CN107686486B - 含氮三环化合物及其在药物中的应用 - Google Patents
含氮三环化合物及其在药物中的应用 Download PDFInfo
- Publication number
- CN107686486B CN107686486B CN201710653056.0A CN201710653056A CN107686486B CN 107686486 B CN107686486 B CN 107686486B CN 201710653056 A CN201710653056 A CN 201710653056A CN 107686486 B CN107686486 B CN 107686486B
- Authority
- CN
- China
- Prior art keywords
- compound
- methyl
- mmol
- alkyl
- amino
- 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.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2016106400435 | 2016-08-05 | ||
| CN201610640043 | 2016-08-05 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107686486A CN107686486A (zh) | 2018-02-13 |
| CN107686486B true CN107686486B (zh) | 2020-12-22 |
Family
ID=61072781
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710653056.0A Active CN107686486B (zh) | 2016-08-05 | 2017-08-02 | 含氮三环化合物及其在药物中的应用 |
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 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101448791A (zh) * | 2006-05-24 | 2009-06-03 | 伊莱利利公司 | Fxr激动剂 |
| EP2128158A1 (en) * | 2008-05-26 | 2009-12-02 | Phenex Pharmaceuticals AG | Heterocyclic cyclopropyl-substituted FXR binding compounds |
| CN102548974A (zh) * | 2009-08-19 | 2012-07-04 | 菲尼克斯药品股份公司 | 新型fxr(nr1h4)结合和活性调节化合物 |
| WO2016103037A1 (en) * | 2014-12-22 | 2016-06-30 | Akarna Therapeutics, Ltd. | Fused bicyclic compounds for the treatment of disease |
| CN105884758A (zh) * | 2015-02-13 | 2016-08-24 | 广东东阳光药业有限公司 | 三环化合物及其在药物中的应用 |
Family Cites Families (54)
| 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 |
| 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 |
| 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. |
| 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
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101448791A (zh) * | 2006-05-24 | 2009-06-03 | 伊莱利利公司 | Fxr激动剂 |
| EP2128158A1 (en) * | 2008-05-26 | 2009-12-02 | Phenex Pharmaceuticals AG | Heterocyclic cyclopropyl-substituted FXR binding compounds |
| CN102548974A (zh) * | 2009-08-19 | 2012-07-04 | 菲尼克斯药品股份公司 | 新型fxr(nr1h4)结合和活性调节化合物 |
| WO2016103037A1 (en) * | 2014-12-22 | 2016-06-30 | Akarna Therapeutics, Ltd. | Fused bicyclic compounds for the treatment of disease |
| CN105884758A (zh) * | 2015-02-13 | 2016-08-24 | 广东东阳光药业有限公司 | 三环化合物及其在药物中的应用 |
Non-Patent Citations (1)
| Title |
|---|
| 法呢醇X受体激动剂研究进展;贾薇;《中国药物化学杂志》;20100228;第20卷(第1期);64-69 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3494118A1 (en) | 2019-06-12 |
| TW201808283A (zh) | 2018-03-16 |
| WO2018024224A1 (en) | 2018-02-08 |
| CN107686486A (zh) | 2018-02-13 |
| US10562910B2 (en) | 2020-02-18 |
| EP3494118A4 (en) | 2020-02-26 |
| CA3030377A1 (en) | 2018-02-08 |
| ES2950412T3 (es) | 2023-10-09 |
| CA3030377C (en) | 2023-12-12 |
| JP6983225B2 (ja) | 2021-12-17 |
| AU2017306605A1 (en) | 2019-02-14 |
| JP2019524784A (ja) | 2019-09-05 |
| AU2017306605B2 (en) | 2021-08-05 |
| EP3494118B1 (en) | 2023-06-21 |
| US20190169203A1 (en) | 2019-06-06 |
| AR109295A1 (es) | 2018-11-14 |
| KR102368298B1 (ko) | 2022-02-28 |
| KR20190035766A (ko) | 2019-04-03 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN107686486B (zh) | 含氮三环化合物及其在药物中的应用 | |
| ES2791401T3 (es) | Compuestos tricíclicos y sus usos en medicina | |
| JP7451765B2 (ja) | Cdk阻害剤としてのピリジンアセトアミド系誘導体、その調製方法及び用途 | |
| CN108430998B (zh) | 氮杂双环衍生物及其制备方法和用途 | |
| TWI776156B (zh) | 作為hdac抑制劑之 3-芳基-4-醯胺基-雙環[4,5,0]異羥肟酸 | |
| TWI801492B (zh) | 含氮三環化合物及其在藥物中的應用 | |
| CN110770233B (zh) | 稠合双环类化合物及其在药物中的应用 | |
| US9617259B2 (en) | Histone deacetylase inhibitors and compositions and methods of use thereof | |
| TW201514150A (zh) | 組蛋白去乙醯酶抑制劑及組成物,暨其使用之方法 | |
| CN109071548A (zh) | 可用于治疗尤其是癌症的吡咯并咪唑衍生物或其类似物 | |
| CN107406427A (zh) | 炔基醇及其使用方法 | |
| WO2023109471A1 (zh) | 螺环嘧啶酮衍生物、其制备方法、药物组合物和用途 | |
| JP7406008B2 (ja) | Cdk9阻害剤としての多環式アミド系誘導体、その調製方法及び用途 | |
| CN115557913A (zh) | 苯并氮杂环类化合物及其在药物中的应用 | |
| CN110357875A (zh) | 氮杂双环辛烷类衍生物、其制备方法及其在医药上的用途 | |
| WO2020207263A1 (zh) | 苯并咪唑化合物、其制备方法及其用途 | |
| WO2025020191A1 (zh) | 甾类化合物、其制备方法和应用 | |
| WO2025201078A1 (zh) | 化合物、包含其的药物组合物及其制备方法和用途 | |
| WO2025021193A1 (zh) | 甾类化合物、其制备方法和应用 | |
| JP2025521097A (ja) | Lrrk2阻害剤 | |
| WO2024179393A1 (zh) | 亚砜酰亚胺化合物及其作为lrrk2蛋白激酶抑制剂的应用 | |
| WO2021136326A1 (zh) | 芳香酰胺类化合物及其在药物中的应用 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CP03 | Change of name, title or address |
Address after: 523808 No.1, Gongye North Road, Songshanhu Park, Dongguan City, Guangdong Province Patentee after: Guangdong Dongyangguang Pharmaceutical Co.,Ltd. Address before: 523000 Songshan Lake Science and Technology Industrial Park, Dongguan, Guangdong Patentee before: SUNSHINE LAKE PHARMA Co.,Ltd. |
|
| CP03 | Change of name, title or address |