JP2014520823A5 - - Google Patents
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- JP2014520823A5 JP2014520823A5 JP2014519453A JP2014519453A JP2014520823A5 JP 2014520823 A5 JP2014520823 A5 JP 2014520823A5 JP 2014519453 A JP2014519453 A JP 2014519453A JP 2014519453 A JP2014519453 A JP 2014519453A JP 2014520823 A5 JP2014520823 A5 JP 2014520823A5
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- disease
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- liver
- compound
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- 125000000217 alkyl group Chemical group 0.000 claims description 27
- 150000001875 compounds Chemical class 0.000 claims description 16
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 3
- 239000000651 prodrug Substances 0.000 claims description 3
- 229940002612 prodrug Drugs 0.000 claims description 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 2
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims description 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims description 2
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims description 2
- 125000002541 furyl group Chemical group 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims description 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 22
- 201000010099 disease Diseases 0.000 claims 18
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 8
- 230000001684 chronic effect Effects 0.000 claims 7
- 206010016654 Fibrosis Diseases 0.000 claims 6
- 208000019425 cirrhosis of liver Diseases 0.000 claims 6
- 210000004185 liver Anatomy 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 206010048832 Colon adenoma Diseases 0.000 claims 4
- 208000004930 Fatty Liver Diseases 0.000 claims 4
- 230000001587 cholestatic effect Effects 0.000 claims 4
- 230000007882 cirrhosis Effects 0.000 claims 4
- 206010012601 diabetes mellitus Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 230000003176 fibrotic effect Effects 0.000 claims 4
- 230000003463 hyperproliferative effect Effects 0.000 claims 4
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 4
- 230000000414 obstructive effect Effects 0.000 claims 4
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 208000007788 Acute Liver Failure Diseases 0.000 claims 2
- 206010000804 Acute hepatic failure 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
- 206010061000 Benign pancreatic neoplasm Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm 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
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 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
- 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
- 208000031112 adenoma of pancreas Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 238000002512 chemotherapy Methods 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 208000010706 fatty liver disease Diseases 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
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 208000028867 ischemia Diseases 0.000 claims 2
- 125000003473 lipid group Chemical group 0.000 claims 2
- 150000002632 lipids Chemical class 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
- 230000003211 malignant 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
- 230000037361 pathway Effects 0.000 claims 2
- 208000015768 polyposis Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000007863 steatosis Effects 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 238000012752 Hepatectomy Methods 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000037356 lipid metabolism Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002271 resection Methods 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161507153P | 2011-07-13 | 2011-07-13 | |
| EP11005722.1 | 2011-07-13 | ||
| US61/507,153 | 2011-07-13 | ||
| EP11005722A EP2545964A1 (en) | 2011-07-13 | 2011-07-13 | Novel FXR (NR1H4) binding and activity modulating compounds |
| PCT/EP2012/002941 WO2013007387A1 (en) | 2011-07-13 | 2012-07-12 | Novel fxr (nr1h4) binding and activity modulating compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016154511A Division JP6321097B2 (ja) | 2011-07-13 | 2016-08-05 | 新規なｆｘｒ（ｎｒ１ｈ４）結合および活性調節化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014520823A JP2014520823A (ja) | 2014-08-25 |
| JP2014520823A5 true JP2014520823A5 (enExample) | 2016-08-04 |
| JP5986633B2 JP5986633B2 (ja) | 2016-09-06 |
Family
ID=44513243
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014519453A Active JP5986633B2 (ja) | 2011-07-13 | 2012-07-12 | 新規なｆｘｒ（ｎｒ１ｈ４）結合および活性調節化合物 |
| JP2016154511A Active JP6321097B2 (ja) | 2011-07-13 | 2016-08-05 | 新規なｆｘｒ（ｎｒ１ｈ４）結合および活性調節化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016154511A Active JP6321097B2 (ja) | 2011-07-13 | 2016-08-05 | 新規なｆｘｒ（ｎｒ１ｈ４）結合および活性調節化合物 |
Country Status (31)
| Country | Link |
|---|---|
| US (5) | US9139539B2 (enExample) |
| EP (5) | EP2545964A1 (enExample) |
| JP (2) | JP5986633B2 (enExample) |
| KR (4) | KR101934335B1 (enExample) |
| CN (2) | CN107252424B (enExample) |
| AR (1) | AR087127A1 (enExample) |
| AU (4) | AU2012283387C1 (enExample) |
| BR (3) | BR122020008872B1 (enExample) |
| CA (1) | CA2839357C (enExample) |
| CY (1) | CY1117453T1 (enExample) |
| DK (2) | DK2731676T3 (enExample) |
| EA (1) | EA024843B1 (enExample) |
| ES (3) | ES2569718T3 (enExample) |
| FI (1) | FI3246070T3 (enExample) |
| HR (2) | HRP20160442T1 (enExample) |
| HU (2) | HUE027931T2 (enExample) |
| IL (1) | IL229944A (enExample) |
| LT (1) | LT3246070T (enExample) |
| ME (1) | ME02434B (enExample) |
| MX (2) | MX368371B (enExample) |
| MY (1) | MY161158A (enExample) |
| PH (1) | PH12014500124A1 (enExample) |
| PL (3) | PL3246070T3 (enExample) |
| PT (2) | PT3246070T (enExample) |
| RS (1) | RS54786B1 (enExample) |
| SI (3) | SI2731676T1 (enExample) |
| SM (1) | SMT201600169B (enExample) |
| TW (1) | TWI439455B (enExample) |
| UY (1) | UY34196A (enExample) |
| WO (1) | WO2013007387A1 (enExample) |
| ZA (1) | ZA201309521B (enExample) |
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| TWI625121B (zh) | 2009-07-13 | 2018-06-01 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| IL253437A0 (en) * | 2011-07-13 | 2017-09-28 | Gilead Sciences Inc | New compounds modulate fxr (nr1h4) activity and bind |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| DK3043865T3 (da) | 2013-09-11 | 2021-02-01 | Univ Claude Bernard Lyon | Fremgangsmåder og farmaceutiske sammensætningr til behandlingen af hepatitis b-virusinfektion |
| NZ729678A (en) | 2014-09-24 | 2018-07-27 | Gilead Sciences Inc | Methods of treating non-alcoholic steatohepatitis using ask1 inhibitor in combination with a fxr agonist |
| EP3006939A1 (en) | 2014-10-06 | 2016-04-13 | Gilead Sciences, Inc. | Histidine-rich Glycoprotein as a marker for hepatic Farnesoid X receptor activation |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| EP3034499A1 (en) | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Novel FXR (NR1H4) modulating compounds |
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| BR112017013382A2 (pt) | 2014-12-23 | 2018-02-14 | Gilead Sciences Inc | método para preparar um composto, composto, e, ácido. |
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