JP2016518429A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016518429A5 JP2016518429A5 JP2016513357A JP2016513357A JP2016518429A5 JP 2016518429 A5 JP2016518429 A5 JP 2016518429A5 JP 2016513357 A JP2016513357 A JP 2016513357A JP 2016513357 A JP2016513357 A JP 2016513357A JP 2016518429 A5 JP2016518429 A5 JP 2016518429A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- amino acid
- item
- compound
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 91
- 150000003839 salts Chemical class 0.000 claims description 46
- 150000001413 amino acids Chemical class 0.000 claims description 44
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 27
- 229910052739 hydrogen Inorganic materials 0.000 claims description 25
- 239000001257 hydrogen Substances 0.000 claims description 25
- 125000000217 alkyl group Chemical group 0.000 claims description 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 13
- 229910052736 halogen Inorganic materials 0.000 claims description 13
- 150000002367 halogens Chemical class 0.000 claims description 13
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 10
- 206010008635 Cholestasis Diseases 0.000 claims description 9
- 230000007870 cholestasis Effects 0.000 claims description 9
- 231100000359 cholestasis Toxicity 0.000 claims description 9
- 210000004185 liver Anatomy 0.000 claims description 9
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 6
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 208000019423 liver disease Diseases 0.000 claims description 6
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 6
- 238000002054 transplantation Methods 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 5
- 230000008929 regeneration Effects 0.000 claims description 5
- 238000011069 regeneration method Methods 0.000 claims description 5
- 206010048215 Xanthomatosis Diseases 0.000 claims description 4
- 230000001580 bacterial effect Effects 0.000 claims description 4
- 230000001684 chronic effect Effects 0.000 claims description 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 208000022309 Alcoholic Liver disease Diseases 0.000 claims description 3
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims description 3
- 206010004637 Bile duct stone Diseases 0.000 claims description 3
- 201000009331 Choledocholithiasis Diseases 0.000 claims description 3
- 206010010356 Congenital anomaly Diseases 0.000 claims description 3
- 208000015872 Gaucher disease Diseases 0.000 claims description 3
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 3
- 208000024815 Granulomatous liver disease Diseases 0.000 claims description 3
- 208000018565 Hemochromatosis Diseases 0.000 claims description 3
- 206010019799 Hepatitis viral Diseases 0.000 claims description 3
- 208000012868 Overgrowth Diseases 0.000 claims description 3
- 206010040047 Sepsis Diseases 0.000 claims description 3
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 3
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 claims description 3
- 230000002490 cerebral effect Effects 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 208000024908 graft versus host disease Diseases 0.000 claims description 3
- 201000002161 intrahepatic cholestasis of pregnancy Diseases 0.000 claims description 3
- 230000036210 malignancy Effects 0.000 claims description 3
- 235000016236 parenteral nutrition Nutrition 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 201000000306 sarcoidosis Diseases 0.000 claims description 3
- 208000010157 sclerosing cholangitis Diseases 0.000 claims description 3
- 210000002435 tendon Anatomy 0.000 claims description 3
- 201000001862 viral hepatitis Diseases 0.000 claims description 3
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 6
- 208000017667 Chronic Disease Diseases 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 238000004581 coalescence Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 44
- 239000012453 solvate Substances 0.000 description 25
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 18
- 201000010099 disease Diseases 0.000 description 16
- 210000004027 cell Anatomy 0.000 description 6
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 6
- 108090000623 proteins and genes Proteins 0.000 description 5
- 206010012601 diabetes mellitus Diseases 0.000 description 4
- 206010016654 Fibrosis Diseases 0.000 description 3
- 208000022559 Inflammatory bowel disease Diseases 0.000 description 3
- 208000012902 Nervous system disease Diseases 0.000 description 3
- 229940121360 farnesoid X receptor (fxr) agonists Drugs 0.000 description 3
- 230000004761 fibrosis Effects 0.000 description 3
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical compound C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 description 2
- IGRCWJPBLWGNPX-UHFFFAOYSA-N 3-(2-chlorophenyl)-n-(4-chlorophenyl)-n,5-dimethyl-1,2-oxazole-4-carboxamide Chemical compound C=1C=C(Cl)C=CC=1N(C)C(=O)C1=C(C)ON=C1C1=CC=CC=C1Cl IGRCWJPBLWGNPX-UHFFFAOYSA-N 0.000 description 2
- 102100038495 Bile acid receptor Human genes 0.000 description 2
- 208000024172 Cardiovascular disease Diseases 0.000 description 2
- 108010081668 Cytochrome P-450 CYP3A Proteins 0.000 description 2
- 102100039205 Cytochrome P450 3A4 Human genes 0.000 description 2
- 102100025353 G-protein coupled bile acid receptor 1 Human genes 0.000 description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- 101000857733 Homo sapiens G-protein coupled bile acid receptor 1 Proteins 0.000 description 2
- 208000035150 Hypercholesterolemia Diseases 0.000 description 2
- 208000031226 Hyperlipidaemia Diseases 0.000 description 2
- 208000025966 Neurological disease Diseases 0.000 description 2
- 208000008589 Obesity Diseases 0.000 description 2
- 230000006907 apoptotic process Effects 0.000 description 2
- 239000003613 bile acid Substances 0.000 description 2
- 201000001883 cholelithiasis Diseases 0.000 description 2
- 208000010643 digestive system disease Diseases 0.000 description 2
- 208000016097 disease of metabolism Diseases 0.000 description 2
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 description 2
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 description 2
- 208000018685 gastrointestinal system disease Diseases 0.000 description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 description 2
- 208000017169 kidney disease Diseases 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
- 208000030159 metabolic disease Diseases 0.000 description 2
- 235000020824 obesity Nutrition 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 2
- -1 APOCII Proteins 0.000 description 1
- 206010002383 Angina Pectoris Diseases 0.000 description 1
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 208000014882 Carotid artery disease Diseases 0.000 description 1
- 206010065559 Cerebral arteriosclerosis Diseases 0.000 description 1
- 206010009900 Colitis ulcerative Diseases 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 1
- 102000012437 Copper-Transporting ATPases Human genes 0.000 description 1
- 208000011231 Crohn disease Diseases 0.000 description 1
- 108010074922 Cytochrome P-450 CYP1A2 Proteins 0.000 description 1
- 108010026925 Cytochrome P-450 CYP2C19 Proteins 0.000 description 1
- 108010000543 Cytochrome P-450 CYP2C9 Proteins 0.000 description 1
- 108010001237 Cytochrome P-450 CYP2D6 Proteins 0.000 description 1
- 108010001202 Cytochrome P-450 CYP2E1 Proteins 0.000 description 1
- 102100026533 Cytochrome P450 1A2 Human genes 0.000 description 1
- 102100029363 Cytochrome P450 2C19 Human genes 0.000 description 1
- 102100029358 Cytochrome P450 2C9 Human genes 0.000 description 1
- 102100021704 Cytochrome P450 2D6 Human genes 0.000 description 1
- 102100024889 Cytochrome P450 2E1 Human genes 0.000 description 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 description 1
- 208000032928 Dyslipidaemia Diseases 0.000 description 1
- 102000009427 Ether-A-Go-Go Potassium Channels Human genes 0.000 description 1
- 102100031734 Fibroblast growth factor 19 Human genes 0.000 description 1
- 206010018367 Glomerulonephritis chronic Diseases 0.000 description 1
- 206010051920 Glomerulonephropathy Diseases 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- 208000002972 Hepatolenticular Degeneration Diseases 0.000 description 1
- 101000846394 Homo sapiens Fibroblast growth factor 19 Proteins 0.000 description 1
- 101000978937 Homo sapiens Nuclear receptor subfamily 0 group B member 2 Proteins 0.000 description 1
- 101001010792 Homo sapiens Transcriptional regulator ERG Proteins 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 206010022489 Insulin Resistance Diseases 0.000 description 1
- 208000017170 Lipid metabolism disease Diseases 0.000 description 1
- 206010025476 Malabsorption Diseases 0.000 description 1
- 208000004155 Malabsorption Syndromes Diseases 0.000 description 1
- 108010093662 Member 11 Subfamily B ATP Binding Cassette Transporter Proteins 0.000 description 1
- 102000001479 Member 11 Subfamily B ATP Binding Cassette Transporter Human genes 0.000 description 1
- 208000001145 Metabolic Syndrome Diseases 0.000 description 1
- 101710202677 Non-specific lipid-transfer protein Proteins 0.000 description 1
- 108020005497 Nuclear hormone receptor Proteins 0.000 description 1
- 102100023172 Nuclear receptor subfamily 0 group B member 2 Human genes 0.000 description 1
- 102100039506 Organic solute transporter subunit alpha Human genes 0.000 description 1
- 102100030111 Organic solute transporter subunit beta Human genes 0.000 description 1
- 108010016731 PPAR gamma Proteins 0.000 description 1
- 102100038825 Peroxisome proliferator-activated receptor gamma Human genes 0.000 description 1
- 108090000472 Phosphoenolpyruvate carboxykinase (ATP) Proteins 0.000 description 1
- 102100034792 Phosphoenolpyruvate carboxykinase [GTP], mitochondrial Human genes 0.000 description 1
- 102100022428 Phospholipid transfer protein Human genes 0.000 description 1
- 108010029485 Protein Isoforms Proteins 0.000 description 1
- 102000001708 Protein Isoforms Human genes 0.000 description 1
- 108091007630 SLC51A1 Proteins 0.000 description 1
- 108091007633 SLC51B Proteins 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 101001082043 Sulfolobus acidocaldarius (strain ATCC 33909 / DSM 639 / JCM 8929 / NBRC 15157 / NCIMB 11770) Translation initiation factor 5A Proteins 0.000 description 1
- 206010048302 Tubulointerstitial nephritis Diseases 0.000 description 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 1
- 102100029785 UDP-glucuronosyltransferase 2B4 Human genes 0.000 description 1
- 101710200334 UDP-glucuronosyltransferase 2B4 Proteins 0.000 description 1
- 201000006704 Ulcerative Colitis Diseases 0.000 description 1
- 208000018839 Wilson disease Diseases 0.000 description 1
- 206010048214 Xanthoma Diseases 0.000 description 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 description 1
- 230000009102 absorption Effects 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 208000011775 arteriosclerosis disease Diseases 0.000 description 1
- 210000000941 bile Anatomy 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 235000012000 cholesterol Nutrition 0.000 description 1
- 231100000850 chronic interstitial nephritis Toxicity 0.000 description 1
- 206010009887 colitis Diseases 0.000 description 1
- 208000029078 coronary artery disease Diseases 0.000 description 1
- 231100000433 cytotoxic Toxicity 0.000 description 1
- 230000001472 cytotoxic effect Effects 0.000 description 1
- 208000033679 diabetic kidney disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 230000002222 downregulating effect Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 208000001130 gallstones Diseases 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 230000013632 homeostatic process Effects 0.000 description 1
- 201000001421 hyperglycemia Diseases 0.000 description 1
- 208000020346 hyperlipoproteinemia Diseases 0.000 description 1
- 230000001631 hypertensive effect Effects 0.000 description 1
- 208000006575 hypertriglyceridemia Diseases 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 201000005851 intracranial arteriosclerosis Diseases 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 230000006372 lipid accumulation Effects 0.000 description 1
- 230000037356 lipid metabolism Effects 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 208000008275 microscopic colitis Diseases 0.000 description 1
- 201000009925 nephrosclerosis Diseases 0.000 description 1
- 102000006255 nuclear receptors Human genes 0.000 description 1
- 108020004017 nuclear receptors Proteins 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 208000030761 polycystic kidney disease Diseases 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000004141 reverse cholesterol transport Effects 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- 229960003080 taurine Drugs 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361823169P | 2013-05-14 | 2013-05-14 | |
| US61/823,169 | 2013-05-14 | ||
| PCT/EP2014/059896 WO2014184271A1 (en) | 2013-05-14 | 2014-05-14 | 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018077654A Division JP2018127481A (ja) | 2013-05-14 | 2018-04-13 | ファルネソイドｘ受容体調節物質としての、胆汁酸の１１−ヒドロキシル誘導体およびそのアミノ酸抱合体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016518429A JP2016518429A (ja) | 2016-06-23 |
| JP2016518429A5 true JP2016518429A5 (https=) | 2017-05-18 |
| JP6326131B2 JP6326131B2 (ja) | 2018-05-16 |
Family
ID=50721801
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016513357A Active JP6326131B2 (ja) | 2013-05-14 | 2014-05-14 | ファルネソイドｘ受容体調節物質としての、胆汁酸の１１−ヒドロキシル誘導体およびそのアミノ酸抱合体 |
| JP2018077654A Withdrawn JP2018127481A (ja) | 2013-05-14 | 2018-04-13 | ファルネソイドｘ受容体調節物質としての、胆汁酸の１１−ヒドロキシル誘導体およびそのアミノ酸抱合体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018077654A Withdrawn JP2018127481A (ja) | 2013-05-14 | 2018-04-13 | ファルネソイドｘ受容体調節物質としての、胆汁酸の１１−ヒドロキシル誘導体およびそのアミノ酸抱合体 |
Country Status (37)
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2002308295B2 (en) | 2001-03-12 | 2007-08-23 | Intercept Pharmaceuticals, Inc. | Steroids as agonists for FXR |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| CA2912139C (en) | 2013-05-14 | 2021-04-20 | Roberto Pellicciari | 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators |
| US10077268B2 (en) | 2014-03-13 | 2018-09-18 | Salk Institute For Biological Studies | FXR agonists and methods for making and using |
| US10301268B2 (en) | 2014-03-13 | 2019-05-28 | The Salk Institute For Biological Studies | Analogs of fexaramine and methods of making and using |
| US10407462B2 (en) | 2014-05-29 | 2019-09-10 | Bar Pharmaceuticals S.R.L. | Cholane derivatives for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases |
| WO2016073767A1 (en) | 2014-11-06 | 2016-05-12 | Enanta Pharmaceuticals, Inc. | Bile acid analogs an fxr/tgr5 agonists and methods of use thereof |
| TWI688571B (zh) | 2014-11-19 | 2020-03-21 | 英商Ｎｚｐ英國有限公司 | 化合物（四） |
| US10131688B2 (en) | 2014-11-19 | 2018-11-20 | NZP UK Limited | 5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal FXR modulators |
| US10538550B2 (en) | 2014-11-19 | 2020-01-21 | NZP UK Limited | 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal FXR modulators |
| KR102526631B1 (ko) | 2014-11-19 | 2023-04-27 | 엔제트피 유케이 리미티드 | 스테로이드 fxr 조절인자를 제조하기 위한 중간체로서의 6-알킬-7-하이드록시-4-엔-3-온 스테로이드 |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| US11578097B2 (en) | 2014-11-26 | 2023-02-14 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof |
| JP2017535570A (ja) | 2014-11-26 | 2017-11-30 | エナンタ ファーマシューティカルズ インコーポレイテッド | Ｆｘｒ／ｔｇｒ５アゴニストとしての胆汁酸類似体およびその使用方法 |
| MA41094A (fr) * | 2014-12-02 | 2017-10-10 | Lilly Co Eli | Procédés de traitement de troubles rénaux |
| CN105348365A (zh) * | 2014-12-03 | 2016-02-24 | 四川百利药业有限责任公司 | 一种胆酸衍生物及其制备方法、药物组合物和用途 |
| CN104523703A (zh) * | 2014-12-24 | 2015-04-22 | 聂飚 | 一种游离脂肪酸转运蛋白小分子抑制物的应用 |
| EA036404B1 (ru) * | 2015-02-06 | 2020-11-06 | Интерсепт Фармасьютикалз, Инк. | Фармацевтические композиции для комбинированной терапии |
| MX2017010376A (es) | 2015-02-11 | 2017-12-20 | Enanta Pharm Inc | Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos. |
| MX2017011399A (es) * | 2015-03-09 | 2018-03-16 | Intercept Pharmaceuticals Inc | Métodos para modular la densidad ósea. |
| US11072630B2 (en) | 2015-03-10 | 2021-07-27 | Metselex, Inc. | Fluorinated and alkylated bile acids |
| JP2018510866A (ja) * | 2015-03-13 | 2018-04-19 | ソーク インスティテュート フォー バイオロジカル スタディーズ | 腸受容体を活性化させるための、ファルネソイドｘ受容体アゴニストでの、成体の潜在性自己免疫性糖尿病の治療 |
| CA2981503C (en) | 2015-03-31 | 2023-09-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| CR20170456A (es) | 2015-04-07 | 2018-06-13 | Intercept Pharmaceuticals Inc | Composiciones farmacéuticas para terapias combinadas |
| WO2016168553A1 (en) * | 2015-04-17 | 2016-10-20 | Concert Pharmaceuticals, Inc. | Deuterated obeticholic acid |
| PE20180690A1 (es) | 2015-04-27 | 2018-04-23 | Intercept Pharmaceuticals Inc | Composiciones de acido obeticolico y metodos de uso |
| CN106478759A (zh) * | 2015-08-31 | 2017-03-08 | 陕西合成药业股份有限公司 | 奥贝胆酸衍生物及其制备方法和用途 |
| KR20180054770A (ko) | 2015-09-21 | 2018-05-24 | 인터셉트 파마슈티컬즈, 인크. | 간 재생 촉진 방법 |
| EP3981779A1 (en) | 2015-10-07 | 2022-04-13 | Intercept Pharmaceuticals, Inc. | Farnesoid x receptor modulators |
| US10875888B2 (en) * | 2016-01-28 | 2020-12-29 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Steroid derivative FXR agonist |
| US10323060B2 (en) | 2016-02-23 | 2019-06-18 | Enanta Pharmaceuticals, Inc. | Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof |
| WO2017147174A1 (en) * | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Heteroaryl containing bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
| WO2017147159A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Deuterated bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| EP3426348B1 (en) | 2016-03-11 | 2021-05-05 | Intercept Pharmaceuticals, Inc. | 3-desoxy derivative and pharmaceutical compositions thereof |
| WO2017180577A1 (en) * | 2016-04-13 | 2017-10-19 | Intercept Pharmaceuticals, Inc. | Methods of treating cancer |
| GB201608777D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Compounds |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences, Inc. | FXR MODULATING COMPOUNDS (NR1H4) |
| NZ748641A (en) | 2016-06-13 | 2020-04-24 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| CA3045023A1 (en) | 2016-11-29 | 2018-06-07 | Enanta Pharmaceuticals, Inc. | Process for preparation of sulfonylurea bile acid derivatives |
| US10472386B2 (en) | 2017-02-14 | 2019-11-12 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR agonists and methods of use thereof |
| 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 |
| KR20190117687A (ko) * | 2017-02-23 | 2019-10-16 | 인터셉트 파마슈티컬즈, 인크. | 담즙산 유도체와 마이크로바이옴의 약학 조성물 및 이의 용도 |
| SI4122464T1 (sl) | 2017-03-28 | 2024-07-31 | Gilead Sciences, Inc. | Terapevtske kombinacije za zdravljenje bolezni jeter |
| CA3058754A1 (en) | 2017-04-07 | 2018-10-11 | Enanta Pharmaceuticals, Inc. | Process for preparation of sulfonyl carbamate bile acid derivatives |
| WO2018226724A1 (en) * | 2017-06-05 | 2018-12-13 | Intercept Pharmaceuticals, Inc. | Treatment and prevention of diabetic eye diseases with a bile acid derivatives |
| JP7224307B2 (ja) * | 2017-06-23 | 2023-02-17 | インターセプト ファーマシューティカルズ， インコーポレイテッド | 胆汁酸誘導体の調製のための方法及び中間体 |
| WO2019023103A1 (en) | 2017-07-24 | 2019-01-31 | Intercept Pharmaceuticals, Inc. | BILIARY ACID DERIVATIVES WITH ISOTOPIC MARKING |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| CN109182451B (zh) * | 2018-08-21 | 2021-06-11 | 四川大学 | 细胞色素cyp3a7酶的新型特异性探针反应及其应用 |
| PT3911647T (pt) | 2019-01-15 | 2024-03-04 | Gilead Sciences Inc | Composto de isoxazole como agonista de fxr e composições farmacêuticas que o contenham |
| JP2022519906A (ja) | 2019-02-19 | 2022-03-25 | ギリアード サイエンシーズ， インコーポレイテッド | Ｆｘｒアゴニストの固体形態 |
| SG11202113155XA (en) | 2019-05-30 | 2021-12-30 | Intercept Pharmaceuticals Inc | Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease |
| EP3999101A1 (en) | 2019-07-18 | 2022-05-25 | ENYO Pharma | Method for decreasing adverse-effects of interferon |
| CN110540955B (zh) * | 2019-08-28 | 2021-09-17 | 北京协同创新研究院 | 一种提高分化细胞中nrob2基因表达量的方法 |
| WO2021144330A1 (en) | 2020-01-15 | 2021-07-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of fxr agonists for treating an infection by hepatitis d virus |
| KR20230154806A (ko) | 2021-01-14 | 2023-11-09 | 엔요 파마 | Hbv 감염 치료를 위한 fxr 작용제 및 ifn의 상승작용효과 |
| CN117320722A (zh) | 2021-04-28 | 2023-12-29 | 埃尼奥制药公司 | 使用fxr激动剂作为联合治疗强烈增强tlr3激动剂的作用 |
| WO2022233398A1 (en) * | 2021-05-04 | 2022-11-10 | Kostner Pharma Gmbh | COMPOUNDS FOR REDUCING LIPOPROTEIN(a) |
| WO2023288123A1 (en) | 2021-07-16 | 2023-01-19 | Interecept Pharmaceuticals, Inc. | Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid |
| WO2025059651A1 (en) * | 2023-09-14 | 2025-03-20 | The Regents Of The University Of California | Bile salt modification to prevent and treat enteric disease |
| WO2025240669A1 (en) * | 2024-05-15 | 2025-11-20 | Intercept Pharmaceuticals, Inc. | Crystalline forms of a farnesoid x receptor agonist |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2080775A (en) * | 1934-08-22 | 1937-05-18 | Celanese Corp | Shedding mechanism for circular looms |
| US2802775A (en) * | 1953-05-29 | 1957-08-13 | Merck & Co Inc | 11 alpha-hydroxylation of steroids by aspergillus ochraceus |
| JPS59205396A (ja) * | 1983-05-09 | 1984-11-20 | Kuraray Co Ltd | １１β−ヒドロキシプレグナ−４−エン−３−オン−２０−カルブアルデヒド及びその製造法 |
| JP2002532729A (ja) | 1998-12-23 | 2002-10-02 | グラクソ グループ リミテッド | 核内受容体のリガンドのアッセイ |
| ITMI20021532A1 (it) * | 2002-07-12 | 2004-01-12 | Roberto Pellicciari | Composti chimici |
| EP1568706A1 (en) * | 2004-02-26 | 2005-08-31 | Intercept Pharmaceuticals, Inc. | Novel steroid agonist for FXR |
| EP1734970B1 (en) * | 2004-03-12 | 2014-12-31 | Intercept Pharmaceuticals, Inc. | Treatment of fibrosis using fxr ligands |
| PT2040713E (pt) * | 2006-06-27 | 2014-10-13 | Intercept Pharmaceuticals Inc | Para a prevenção ou o tratamento de doenças ou estados clínicos mediados por fxr |
| CA2912139C (en) | 2013-05-14 | 2021-04-20 | Roberto Pellicciari | 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators |
-
2014
- 2014-05-14 CA CA2912139A patent/CA2912139C/en active Active
- 2014-05-14 EP EP18163623.4A patent/EP3360882B1/en active Active
- 2014-05-14 PL PL18163622T patent/PL3360881T3/pl unknown
- 2014-05-14 WO PCT/EP2014/059896 patent/WO2014184271A1/en not_active Ceased
- 2014-05-14 US US14/120,366 patent/US9611289B2/en active Active
- 2014-05-14 MY MYPI2015002734A patent/MY187886A/en unknown
- 2014-05-14 MX MX2015015730A patent/MX352065B/es active IP Right Grant
- 2014-05-14 TN TN2015000497A patent/TN2015000497A1/en unknown
- 2014-05-14 KR KR1020157034951A patent/KR102229952B1/ko active Active
- 2014-05-14 SM SM20180326T patent/SMT201800326T1/it unknown
- 2014-05-14 MA MA38647A patent/MA38647B1/fr unknown
- 2014-05-14 ES ES18163623T patent/ES2843737T3/es active Active
- 2014-05-14 SG SG11201509352XA patent/SG11201509352XA/en unknown
- 2014-05-14 PL PL18163623T patent/PL3360882T3/pl unknown
- 2014-05-14 DK DK14723820.8T patent/DK2997035T3/en active
- 2014-05-14 CN CN201480036949.5A patent/CN105377870B/zh active Active
- 2014-05-14 PL PL14723820T patent/PL2997035T3/pl unknown
- 2014-05-14 SI SI201431741T patent/SI3360882T1/sl unknown
- 2014-05-14 ME MEP-2018-159A patent/ME03082B/me unknown
- 2014-05-14 ES ES20211780T patent/ES2936638T3/es active Active
- 2014-05-14 EP EP14723820.8A patent/EP2997035B8/en active Active
- 2014-05-14 ES ES18163622T patent/ES2847002T3/es active Active
- 2014-05-14 HU HUE14723820A patent/HUE037996T2/hu unknown
- 2014-05-14 SI SI201430701T patent/SI2997035T1/sl unknown
- 2014-05-14 EP EP18163622.6A patent/EP3360881B1/en active Active
- 2014-05-14 DK DK18163622.6T patent/DK3360881T3/da active
- 2014-05-14 SI SI201431742T patent/SI3360881T1/sl unknown
- 2014-05-14 RS RS20180690A patent/RS57372B1/sr unknown
- 2014-05-14 LT LTEP14723820.8T patent/LT2997035T/lt unknown
- 2014-05-14 DK DK20211780.0T patent/DK3848038T3/da active
- 2014-05-14 HR HRP20180931TT patent/HRP20180931T1/hr unknown
- 2014-05-14 UA UAA201511098A patent/UA118673C2/uk unknown
- 2014-05-14 PE PE2015002397A patent/PE20160665A1/es unknown
- 2014-05-14 AU AU2014267324A patent/AU2014267324B2/en active Active
- 2014-05-14 PE PE2020000355A patent/PE20200844A1/es unknown
- 2014-05-14 PT PT181636226T patent/PT3360881T/pt unknown
- 2014-05-14 EA EA201592055A patent/EA030152B1/ru unknown
- 2014-05-14 CN CN201810162562.4A patent/CN108245523B/zh not_active Expired - Fee Related
- 2014-05-14 BR BR112015028399-3A patent/BR112015028399B1/pt active IP Right Grant
- 2014-05-14 PT PT181636234T patent/PT3360882T/pt unknown
- 2014-05-14 TR TR2018/09041T patent/TR201809041T4/tr unknown
- 2014-05-14 EP EP20211780.0A patent/EP3848038B1/en active Active
- 2014-05-14 PT PT147238208T patent/PT2997035T/pt unknown
- 2014-05-14 ES ES14723820.8T patent/ES2671427T3/es active Active
- 2014-05-14 DK DK18163623.4T patent/DK3360882T3/da active
- 2014-05-14 JP JP2016513357A patent/JP6326131B2/ja active Active
-
2015
- 2015-11-12 IL IL242555A patent/IL242555B/en active IP Right Grant
- 2015-11-12 SA SA515370140A patent/SA515370140B1/ar unknown
- 2015-11-13 PH PH12015502576A patent/PH12015502576B1/en unknown
- 2015-11-13 GT GT201500324A patent/GT201500324A/es unknown
- 2015-11-13 CL CL2015003344A patent/CL2015003344A1/es unknown
- 2015-11-13 NI NI201500160A patent/NI201500160A/es unknown
- 2015-12-07 CR CR20150643A patent/CR20150643A/es unknown
-
2016
- 2016-07-15 CL CL2016001809A patent/CL2016001809A1/es unknown
-
2017
- 2017-02-16 US US15/434,685 patent/US20170216316A1/en not_active Abandoned
-
2018
- 2018-04-13 JP JP2018077654A patent/JP2018127481A/ja not_active Withdrawn
- 2018-06-01 CY CY20181100583T patent/CY1122614T1/el unknown
- 2018-09-06 US US16/124,139 patent/US10532061B2/en active Active
-
2019
- 2019-11-26 US US16/695,528 patent/US11000532B2/en active Active
-
2020
- 2020-02-17 IL IL272718A patent/IL272718B/en active IP Right Grant
-
2021
- 2021-04-13 US US17/228,819 patent/US20210228599A1/en not_active Abandoned
-
2023
- 2023-04-03 US US18/295,091 patent/US20230233581A1/en not_active Abandoned
-
2024
- 2024-08-12 US US18/800,808 patent/US20240398834A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2016518429A5 (https=) | ||
| JP2010500285A5 (https=) | ||
| JP2018530559A5 (https=) | ||
| RU2017130466A (ru) | Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения | |
| RU2017120970A (ru) | Производные желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения | |
| RU2017118569A (ru) | Аналоги желчных кислот как агонисты fxr/tgr5 и способы их применения | |
| TWI865487B (zh) | 苯并噻二氮呯化合物及其用作膽酸調節物之用途 | |
| TWI877262B (zh) | 苯并噻氮呯化合物及其作為膽酸調節劑之用途 | |
| TWI835997B (zh) | 苯并噻氮呯化合物及其用作膽酸調節劑之用途 | |
| JP2017537061A5 (https=) | ||
| HRP20211066T1 (hr) | Derivati žučnih kiselina kao agonisti fxr/tgr5 i postupci njihove uporabe | |
| IL272718A (en) | 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators | |
| CN108348530B (zh) | 法尼醇x受体调节剂 | |
| JP2019504899A5 (https=) | ||
| JP2019504898A5 (https=) | ||
| JP2024541920A5 (https=) | ||
| JP2024534621A5 (https=) | ||
| JP2014520823A5 (https=) | ||
| JP2010526814A5 (https=) | ||
| JP2011513367A5 (https=) | ||
| IL287159B2 (en) | Small molecules agonists for FXR (farnesoid X receptor) and method for their preparation and use | |
| WO2017162211A1 (zh) | 药物组合物及其用途 | |
| JP2022507805A5 (https=) | ||
| CN111655678A (zh) | 细胞凋亡信号调节激酶-1抑制剂及其应用 | |
| JP2021533206A5 (https=) |