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
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- JP
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- Prior art keywords
- alkyl
- independently
- deuterium
- amino
- hydroxy
- Prior art date
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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 (enExample) | 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 (enExample) |
| EP (1) | EP3494118B1 (enExample) |
| JP (1) | JP6983225B2 (enExample) |
| KR (1) | KR102368298B1 (enExample) |
| CN (1) | CN107686486B (enExample) |
| AR (1) | AR109295A1 (enExample) |
| AU (1) | AU2017306605B2 (enExample) |
| CA (1) | CA3030377C (enExample) |
| ES (1) | ES2950412T3 (enExample) |
| TW (1) | TW201808283A (enExample) |
| WO (1) | WO2018024224A1 (enExample) |
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 |
| EA201790802A1 (ru) | 2014-10-06 | 2017-08-31 | Экзикьюр, Инк. | Соединения против tnf |
| 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 |
| BR112018075734A2 (pt) | 2016-06-13 | 2019-04-02 | Gilead Sciences, Inc. | composto, composição farmacêutica, método para tratar um paciente com uma doença ou condição mediada pelo menos em parte por fxr, e, uso de um composto. |
| WO2018067704A1 (en) | 2016-10-04 | 2018-04-12 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| US10597391B2 (en) | 2016-10-26 | 2020-03-24 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof |
| CN110461328A (zh) | 2017-03-28 | 2019-11-15 | 吉利德科学公司 | 治疗肝疾病的治疗组合 |
| WO2019089665A1 (en) * | 2017-11-01 | 2019-05-09 | Bristol-Myers Squibb Company | Alkene spirocyclic compounds as farnesoid x receptor modulators |
| 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 |
| US10829486B2 (en) | 2018-02-14 | 2020-11-10 | Enanta Pharmacueticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| EP4360632B1 (en) | 2019-01-15 | 2025-10-29 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| US11524005B2 (en) | 2019-02-19 | 2022-12-13 | 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 |
| CN114080234A (zh) | 2019-07-23 | 2022-02-22 | 诺华股份有限公司 | 包含fxr激动剂的治疗 |
| EP4003349A1 (en) | 2019-07-23 | 2022-06-01 | Novartis AG | Combination treatment of liver diseases using fxr agonists |
| CA3153062A1 (en) | 2019-09-03 | 2021-03-11 | Novartis Ag | Treatment of liver disease or disorder comprising actrii receptor antagonists |
| WO2021053618A1 (en) | 2019-09-19 | 2021-03-25 | Novartis Ag | Treatment comprising fxr agonists |
| EP4041233A1 (en) | 2019-09-30 | 2022-08-17 | 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 |
| CN112876492B (zh) * | 2019-11-29 | 2023-07-18 | 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 |
| US20230002400A1 (en) * | 2019-11-29 | 2023-01-05 | Sunshine Lake Pharma Co., Ltd. | Amorphous form of nitrogen-containing tricyclic compound and use thereof |
| TW202135811A (zh) | 2019-12-20 | 2021-10-01 | 瑞士商諾華公司 | 使用整聯蛋白抑制劑組合治療肝臟疾病 |
| WO2022101853A1 (en) | 2020-11-16 | 2022-05-19 | Novartis Ag | Method of determining liver fibrosis |
| CN115974884B (zh) * | 2021-10-15 | 2026-04-28 | 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 |
| WO2023061468A1 (zh) | 2021-10-15 | 2023-04-20 | 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 |
| 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 |
| US20250262191A1 (en) * | 2021-10-15 | 2025-08-21 | 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 |
| WO2025015951A1 (zh) * | 2023-07-17 | 2025-01-23 | 上海枢境生物科技有限公司 | 双环[5,6]咪唑嘧啶酮类衍生物、其制备方法和应用 |
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. |
| ES2326850T3 (es) | 1998-12-23 | 2009-10-20 | Glaxo Group Limited | Ensayos para ligandos de receptores nucleares. |
| IL146732A0 (en) * | 1999-06-03 | 2002-07-25 | Nippon Suisan Kaisha Ltd | Tricyclic fused heterocycle compounds, process for preparing the same and use thereof |
| EP1285914B1 (en) | 2001-08-13 | 2007-12-19 | PheneX Pharmaceuticals AG | Nr1h4 nuclear receptor binding compounds |
| JP2006515838A (ja) | 2002-11-22 | 2006-06-08 | スミスクライン ビーチャム コーポレーション | ファルネソイドx受容体アゴニスト |
| WO2007076260A2 (en) | 2005-12-19 | 2007-07-05 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
| JP5301286B2 (ja) | 2006-02-03 | 2013-09-25 | イーライ リリー アンド カンパニー | Fx受容体を調節するための化合物及び方法 |
| JP2007230909A (ja) | 2006-03-01 | 2007-09-13 | Univ Of Tokyo | 置換イソキサゾール誘導体 |
| AU2007267692B2 (en) | 2006-05-24 | 2012-06-14 | Eli Lilly And Company | Compounds and methods for modulating FXR |
| DK2029547T3 (da) * | 2006-05-24 | 2010-07-26 | Lilly Co Eli | FXR-agonister |
| 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, |
| WO2008073825A1 (en) * | 2006-12-08 | 2008-06-19 | Exelixis, Inc. | Lxr and fxr modulators |
| EA200901512A1 (ru) | 2007-06-13 | 2010-06-30 | ГЛАКСОСМИТКЛАЙН ЭлЭлСи | Агонисты фарнезоидных х-рецепторов |
| AU2008270784A1 (en) * | 2007-07-02 | 2009-01-08 | Glaxosmithkline Llc | Farnesoid X receptor agonists |
| 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 |
| 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 |
| US20140039007A1 (en) | 2010-12-20 | 2014-02-06 | David C. Tully | 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 |
| 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 |
| KR20170095965A (ko) | 2014-12-18 | 2017-08-23 | 노파르티스 아게 | 간 및 위장 질환의 치료에 사용하기 위한 fxr 효능제로서의 아자비시클로옥탄 유도체 |
| JP2017538773A (ja) * | 2014-12-22 | 2017-12-28 | アカーナ・セラピューティクス・リミテッドAkarna Therapeutics, Ltd. | 疾患の処置のための縮合二環式化合物 |
| 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 |
| WO2016174616A1 (en) * | 2015-04-30 | 2016-11-03 | Novartis Ag | Fused tricyclic pyrazole derivatives useful for modulating farnesoid x receptors |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2017189652A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US10080742B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives 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 |
| US10144729B2 (en) | 2016-05-18 | 2018-12-04 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs 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 |
| BR112018075734A2 (pt) | 2016-06-13 | 2019-04-02 | Gilead Sciences, Inc. | composto, composição farmacêutica, método para tratar um paciente com uma doença ou condição mediada pelo menos em parte por fxr, e, uso de um composto. |
| AR108711A1 (es) | 2016-06-13 | 2018-09-19 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4) |
| US11091482B2 (en) | 2016-08-23 | 2021-08-17 | Ardelyx, Inc. | Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as FXR activators |
| EP3504205B1 (en) | 2016-08-23 | 2021-08-04 | Ardelyx, Inc. | 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 |
| WO2018067704A1 (en) | 2016-10-04 | 2018-04-12 | 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 |
| US10597391B2 (en) | 2016-10-26 | 2020-03-24 | 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 JP JP2019506117A patent/JP6983225B2/ja active Active
- 2017-08-02 CA CA3030377A patent/CA3030377C/en active Active
- 2017-08-02 EP EP17836406.3A patent/EP3494118B1/en active Active
- 2017-08-02 US US16/322,945 patent/US10562910B2/en active Active
- 2017-08-02 KR KR1020197005041A patent/KR102368298B1/ko active Active
- 2017-08-02 CN CN201710653056.0A patent/CN107686486B/zh active Active
- 2017-08-02 AU AU2017306605A patent/AU2017306605B2/en active Active
- 2017-08-02 ES ES17836406T patent/ES2950412T3/es active Active
- 2017-08-02 WO PCT/CN2017/095724 patent/WO2018024224A1/en not_active Ceased
- 2017-08-04 AR ARP170102212A patent/AR109295A1/es active IP Right Grant