CL2012000369A1 - Compuestos derivados de heterociclicos nitrogenados sustituidos, moduladores del receptor nr1h4(fxr); y uso para el tratamiento de trastornos hiperproliferativos malignos y no malignos, tratamiento de condiciones colestaticas cronicas intra y extrahepaticas, desordenes metabolicos en lipidos o diabetes, entre otros. - Google Patents
Compuestos derivados de heterociclicos nitrogenados sustituidos, moduladores del receptor nr1h4(fxr); y uso para el tratamiento de trastornos hiperproliferativos malignos y no malignos, tratamiento de condiciones colestaticas cronicas intra y extrahepaticas, desordenes metabolicos en lipidos o diabetes, entre otros.Info
- Publication number
- CL2012000369A1 CL2012000369A1 CL2012000369A CL2012000369A CL2012000369A1 CL 2012000369 A1 CL2012000369 A1 CL 2012000369A1 CL 2012000369 A CL2012000369 A CL 2012000369A CL 2012000369 A CL2012000369 A CL 2012000369A CL 2012000369 A1 CL2012000369 A1 CL 2012000369A1
- Authority
- CL
- Chile
- Prior art keywords
- treatment
- malignant
- receptor
- fxr
- nr1h4
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 230000003211 malignant effect Effects 0.000 title 2
- 230000001587 cholestatic effect Effects 0.000 title 1
- 230000001684 chronic effect Effects 0.000 title 1
- 206010012601 diabetes mellitus Diseases 0.000 title 1
- 230000003463 hyperproliferative effect Effects 0.000 title 1
- 150000002632 lipids Chemical class 0.000 title 1
- 208000030159 metabolic disease Diseases 0.000 title 1
- 229910052757 nitrogen Inorganic materials 0.000 title 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 title 1
- 102100038495 Bile acid receptor Human genes 0.000 abstract 3
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 abstract 3
- 108020005497 Nuclear hormone receptor Proteins 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 229940126601 medicinal product Drugs 0.000 abstract 1
- 102000006255 nuclear receptors Human genes 0.000 abstract 1
- 108020004017 nuclear receptors Proteins 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
Classifications
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- 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
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/4192—1,2,3-Triazoles
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- 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
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- 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
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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- A61K31/42—Oxazoles
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
- C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring 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
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- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
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- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Obesity (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
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- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Vascular Medicine (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23511709P | 2009-08-19 | 2009-08-19 | |
| EP09010676A EP2289883A1 (en) | 2009-08-19 | 2009-08-19 | Novel FXR (NR1H4) binding and activity modulating compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2012000369A1 true CL2012000369A1 (es) | 2012-07-13 |
Family
ID=41137753
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2012000369A CL2012000369A1 (es) | 2009-08-19 | 2012-02-13 | Compuestos derivados de heterociclicos nitrogenados sustituidos, moduladores del receptor nr1h4(fxr); y uso para el tratamiento de trastornos hiperproliferativos malignos y no malignos, tratamiento de condiciones colestaticas cronicas intra y extrahepaticas, desordenes metabolicos en lipidos o diabetes, entre otros. |
Country Status (30)
Families Citing this family (80)
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| 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 |
| 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 |
| WO2013037482A1 (en) | 2011-09-15 | 2013-03-21 | Phenex Pharmaceuticals Ag | Farnesoid x receptor agonists for cancer treatment and prevention |
| WO2014001278A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| WO2014001279A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| WO2014001280A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| CN104411703A (zh) | 2012-06-26 | 2015-03-11 | 萨尼奥纳有限责任公司 | 苯基三唑衍生物及其调节gabaa受体复合体的用途 |
| MX357504B (es) | 2012-06-26 | 2018-07-12 | Saniona Aps | Derivado de feniltriazol y su uso para modular complejo del receptor gabaa. |
| JO3215B1 (ar) | 2012-08-09 | 2018-03-08 | Phenex Pharmaceuticals Ag | حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy |
| CN102976946A (zh) * | 2012-12-13 | 2013-03-20 | 烟台泰和新材料股份有限公司 | 合成间苯二甲酸二甲酯的方法 |
| CN103232378B (zh) * | 2013-04-27 | 2015-11-18 | 国家海洋局第三海洋研究所 | 一种含6-溴吲哚满二酮的荔枝螺提取物及制备方法与其抗癌应用 |
| AU2014320463B2 (en) | 2013-09-11 | 2018-08-02 | Centre National De La Recherche Scientifique (Cnrs) | Methods and pharmaceutical compositions for the treatment of hepatitis B virus infection |
| WO2016049069A1 (en) | 2014-09-24 | 2016-03-31 | Gilead Sciences, Inc. | Methods of treating liver disease |
| 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 |
| EP3034501A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Hydroxy containing FXR (NR1H4) modulating compounds |
| EA036404B1 (ru) | 2015-02-06 | 2020-11-06 | Интерсепт Фармасьютикалз, Инк. | Фармацевтические композиции для комбинированной терапии |
| 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 |
| PT3277286T (pt) | 2015-03-31 | 2021-07-01 | Enanta Pharm Inc | Derivados de ácidos biliares como agonistas de fxr/tgr5 e métodos de utilização destes |
| PE20180034A1 (es) | 2015-04-07 | 2018-01-09 | Intercept Pharmaceuticals Inc | Composiciones farmaceuticas para terapias combinadas |
| 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 |
| 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 |
| CN109152840A (zh) | 2016-03-28 | 2019-01-04 | 英特塞普特医药品公司 | 通过结合fxr激动剂和arb获得的药物 |
| 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 |
| 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 |
| AR108711A1 (es) * | 2016-06-13 | 2018-09-19 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4) |
| JP6678779B2 (ja) | 2016-06-13 | 2020-04-08 | ギリアード サイエンシーズ， インコーポレイテッド | Ｆｘｒ（ｎｒ１ｈ４）調節化合物 |
| 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 |
| CN106237332A (zh) * | 2016-08-11 | 2016-12-21 | 河南大学 | 核受体fxr在肝癌干细胞靶向治疗中的应用 |
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