JP2019524784A5 - - Google Patents
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- JP2019524784A5 JP2019524784A5 JP2019506117A JP2019506117A JP2019524784A5 JP 2019524784 A5 JP2019524784 A5 JP 2019524784A5 JP 2019506117 A JP2019506117 A JP 2019506117A JP 2019506117 A JP2019506117 A JP 2019506117A JP 2019524784 A5 JP2019524784 A5 JP 2019524784A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- deuterium
- amino
- hydroxy
- 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.)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610640043 | 2016-08-05 | ||
| CN201610640043.5 | 2016-08-05 | ||
| PCT/CN2017/095724 WO2018024224A1 (en) | 2016-08-05 | 2017-08-02 | Nitrogen-containing tricyclic compounds and uses thereof in medicine |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019524784A JP2019524784A (ja) | 2019-09-05 |
| JP2019524784A5 true JP2019524784A5 (https=) | 2020-07-30 |
| JP6983225B2 JP6983225B2 (ja) | 2021-12-17 |
Family
ID=61072781
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019506117A Active JP6983225B2 (ja) | 2016-08-05 | 2017-08-02 | 窒素含有三環式化合物、および医薬におけるその使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10562910B2 (https=) |
| EP (1) | EP3494118B1 (https=) |
| JP (1) | JP6983225B2 (https=) |
| KR (1) | KR102368298B1 (https=) |
| CN (1) | CN107686486B (https=) |
| AR (1) | AR109295A1 (https=) |
| AU (1) | AU2017306605B2 (https=) |
| CA (1) | CA3030377C (https=) |
| ES (1) | ES2950412T3 (https=) |
| TW (1) | TW201808283A (https=) |
| WO (1) | WO2018024224A1 (https=) |
Families Citing this family (34)
| 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 |
| CA2963931A1 (en) | 2014-10-06 | 2016-04-14 | Exicure, Inc. | Anti-tnf compounds |
| WO2016161003A1 (en) | 2015-03-31 | 2016-10-06 | Enanta Phamraceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds |
| MX385718B (es) | 2016-06-13 | 2025-03-18 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4). |
| US10450306B2 (en) | 2016-10-04 | 2019-10-22 | 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 |
| PT3600309T (pt) | 2017-03-28 | 2022-10-03 | Gilead Sciences Inc | Combinações terapêuticas para o tratamento de doenças hepáticas |
| AU2018360575A1 (en) * | 2017-11-01 | 2020-06-18 | Bristol-Myers Squibb Company | Alkene spirocyclic compounds as farnesoid X receptor modulators |
| WO2019118571A1 (en) | 2017-12-12 | 2019-06-20 | 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 |
| US10829486B2 (en) | 2018-02-14 | 2020-11-10 | Enanta Pharmacueticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| EP3911647B1 (en) | 2019-01-15 | 2023-12-13 | Gilead Sciences, Inc. | Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same |
| CA3233305A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| WO2020231917A1 (en) | 2019-05-13 | 2020-11-19 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| CN110028443B (zh) * | 2019-05-29 | 2022-03-04 | 济南周行医药科技有限公司 | 一种调节fxr活性的三环化合物类药物中间体的制备方法 |
| KR20220038368A (ko) | 2019-07-23 | 2022-03-28 | 노파르티스 아게 | Fxr 작용제를 이용하는 간 질환의 병용 치료 |
| WO2021014349A1 (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 |
| CN114401745A (zh) | 2019-09-19 | 2022-04-26 | 诺华股份有限公司 | 包含fxr激动剂的治疗 |
| WO2021064575A1 (en) | 2019-09-30 | 2021-04-08 | Novartis Ag | Treatment comprising the use of fxr agonists |
| CN112876490A (zh) * | 2019-11-29 | 2021-06-01 | 广东东阳光药业有限公司 | 含氮三环化合物的晶型及其用途 |
| CN112876493B (zh) * | 2019-11-29 | 2023-05-09 | 广东东阳光药业有限公司 | 含氮三环化合物的盐及其用途 |
| JP7750836B2 (ja) * | 2019-11-29 | 2025-10-07 | ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 | 三環式含窒素化合物の非晶質及びその用途 |
| US12492211B2 (en) | 2019-11-29 | 2025-12-09 | Sunshine Lake Pharma Co., Ltd. | Crystalline form of nitrogen-containing tricyclic compound and use thereof |
| KR20220119424A (ko) | 2019-12-20 | 2022-08-29 | 노파르티스 아게 | 인테그린 억제제를 사용한 간 질환의 조합 치료 |
| WO2022101853A1 (en) | 2020-11-16 | 2022-05-19 | Novartis Ag | Method of determining liver fibrosis |
| EP4417611A4 (en) * | 2021-10-15 | 2025-10-22 | Sunshine Lake Pharma Co Ltd | NEW CRYSTALLINE FORM OF A NITROGEN-CONTAINING TRICYCLIC COMPOUND AND ITS USE |
| CN115974885A (zh) * | 2021-10-15 | 2023-04-18 | 广东东阳光药业有限公司 | 含氮三环化合物的新晶型及其用途 |
| US20240409549A1 (en) | 2021-10-15 | 2024-12-12 | Sunshine Lake Pharma Co., Ltd. | New crystal form and use of nitrogenous tricyclic compound |
| US20250268871A1 (en) | 2021-10-15 | 2025-08-28 | Sunshine Lake Pharma Co., Ltd. | New crystal form of nitrogen-containing tricyclic compound and use thereof |
| CN118271327A (zh) * | 2022-12-30 | 2024-07-02 | 广东东阳光药业股份有限公司 | 三环化合物的晶型及其用途 |
| WO2024212943A1 (zh) * | 2023-04-10 | 2024-10-17 | 广东东阳光药业股份有限公司 | 含氮三环化合物的新晶型及其用途 |
| TWI896037B (zh) * | 2023-07-17 | 2025-09-01 | 大陸商上海樞境生物科技有限公司 | 雙環[5,6]咪唑嘧啶酮類衍生物、其製備方法和應用 |
Family Cites Families (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US801249A (en) * | 1904-03-10 | 1905-10-10 | Edward Keagy | Concrete-block mold. |
| DE69940958D1 (de) | 1998-12-23 | 2009-07-16 | Glaxo Group Ltd | Bestimmungsmethode fur liganden der nuklearen rezeptoren |
| IL146732A0 (en) | 1999-06-03 | 2002-07-25 | Nippon Suisan Kaisha Ltd | Tricyclic fused heterocycle compounds, process for preparing the same and use thereof |
| ATE381542T1 (de) | 2001-08-13 | 2008-01-15 | Phenex Pharmaceuticals Ag | Nr1h4-kern-rezeptor-bindende verbindungen |
| WO2004048349A1 (en) | 2002-11-22 | 2004-06-10 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
| WO2007076260A2 (en) | 2005-12-19 | 2007-07-05 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
| CA2640476A1 (en) | 2006-02-03 | 2007-08-16 | Eli Lilly And Company | Compounds and methods for modulating fx-receptors |
| JP2007230909A (ja) | 2006-03-01 | 2007-09-13 | Univ Of Tokyo | 置換イソキサゾール誘導体 |
| CN101448791B (zh) * | 2006-05-24 | 2011-11-16 | 伊莱利利公司 | Fxr激动剂 |
| TW200812982A (en) | 2006-05-24 | 2008-03-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
| 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 |
| 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, |
| KR20090094125A (ko) * | 2006-12-08 | 2009-09-03 | 엑셀리시스, 인코포레이티드 | Ｌｘｒ 및 ｆｘｒ 조절자 |
| KR20100038102A (ko) * | 2007-06-13 | 2010-04-12 | 글락소스미스클라인 엘엘씨 | 파네소이드 ｘ 수용체 작용제 |
| MX2009013946A (es) * | 2007-07-02 | 2010-03-10 | Glaxosmithkline Llc | Agonistas del receptor de farnesoide x. |
| TW200906823A (en) | 2007-07-16 | 2009-02-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
| EP2128158A1 (en) | 2008-05-26 | 2009-12-02 | Phenex Pharmaceuticals AG | Heterocyclic cyclopropyl-substituted FXR binding compounds |
| EP2289883A1 (en) * | 2009-08-19 | 2011-03-02 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| WO2012087521A1 (en) | 2010-12-20 | 2012-06-28 | Irm Llc | Compositions and methods for modulating farnesoid x receptors |
| EP2655368A1 (en) | 2010-12-20 | 2013-10-30 | Irm Llc | Compositions and methods for modulating farnesoid x receptors |
| CU24152B1 (es) | 2010-12-20 | 2016-02-29 | Irm Llc | 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| 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 |
| 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 |
| 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 |
| MX2017008057A (es) | 2014-12-18 | 2017-09-28 | Novartis Ag | Derivados de azabiciclooctano como agonistas de fxr para el uso en el tratamiento de enfermedades hepaticas y gastrointestinales. |
| CN107438612A (zh) * | 2014-12-22 | 2017-12-05 | 阿卡纳治疗学有限公司 | 用于治疗疾病的稠合双环化合物 |
| 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 |
| 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 |
| CN107531721B (zh) * | 2015-04-30 | 2020-07-17 | 诺华股份有限公司 | 用于调节法尼醇x受体的稠合的三环吡唑衍生物 |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2017189663A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US10080741B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189651A1 (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 |
| WO2017201152A1 (en) | 2016-05-18 | 2017-11-23 | 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 |
| MX385718B (es) | 2016-06-13 | 2025-03-18 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4). |
| AR108711A1 (es) | 2016-06-13 | 2018-09-19 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4) |
| CN116854681A (zh) | 2016-08-23 | 2023-10-10 | 阿德利克斯股份有限公司 | 用于治疗代谢病状和病症的激素受体调节剂 |
| WO2018039384A1 (en) | 2016-08-23 | 2018-03-01 | Ardelyx, Inc. | Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as fxr activators |
| 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 |
| US10450306B2 (en) | 2016-10-04 | 2019-10-22 | 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 |
| 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 |
| 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 |
| 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 |
| CN108264506B (zh) | 2018-01-17 | 2021-01-26 | 中国药科大学 | 异黄酮衍生物、其制备方法和医药用途 |
| 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 |
-
2017
- 2017-08-01 TW TW106125961A patent/TW201808283A/zh unknown
- 2017-08-02 EP EP17836406.3A patent/EP3494118B1/en active Active
- 2017-08-02 KR KR1020197005041A patent/KR102368298B1/ko active Active
- 2017-08-02 WO PCT/CN2017/095724 patent/WO2018024224A1/en not_active Ceased
- 2017-08-02 ES ES17836406T patent/ES2950412T3/es active Active
- 2017-08-02 AU AU2017306605A patent/AU2017306605B2/en active Active
- 2017-08-02 US US16/322,945 patent/US10562910B2/en active Active
- 2017-08-02 CA CA3030377A patent/CA3030377C/en active Active
- 2017-08-02 JP JP2019506117A patent/JP6983225B2/ja active Active
- 2017-08-02 CN CN201710653056.0A patent/CN107686486B/zh active Active
- 2017-08-04 AR ARP170102212A patent/AR109295A1/es active IP Right Grant