JP2019537557A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019537557A5 JP2019537557A5 JP2019517767A JP2019517767A JP2019537557A5 JP 2019537557 A5 JP2019537557 A5 JP 2019537557A5 JP 2019517767 A JP2019517767 A JP 2019517767A JP 2019517767 A JP2019517767 A JP 2019517767A JP 2019537557 A5 JP2019537557 A5 JP 2019537557A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- formula
- compound according
- pharmaceutically acceptable
- acceptable salt
- 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.)
- Abandoned
Links
- 150000001875 compounds Chemical class 0.000 claims description 69
- -1 substituted Chemical class 0.000 claims description 66
- 150000003839 salts Chemical class 0.000 claims description 27
- 229910052739 hydrogen Inorganic materials 0.000 claims description 22
- 239000001257 hydrogen Substances 0.000 claims description 22
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 20
- 201000010099 disease Diseases 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 125000000217 alkyl group Chemical group 0.000 claims description 15
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- 125000003107 substituted aryl group Chemical group 0.000 claims description 13
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 11
- 125000000304 alkynyl group Chemical group 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 125000003342 alkenyl group Chemical group 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 229910052736 halogen Inorganic materials 0.000 claims description 8
- 150000002367 halogens Chemical class 0.000 claims description 8
- 230000001404 mediated effect Effects 0.000 claims description 8
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 6
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims description 6
- 206010008635 Cholestasis Diseases 0.000 claims description 6
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 6
- 230000007870 cholestasis Effects 0.000 claims description 6
- 231100000359 cholestasis Toxicity 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 6
- 210000004185 liver Anatomy 0.000 claims description 6
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 230000001684 chronic effect Effects 0.000 claims description 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 4
- 230000003176 fibrotic effect Effects 0.000 claims description 4
- 201000005206 focal segmental glomerulosclerosis Diseases 0.000 claims description 4
- 231100000854 focal segmental glomerulosclerosis Toxicity 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 208000017169 kidney disease Diseases 0.000 claims description 4
- 208000019423 liver disease Diseases 0.000 claims description 4
- 208000030159 metabolic disease Diseases 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims description 4
- 208000010157 sclerosing cholangitis Diseases 0.000 claims description 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 208000022309 Alcoholic Liver disease Diseases 0.000 claims description 2
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims description 2
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims description 2
- 206010010356 Congenital anomaly Diseases 0.000 claims description 2
- 208000026292 Cystic Kidney disease Diseases 0.000 claims description 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 2
- 206010018367 Glomerulonephritis chronic Diseases 0.000 claims description 2
- 206010051920 Glomerulonephropathy Diseases 0.000 claims description 2
- 208000024815 Granulomatous liver disease Diseases 0.000 claims description 2
- 208000018565 Hemochromatosis Diseases 0.000 claims description 2
- 206010019799 Hepatitis viral Diseases 0.000 claims description 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims description 2
- 206010055171 Hypertensive nephropathy Diseases 0.000 claims description 2
- 206010022489 Insulin Resistance Diseases 0.000 claims description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 208000012868 Overgrowth Diseases 0.000 claims description 2
- 206010040047 Sepsis Diseases 0.000 claims description 2
- 206010048302 Tubulointerstitial nephritis Diseases 0.000 claims description 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 2
- 230000001476 alcoholic effect Effects 0.000 claims description 2
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 claims description 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 230000001580 bacterial effect Effects 0.000 claims description 2
- 125000005841 biaryl group Chemical group 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 230000002490 cerebral effect Effects 0.000 claims description 2
- 230000001587 cholestatic effect Effects 0.000 claims description 2
- 231100000850 chronic interstitial nephritis Toxicity 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 2
- 208000010643 digestive system disease Diseases 0.000 claims description 2
- 208000016097 disease of metabolism Diseases 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 2
- 208000018685 gastrointestinal system disease Diseases 0.000 claims description 2
- 208000006454 hepatitis Diseases 0.000 claims description 2
- 231100000283 hepatitis Toxicity 0.000 claims description 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 2
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims description 2
- 208000006575 hypertriglyceridemia Diseases 0.000 claims description 2
- 208000001024 intrahepatic cholestasis Diseases 0.000 claims description 2
- 230000007872 intrahepatic cholestasis Effects 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 235000016236 parenteral nutrition Nutrition 0.000 claims description 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 2
- 229940127557 pharmaceutical product Drugs 0.000 claims description 2
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims description 2
- 208000005069 pulmonary fibrosis Diseases 0.000 claims description 2
- 230000008929 regeneration Effects 0.000 claims description 2
- 238000011069 regeneration method Methods 0.000 claims description 2
- 201000002793 renal fibrosis Diseases 0.000 claims description 2
- 201000000306 sarcoidosis Diseases 0.000 claims description 2
- 208000013223 septicemia Diseases 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 210000002435 tendon Anatomy 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 2
- 201000001862 viral hepatitis Diseases 0.000 claims description 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000000126 substance Substances 0.000 description 35
- 238000000034 method Methods 0.000 description 9
- 125000003545 alkoxy group Chemical group 0.000 description 4
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 125000000000 cycloalkoxy group Chemical group 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662404059P | 2016-10-04 | 2016-10-04 | |
| US62/404,059 | 2016-10-04 | ||
| PCT/US2017/055147 WO2018067704A1 (en) | 2016-10-04 | 2017-10-04 | Isoxazole analogs as fxr agonists and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019537557A JP2019537557A (ja) | 2019-12-26 |
| JP2019537557A5 true JP2019537557A5 (enExample) | 2020-09-24 |
Family
ID=61830059
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019517767A Abandoned JP2019537557A (ja) | 2016-10-04 | 2017-10-04 | Ｆｘｒアゴニストとしてのイソキサゾール類似体およびその使用方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10450306B2 (enExample) |
| EP (1) | EP3523298A4 (enExample) |
| JP (1) | JP2019537557A (enExample) |
| KR (1) | KR20190056436A (enExample) |
| CN (1) | CN109906223A (enExample) |
| AU (1) | AU2017338853A1 (enExample) |
| BR (1) | BR112019006651A2 (enExample) |
| CA (1) | CA3039124A1 (enExample) |
| IL (1) | IL265803A (enExample) |
| MX (1) | MX2019003790A (enExample) |
| PH (1) | PH12019550050A1 (enExample) |
| RU (1) | RU2019113066A (enExample) |
| WO (1) | WO2018067704A1 (enExample) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| SG10201910670RA (en) | 2015-03-31 | 2020-01-30 | Enanta Pharm Inc | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| WO2017189651A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US10080743B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189652A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US10144729B2 (en) | 2016-05-18 | 2018-12-04 | 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 |
| WO2017201155A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | lSOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF |
| PL3730487T3 (pl) | 2016-06-13 | 2022-08-16 | Gilead Sciences, Inc. | Pochodne azetydyny jako modulatory fxr (nr1h4) |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | 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 |
| AU2017338853A1 (en) | 2016-10-04 | 2019-04-18 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| WO2018081285A1 (en) | 2016-10-26 | 2018-05-03 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as fxr agonists and methods of use thereof |
| CN108017636A (zh) * | 2016-11-04 | 2018-05-11 | 合帕吉恩治疗公司 | 作为fxr调节剂的含氮杂环化合物 |
| EP4122464B1 (en) | 2017-03-28 | 2024-05-15 | Gilead Sciences, Inc. | Therapeutic combinations for treating liver diseases |
| 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 |
| WO2020011146A1 (zh) * | 2018-07-11 | 2020-01-16 | 中国医药研究开发中心有限公司 | 1,2,4-噁二唑类化合物及其制备方法和医药用途 |
| CN110818704B (zh) * | 2018-08-08 | 2023-08-01 | 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 |
| WO2020114307A1 (zh) * | 2018-12-07 | 2020-06-11 | 四川科伦博泰生物医药股份有限公司 | 异噁唑衍生物及其制备方法和用途 |
| PE20211907A1 (es) | 2019-01-15 | 2021-09-28 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4) |
| KR20210123337A (ko) * | 2019-01-31 | 2021-10-13 | 더 내셔널 인스티튜츠 오브 파마슈티컬 알앤디 컴퍼니 리미티드 | 방향족 고리 또는 헤테로방향족 고리 화합물, 이의 제조 방법 및 이의 의학 용도 |
| CA3233305A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| CN111825595A (zh) * | 2019-04-15 | 2020-10-27 | 山东轩竹医药科技有限公司 | 钠通道阻滞剂 |
| KR20250076664A (ko) | 2019-04-19 | 2025-05-29 | 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 | Fxr 소분자 작용제 및 이의 제조 방법과 용도 |
| US11555032B2 (en) | 2019-05-13 | 2023-01-17 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| US20220241376A1 (en) | 2019-07-18 | 2022-08-04 | Enyo Pharma | Method for decreasing adverse-effects of interferon |
| CA3142905A1 (en) | 2019-07-23 | 2021-01-28 | Novartis Ag | Combination treatment of liver diseases using fxr agonists |
| CA3142904A1 (en) | 2019-07-23 | 2021-01-28 | Novartis Ag | Treatment comprising fxr agonists |
| JP7663559B2 (ja) | 2019-09-03 | 2025-04-16 | ノバルティス アーゲー | Ａｃｔｒｉｉ受容体拮抗薬を含む肝疾患または肝臓障害の治療 |
| WO2021053618A1 (en) | 2019-09-19 | 2021-03-25 | Novartis Ag | Treatment comprising fxr agonists |
| WO2021064575A1 (en) | 2019-09-30 | 2021-04-08 | Novartis Ag | Treatment comprising the use of fxr agonists |
| CN110804025B (zh) * | 2019-11-29 | 2022-02-08 | 扬州工业职业技术学院 | 一种卤代苯异噁唑衍生物及其制备方法与应用 |
| AU2020408067B2 (en) | 2019-12-20 | 2024-03-28 | Novartis Ag | Combination treatment of liver diseases using integrin inhibitors |
| IL293892A (en) | 2020-01-15 | 2022-08-01 | Inserm Institut National De La Sant? Et De La Rech M?Dicale | Use of fxr agonists for treating an infection by hepatitis d virus |
| TW202208355A (zh) | 2020-05-04 | 2022-03-01 | 美商安進公司 | 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法 |
| PH12022552933A1 (en) | 2020-05-04 | 2024-02-12 | Amgen Inc | Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use |
| CN114195786B (zh) * | 2020-09-18 | 2023-08-22 | 凯思凯迪（上海）医药科技有限公司 | 新型fxr小分子激动剂制备及其用途 |
| CN114315830B (zh) * | 2020-09-30 | 2025-08-12 | 中国科学院上海药物研究所 | Fxr小分子激动剂及其制备方法和用途 |
| US20220112178A1 (en) * | 2020-10-14 | 2022-04-14 | Tosk, Inc. | Small Molecule Modulators of RAS GTPase |
| US12180220B2 (en) | 2020-10-14 | 2024-12-31 | Tosk, Inc. | Heteroaryl modulators of RAS GTPase |
| WO2022101853A1 (en) | 2020-11-16 | 2022-05-19 | Novartis Ag | Method of determining liver fibrosis |
| CN116568672A (zh) * | 2020-11-17 | 2023-08-08 | H.隆德贝克有限公司 | 用于治疗帕金森病的新儿茶酚胺前药 |
| 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 |
| CN113024552B (zh) * | 2021-03-26 | 2022-08-05 | 厦门市博瑞来医药科技有限公司 | 一类新型非甾体fxr激动剂的合成及其应用 |
| JP2024517181A (ja) | 2021-04-28 | 2024-04-19 | ウエヌイグレックオ・ファーマ | 組合せ治療としてｆｘｒアゴニストを使用するｔｌｒ３アゴニストの効果の強い増強 |
| CN115433175B (zh) * | 2021-06-02 | 2025-05-27 | 上海交通大学 | 一类含炔基取代的喹啉和喹唑啉类化合物及其制备和用途 |
| US20250066346A1 (en) * | 2022-01-17 | 2025-02-27 | Hepagene Therapeutics (HK) Limited | Solid forms of a benzthiazole-piperazinyl-oxazole compound and methods of use thereof |
Family Cites Families (77)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5571809A (en) | 1989-04-20 | 1996-11-05 | Boehringer Ingelheim Pharmaceuticals, Inc. | The treatment of HIV-1 infection using certain pyridodiazepines |
| ES2326850T3 (es) | 1998-12-23 | 2009-10-20 | Glaxo Group Limited | Ensayos para ligandos de receptores nucleares. |
| CA2372150C (en) | 1999-04-30 | 2011-08-30 | The Regents Of The University Of Michigan | Therapeutic applications of pro-apoptotic benzodiazepines |
| EP1392714B1 (en) | 2001-03-12 | 2005-08-31 | Intercept Pharmaceuticals, Inc. | Steroids as agonists for fxr |
| EP1285914B1 (en) | 2001-08-13 | 2007-12-19 | PheneX Pharmaceuticals AG | Nr1h4 nuclear receptor binding compounds |
| US7405230B2 (en) * | 2002-07-19 | 2008-07-29 | Memory Pharmaceuticals Corporation | Phosphodiesterase 4 inhibitors, including N-substituted aniline and diphenylamine analogs |
| AU2003290796A1 (en) | 2002-11-14 | 2004-06-15 | The Scripps Research Institute | Non-steroidal fxr agonists |
| EP1562915A1 (en) | 2002-11-22 | 2005-08-17 | SmithKline Beecham Corporation | Farnesoid x receptor agonists |
| US20070054902A1 (en) | 2003-12-02 | 2007-03-08 | Shionogi & Co., Ltd. | Isoxazole derivatives as peroxisome proliferator-activated receptors agonists |
| ES2374165T3 (es) | 2005-12-19 | 2012-02-14 | Glaxosmithkline Llc | Agonistas del receptor x farnesoide. |
| EA200870217A1 (ru) * | 2006-01-30 | 2009-02-27 | Экселиксис, Инк. | 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции |
| CN101421250A (zh) * | 2006-01-30 | 2009-04-29 | 埃克塞里艾克西斯公司 | 作为jak-2调节剂的4-芳基-2-氨基-嘧啶或4-芳基-2-氨基烷基-嘧啶及包含它们的药物组合物 |
| EP1984360B1 (en) * | 2006-02-03 | 2014-01-15 | Eli Lilly & Company | Compounds and methods for modulating FX-receptors |
| BRPI0712262A2 (pt) | 2006-05-24 | 2012-07-10 | Lilly Co Eli | agonistas de fxr |
| PE20080344A1 (es) | 2006-06-27 | 2008-06-09 | Sanofi Aventis | Compuestos 8-azabiciclo[3.2.1]oct-8-il-1,2,3,4-tetrahidroquinolina sustituidos como inhibidores 11b-hsd1 |
| US8063084B2 (en) * | 2006-08-15 | 2011-11-22 | Novartis Ag | Heterocyclic compounds suitable for the treatment of diseases related to elevated lipid levels |
| EP1894928A1 (en) | 2006-08-29 | 2008-03-05 | PheneX Pharmaceuticals AG | Heterocyclic fxr binding compounds |
| EP1894924A1 (en) | 2006-08-29 | 2008-03-05 | Phenex Pharmaceuticals AG | Heterocyclic FXR binding compounds |
| RU2443586C2 (ru) | 2006-09-15 | 2012-02-27 | Вольво Ластвагнар Аб | Способ адаптации автоматической механической трансмиссии на транспортном средстве большой грузоподъемности |
| 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, |
| EP1918281A1 (en) * | 2006-11-02 | 2008-05-07 | Laboratorios del Dr. Esteve S.A. | Phenylamino-substituted piperidine compounds, their preparation and use as medicaments |
| WO2008075172A2 (en) | 2006-12-19 | 2008-06-26 | Pfizer Products Inc. | Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases |
| CN101668529A (zh) * | 2007-03-15 | 2010-03-10 | 先灵公司 | 用作葡聚糖合成酶抑制剂的哌嗪取代的哒嗪酮衍生物 |
| BRPI0812521A2 (pt) | 2007-06-13 | 2015-06-23 | Glaxosmithkline Llc | Composto, composição farmacêutica, método para o tratamento de doença em um mamífero, processo para a preparação de um composto, e, uso de um composto |
| EP2173174A4 (en) | 2007-07-02 | 2010-08-04 | Glaxosmithkline Llc | FARNESOID X RECEPTOR AGONISTS |
| TW200906823A (en) * | 2007-07-16 | 2009-02-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
| US20090163474A1 (en) | 2007-10-19 | 2009-06-25 | Wyeth | FXR Agonists for the Treatment of Nonalcoholic Fatty Liver and Cholesterol Gallstone Diseases |
| EP2110374A1 (en) * | 2008-04-18 | 2009-10-21 | Merck Sante | Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators |
| EP2128158A1 (en) | 2008-05-26 | 2009-12-02 | Phenex Pharmaceuticals AG | Heterocyclic cyclopropyl-substituted FXR binding compounds |
| US8829027B2 (en) | 2008-10-23 | 2014-09-09 | Boehringer Ingelheim International Gmbh | Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| US8329904B2 (en) | 2009-05-12 | 2012-12-11 | Hoffmann-La Roche Inc. | Azacyclic derivatives |
| WO2011021645A1 (ja) | 2009-08-19 | 2011-02-24 | 大日本住友製薬株式会社 | ２環性ウレア誘導体、またはその薬学的に許容される塩 |
| EP2289883A1 (en) | 2009-08-19 | 2011-03-02 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| DK2496582T3 (en) | 2009-11-05 | 2016-03-21 | Glaxosmithkline Llc | Benzodiazepine-BROMDOMAeNEINHIBITOR. |
| JP2014500319A (ja) | 2010-12-20 | 2014-01-09 | アイアールエム・リミテッド・ライアビリティ・カンパニー | ファルネソイドｘ受容体を調節するための組成物および方法 |
| 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 |
| US20130261108A1 (en) * | 2010-12-20 | 2013-10-03 | 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 |
| US9084826B2 (en) | 2012-05-01 | 2015-07-21 | Catabasis Pharmaceuticals, Inc. | Fatty acid conjugates of statin and FXR agonists; compositions and method of uses |
| MX377523B (es) | 2013-09-11 | 2025-03-10 | Inst Nat Sante Rech Med | Metodos y composiciones farmaceuticas para el tratamiento de la infeccion por el virus de la hepatitis b. |
| SG11201703717SA (en) | 2014-11-06 | 2017-06-29 | Enanta Pharm Inc | Bile acid analogs an 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 |
| US20170368038A1 (en) | 2014-12-18 | 2017-12-28 | Novartis Ag | Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases |
| 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 |
| 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 |
| 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 |
| WO2017133521A1 (zh) | 2016-02-01 | 2017-08-10 | 山东轩竹医药科技有限公司 | Fxr受体激动剂 |
| 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 |
| AU2017223155B2 (en) | 2016-02-22 | 2019-08-22 | Novartis Ag | Methods for using FXR agonists |
| US10080743B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189652A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| WO2017189651A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| WO2017201155A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | lSOXAZOLE 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 |
| US10144729B2 (en) | 2016-05-18 | 2018-12-04 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| PL3730487T3 (pl) | 2016-06-13 | 2022-08-16 | Gilead Sciences, Inc. | Pochodne azetydyny jako modulatory fxr (nr1h4) |
| AR108711A1 (es) | 2016-06-13 | 2018-09-19 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4) |
| TW201808283A (zh) | 2016-08-05 | 2018-03-16 | 廣東東陽光藥業有限公司 | 含氮三環化合物及其在藥物中的應用 |
| EP3504205B1 (en) | 2016-08-23 | 2021-08-04 | Ardelyx, Inc. | Hormone receptor modulators for treating metabolic conditions and disorders |
| AU2017338853A1 (en) | 2016-10-04 | 2019-04-18 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| CN107973790A (zh) | 2016-10-22 | 2018-05-01 | 合帕吉恩治疗公司 | 杂环fxr调节剂 |
| WO2018081285A1 (en) | 2016-10-26 | 2018-05-03 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as fxr agonists and methods of use thereof |
| CN108017636A (zh) | 2016-11-04 | 2018-05-11 | 合帕吉恩治疗公司 | 作为fxr调节剂的含氮杂环化合物 |
| 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 |
| CN109071468B (zh) | 2017-01-20 | 2022-09-02 | 四川科伦博泰生物医药股份有限公司 | 一种杂环化合物及其制备方法和用途 |
| CN108341822B (zh) | 2017-01-23 | 2021-04-16 | 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应用 |
| WO2018170173A1 (en) | 2017-03-15 | 2018-09-20 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
| WO2018190643A1 (en) | 2017-04-12 | 2018-10-18 | Il Dong Pharmaceutical Co., Ltd. | An isoxazole derivatives as nuclear receptor agonists and used thereof |
| CA3064794A1 (en) | 2017-05-26 | 2018-11-29 | Medshine Discovery Inc. | Lactam compound as fxr receptor agonist |
| BR112020000180A2 (pt) | 2017-07-06 | 2020-07-14 | Xuanzhu (Hainan) Biopharmaceutical Co., Ltd. | agonista do receptor fxr |
| WO2019160813A1 (en) | 2018-02-14 | 2019-08-22 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| CN109053751A (zh) | 2018-08-30 | 2018-12-21 | 成都海博锐药业有限公司 | 具有螺环结构的fxr调节剂 |
-
2017
- 2017-10-04 AU AU2017338853A patent/AU2017338853A1/en not_active Abandoned
- 2017-10-04 BR BR112019006651A patent/BR112019006651A2/pt not_active Application Discontinuation
- 2017-10-04 CA CA3039124A patent/CA3039124A1/en not_active Abandoned
- 2017-10-04 JP JP2019517767A patent/JP2019537557A/ja not_active Abandoned
- 2017-10-04 US US15/724,919 patent/US10450306B2/en active Active
- 2017-10-04 EP EP17859120.2A patent/EP3523298A4/en not_active Withdrawn
- 2017-10-04 WO PCT/US2017/055147 patent/WO2018067704A1/en not_active Ceased
- 2017-10-04 MX MX2019003790A patent/MX2019003790A/es unknown
- 2017-10-04 CN CN201780068563.6A patent/CN109906223A/zh active Pending
- 2017-10-04 KR KR1020197012682A patent/KR20190056436A/ko not_active Withdrawn
- 2017-10-04 RU RU2019113066A patent/RU2019113066A/ru not_active Application Discontinuation
-
2019
- 2019-03-28 PH PH12019550050A patent/PH12019550050A1/en unknown
- 2019-04-03 IL IL265803A patent/IL265803A/en unknown
- 2019-09-13 US US16/569,819 patent/US11034684B2/en active Active