-17 | 2004-06-03 | Ping Gao | Pharmaceutical dosage form comprising a sulfite compound |
| US20040131670A1 (en) | 2001-04-17 | 2004-07-08 | Ping Gao | Pellicle-resistant gelatin capsule |
| US20040105885A1 (en) | 2001-04-17 | 2004-06-03 | Ping Gao | Gelatin capsule exhibiting reduced cross-linking |
| WO2003000249A1 (en) | 2001-06-26 | 2003-01-03 | Takeda Chemical Industries, Ltd. | Function regulator for retinoid relative receptor |
| EP1423113A4 (en) | 2001-08-13 | 2007-04-18 | Phenex Pharmaceuticals Ag | NR1H4 NUCLEAR RECEPTOR BINDING COMPOUNDS |
| WO2003016280A1 (en) | 2001-08-13 | 2003-02-27 | Lion Bioscience Ag | Nr1h4 nuclear receptor binding compounds |
| ATE381542T1 (de) | 2001-08-13 | 2008-01-15 | Phenex Pharmaceuticals Ag | Nr1h4-kern-rezeptor-bindende verbindungen |
| 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 |
| TWI341314B (en) | 2002-08-09 | 2011-05-01 | Astrazeneca Ab | New compounds |
| AU2003264018A1 (en) | 2002-08-09 | 2004-02-25 | Astrazeneca Ab | Compounds having an activity at metabotropic glutamate receptors |
| US20040132726A1 (en) | 2002-08-09 | 2004-07-08 | Astrazeneca Ab And Nps Pharmaceuticals, Inc. | 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 |
| 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 |
| 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 |
| EP1745027A4 (en) | 2004-05-14 | 2009-06-03 | 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 |
| EP2301536B1 (en) | 2004-10-13 | 2014-04-09 | PTC Therapeutics, Inc. | Compounds and their use for treating nonsense-related diseases |
| JP2008137894A (ja) | 2005-03-22 | 2008-06-19 | Nippon Kayaku Co Ltd | 新規なアセチレン誘導体 |
| US8952176B2 (en) | 2005-06-07 | 2015-02-10 | Shionogi & Co., Ltd. | Heterocyclic compound having type I 11 β hydroxysteroid dehydrogenase inhibitory activity |
| US20090203577A1 (en) | 2005-12-15 | 2009-08-13 | Exelixis, Inc. | Azepinoindole Derivatives As Pharmaceutical Agents |
| WO2007076260A2 (en) | 2005-12-19 | 2007-07-05 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
| 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 |
| EP1987051A2 (en) | 2006-02-14 | 2008-11-05 | Intercept Pharmaceuticals, Inc. | Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions |
| CA2643924A1 (en) | 2006-04-17 | 2007-10-25 | 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 |
| AU2007267606A1 (en) * | 2006-05-24 | 2007-12-06 | Eli Lilly And Company | FXR agonists |
| TW200812982A (en) * | 2006-05-24 | 2008-03-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
| ATE549338T1 (de) | 2006-05-24 | 2012-03-15 | Boehringer Ingelheim Int | Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind |
| EP2040713B1 (en) | 2006-06-27 | 2014-06-18 | Intercept Pharmaceuticals Inc. | Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated deseases or conditions |
| CA2656290A1 (en) | 2006-07-05 | 2008-01-10 | Exelixis, Inc. | Methods of using igf1r and abl kinase modulators |
| WO2008013660A2 (en) | 2006-07-07 | 2008-01-31 | Biostratum, Inc. | Inhibitors of advanced glycation end products |
| CA2654898A1 (en) | 2006-07-07 | 2008-10-01 | Boehringer Ingelheim International Gmbh | New chemical compounds |
| 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 |
| ES2561355T3 (es) | 2007-02-09 | 2016-02-25 | Dow Agrosciences Llc | Procedimiento para la oxidación de ciertas sulfiliminas substituidas a sulfoximinas insecticidas |
| 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 |
| WO2008157270A1 (en) | 2007-06-13 | 2008-12-24 | Smithkline Beecham Corporation | 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 |
| MX2009013946A (es) | 2007-07-02 | 2010-03-10 | Glaxosmithkline Llc | Agonistas del receptor de farnesoide x. |
| US20100240657A1 (en) | 2007-07-02 | 2010-09-23 | Boehringer Ingelheim International Gmbh | Chemical compounds |
| 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 |
| AU2008281112A1 (en) | 2007-08-01 | 2009-02-05 | H. Lundbeck A/S | Use of KCNQ potassium channel openers for reducing symptoms of or treating disorders or conditions wherein the dopaminergic system is disrupted |
| 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 |
| CA2724232A1 (en) | 2008-05-13 | 2009-11-19 | 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 |
| CA2727389A1 (en) | 2008-06-10 | 2009-12-17 | Prabha N. Ibrahim | 5h-pyrrolo [2,3-b] pyrazine derivatives for kinase modulation, and indications therefor |
| 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 |
| US8044214B2 (en) | 2008-08-25 | 2011-10-25 | Angus Chemical Company | Process for preparing isoxazole compounds |
| WO2010033906A2 (en) | 2008-09-19 | 2010-03-25 | President And Fellows Of Harvard College | Efficient induction of pluripotent stem cells using small molecule compounds |
| BRPI0919057A2 (pt) | 2008-09-25 | 2018-01-09 | Hoffmann La Roche | compostos de indazol ou derivados, processo para a sua preparação, composições farmacêuticas que os compreendem, método para o tratamento ou profilaxia de enfermidades que são afetadas por moduladores de fxr, e uso dos compostos |
| WO2010034657A1 (en) | 2008-09-25 | 2010-04-01 | F. Hoffmann-La Roche Ag | 3-amino-indazole or 3-amino-4,5,6,7-tetrahydro-indazole derivatives |
| CA2736880A1 (en) | 2008-09-26 | 2010-04-01 | Wyeth Llc | 1,2,3,6-tetrahydroazepino[4,5-b]indole-5-carboxylate nuclear receptor inhibitors |
| EP2690095A1 (en) | 2008-10-21 | 2014-01-29 | Camabay Therapeutics, Inc. | Aryl gpr120 receptor agonists and uses thereof |
| EP2393807B1 (en) | 2009-02-04 | 2013-08-14 | Boehringer Ingelheim International GmbH | Cyclic inhibitors of 11 -hydroxysteroid dehydrogenase 1 |
| KR20100092909A (ko) | 2009-02-13 | 2010-08-23 | 주식회사 엘지생명과학 | 잔틴 옥시다제 저해제로서 효과적인 신규 화합물, 그 제조방법 및 그를 함유하는 약제학적 조성물 |
| FR2943059A1 (fr) | 2009-03-16 | 2010-09-17 | Sanofi Aventis | Derives de n-°6-aza-bicyclo°3.2.1!oct-5-yl)-aryl-methyl!- heterobenzamide,leur preparation et leur application en therapeutique |
| EP2451808B1 (en) | 2009-07-06 | 2014-03-26 | Basf Se | Pyridazine compounds for controlling invertebrate pests |
| 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 |
| JP5879273B2 (ja) | 2010-03-01 | 2016-03-08 | ジーティーエックス・インコーポレイテッド | 癌を処置するための化合物 |
| WO2011156640A2 (en) | 2010-06-09 | 2011-12-15 | Afraxis, Inc. | 8-(HETEROARYLMETHYL)PYRIDO[2,3-d]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS |
| WO2012058531A2 (en) | 2010-10-29 | 2012-05-03 | North Carolina State University | Modulation of response regulators by imidazole derivatives |
| TWI408128B (zh) | 2010-12-03 | 2013-09-11 | Nat Univ Tsing Hua | 間-三聯苯衍生物及其在有機發光二極體之應用 |
| 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 |
| EP2655368A1 (en) | 2010-12-20 | 2013-10-30 | Irm Llc | Compositions and methods for modulating farnesoid x receptors |
| 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 |
| EA201990211A1 (ru) | 2012-06-19 | 2019-06-28 | Интерсепт Фармасьютикалз, Инк. | Получение, применение и твердые формы обетихолевой кислоты |
| 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 |
| ES2936638T3 (es) | 2013-05-14 | 2023-03-21 | Intercept Pharmaceuticals Inc | Derivados sustituidos con 11-Hidroxil-6 de ácidos biliares y conjugados de aminoácidos de los mismos como moduladores del receptor X farnesoide |
| JP6556129B2 (ja) | 2013-08-01 | 2019-08-07 | アメリカ合衆国 | ファルネソイドｘ受容体の阻害剤及び医薬としての使用 |
| BR112016005507B1 (pt) | 2013-09-11 | 2023-02-07 | Centre National De La Recherche Scientifique (Cnrs) | Uso de um agonista do receptor farnesoide x (fxr) |
| US20150082981A1 (en) | 2013-09-20 | 2015-03-26 | E I Du Pont De Nemours And Company | Capture of trifluoromethane using ionic liquids |
| CN104513213A (zh) | 2013-09-28 | 2015-04-15 | 山东亨利医药科技有限责任公司 | Fxr激动剂 |
| US20150119345A1 (en) | 2013-10-29 | 2015-04-30 | Lumena Pharmaceuticals, Inc. | Bile acid recycling inhibitors for treatment of gastrointestinal infections |
| EA030430B1 (ru) | 2013-11-05 | 2018-08-31 | Новартис Аг | Композиции и способы модуляции фарнезоидных х-рецепторов |
| 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 |
| AR100073A1 (es) | 2014-04-14 | 2016-09-07 | Gruenenthal Gmbh | Sulfonas heterocíclicas sustituidas con heteroarilos |
| 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 |
| AU2015265893B2 (en) | 2014-05-29 | 2020-11-12 | Bar Pharmaceuticals S.R.L. | Cholane derivatives for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases |
| 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 |
| EP3214151B1 (en) | 2014-10-27 | 2020-10-14 | LG Chem, Ltd. | Organic electroluminescence device |
| HK1243930A1 (zh) | 2014-11-06 | 2018-07-27 | 英安塔制药有限公司 | 作爲fxr/tgr5激动剂的胆汁酸类似物和其使用方法 |
| CN107207513B (zh) | 2014-11-21 | 2020-07-28 | 阿卡纳治疗学有限公司 | 用于治疗疾病的稠合双环化合物 |
| WO2016086115A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof |
| WO2016086134A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| US10519191B2 (en) | 2014-11-26 | 2019-12-31 | Enanta Pharmaceuticals, Inc. | Bile acid analogs 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 |
| JP2017537960A (ja) | 2014-12-18 | 2017-12-21 | ノバルティス アーゲー | 肝疾患および胃腸疾患の治療に使用するためのｆｘｒアゴニストとしてのアザビシクロオクタン誘導体 |
| EA201791258A1 (ru) | 2015-01-09 | 2017-12-29 | Джилид Аполло, Ллс | Комбинированная терапия с применением ингибитора ацетил-коа-карбоксилазы (acc) для лечения неалкогольной жировой болезни печени |
| CA2973873A1 (en) | 2015-01-20 | 2016-07-28 | Merial, 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 |
| US20180192651A1 (en) | 2015-07-13 | 2018-07-12 | Vanderbilt University | Thermal volatilization of orco agonists |
| EP3347450B1 (en) | 2015-09-11 | 2021-03-17 | Propagenix Inc. | Ex vivo proliferation of epithelial cells |
| CN108473466B (zh) | 2015-12-04 | 2022-04-19 | 百时美施贵宝公司 | 爱帕琳肽受体激动剂及使用方法 |
| 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 |
| AU2017204979B2 (en) | 2016-01-10 | 2020-11-19 | 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 |
| US10080742B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189663A1 (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 |
| US10138228B2 (en) | 2016-05-18 | 2018-11-27 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use therof |
| US10149835B2 (en) | 2016-05-18 | 2018-12-11 | Elmore Patent Law Group, P.C. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017201150A1 (en) | 2016-05-18 | 2017-11-23 | 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 |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| SG11201810600WA (en) | 2016-06-13 | 2018-12-28 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| 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 |
| EP3954684A1 (en) | 2016-08-23 | 2022-02-16 | Ardelyx, Inc. | Process for the preparation of hormone receptor modulators for treating metabolic conditions and disorders |
| 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 |
| 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 |
| IL309558A (en) | 2016-11-10 | 2024-02-01 | Galmed Res And Development Ltd | Fibrosis treatment |
| AU2017356160A1 (en) | 2016-11-11 | 2019-05-23 | 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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