CL2016000982A1 - Compuestos derivados de 1,4-dihidrocromeno[4,3-c]-pirazol, 1h-pirazol[4,3-f o 3,4-f]-quinolina, 1h-benzo[g]-indazol, que median una afección por fxr; composiciones y combinaciones farmacológicas; útiles para el tratamiento de una enfermedad hepática, tales como colestasis intrahepática, inducida por los estrógenos, por fármacos, inducida por fármacos, asociada al embarazo, asociada a nutrición parenteral, entre otras. - Google Patents
Compuestos derivados de 1,4-dihidrocromeno[4,3-c]-pirazol, 1h-pirazol[4,3-f o 3,4-f]-quinolina, 1h-benzo[g]-indazol, que median una afección por fxr; composiciones y combinaciones farmacológicas; útiles para el tratamiento de una enfermedad hepática, tales como colestasis intrahepática, inducida por los estrógenos, por fármacos, inducida por fármacos, asociada al embarazo, asociada a nutrición parenteral, entre otras.Info
- Publication number
- CL2016000982A1 CL2016000982A1 CL2016000982A CL2016000982A CL2016000982A1 CL 2016000982 A1 CL2016000982 A1 CL 2016000982A1 CL 2016000982 A CL2016000982 A CL 2016000982A CL 2016000982 A CL2016000982 A CL 2016000982A CL 2016000982 A1 CL2016000982 A1 CL 2016000982A1
- Authority
- CL
- Chile
- Prior art keywords
- induced
- fxr
- treatment
- liver disease
- compounds derived
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
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- 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
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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- 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
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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- 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
- A61K31/44—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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- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/06—Peri-condensed systems
-
- 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
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Chemical & Material Sciences (AREA)
- Health & Medical 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)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Otolaryngology (AREA)
- Hospice & Palliative Care (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
Abstract
COMPUESTOS HETEROCICLICOS DERIVADOS DE ACIDOS CARBOXILICOS SUSTITUIDOS, MODULADORES DE RECEPTORES X FARNESOIDES (FXR); COMPOSICION FARMACEUTICA; COMBINACION FARMACEUTICA; USO EN EL TRATAMIENTO DE ENFERMEDAD HEPATICA, TAL COMO ENFERMEDAD DE HIGADO GRASO NO ALCOHOLICO O ESTEATOHEPATITIS NO ALCOHOLICA, Y DE ENFERMEDAD GASTROINTESTINAL SELECCIONADA DE DIARREA POR MALABSORCION DE ACIDOS BILIARES, GASTRITIS POR REFLUJO DE BILIS Y ENFERMEDAD INFLAMATORIA DEL INTESTINO.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361900013P | 2013-11-05 | 2013-11-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2016000982A1 true CL2016000982A1 (es) | 2016-10-07 |
Family
ID=51982773
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2016000982A CL2016000982A1 (es) | 2013-11-05 | 2016-04-25 | Compuestos derivados de 1,4-dihidrocromeno[4,3-c]-pirazol, 1h-pirazol[4,3-f o 3,4-f]-quinolina, 1h-benzo[g]-indazol, que median una afección por fxr; composiciones y combinaciones farmacológicas; útiles para el tratamiento de una enfermedad hepática, tales como colestasis intrahepática, inducida por los estrógenos, por fármacos, inducida por fármacos, asociada al embarazo, asociada a nutrición parenteral, entre otras. |
Country Status (42)
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11344540B2 (en) | 2016-02-22 | 2022-05-31 | Novartis Ag | Methods for treating liver disorders using FXR agonists |
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| 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 |
| BR112016009630B1 (pt) | 2013-11-05 | 2021-02-09 | Novartis Ag | receptores de farnesoide x, seus usos, combinação e composição farmacêutica |
| 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 |
| 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 |
| 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). |
| RU2019110779A (ru) * | 2016-09-14 | 2020-10-15 | Новартис Аг | Новые схемы введения агонистов fxr |
| PE20190972A1 (es) * | 2016-09-14 | 2019-07-09 | Novartis Ag | Combinacion de agonistas de fxr |
| RU2019113150A (ru) * | 2016-10-05 | 2020-11-06 | Новартис Аг | Комбинация композиций, содержащих агонисты fxr, предназначенная для лечения или предупреждения фиброзирующего, цирротического заболевания или нарушения |
| CN107973790A (zh) * | 2016-10-22 | 2018-05-01 | 合帕吉恩治疗公司 | 杂环fxr调节剂 |
| PT3600309T (pt) | 2017-03-28 | 2022-10-03 | Gilead Sciences Inc | Combinações terapêuticas para o tratamento de doenças hepáticas |
| KR102643558B1 (ko) * | 2017-06-05 | 2024-03-06 | 내셔널 유니버시티 오브 싱가포르 | 인간 트레포일 인자 3을 억제하는데 유용한 화합물 |
| EP3668843A1 (en) | 2017-08-15 | 2020-06-24 | Inflazome Limited | Sulfonylureas and sulfonylthioureas as nlrp3 inhibitors |
| MA49903A (fr) * | 2017-08-15 | 2020-06-24 | Inflazome Ltd | Sulfonylureés et sulfonylthioureés en tant qu'inhibiteurs de nlrp3 |
| UY37848A (es) | 2017-08-15 | 2019-03-29 | Inflazome Ltd | Sulfonilureas y sulfoniltioureas útiles como inhibidores de nlrp3 |
| US20200276178A1 (en) * | 2017-09-13 | 2020-09-03 | Novartis Ag | Combinations comprising fxr agonists |
| CN111315733A (zh) | 2017-11-09 | 2020-06-19 | 英夫拉索姆有限公司 | 新颖磺酰胺甲酰胺化合物 |
| WO2019092171A1 (en) | 2017-11-09 | 2019-05-16 | Inflazome Limited | Novel sulfonamide carboxamide compounds |
| 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 |
| US11905252B2 (en) | 2018-03-02 | 2024-02-20 | Inflazome Limited | Compounds |
| MA53388A (fr) | 2018-07-25 | 2021-06-02 | Novartis Ag | Inhibiteurs d'inflammasome nlrp3 |
| EP3911647B1 (en) | 2019-01-15 | 2023-12-13 | Gilead Sciences, Inc. | Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same |
| US10610280B1 (en) | 2019-02-02 | 2020-04-07 | Ayad K. M. Agha | Surgical method and apparatus for destruction and removal of intraperitoneal, visceral, and subcutaneous fat |
| CA3233305A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| UY38687A (es) | 2019-05-17 | 2023-05-15 | Novartis Ag | Inhibidores del inflamasoma nlrp3, composiciones, combinaciones de los mismos y métodos para su uso |
| KR20220035365A (ko) | 2019-07-18 | 2022-03-22 | 엔요 파마 | 인터페론의 부작용을 감소시키는 방법 |
| WO2021044351A1 (en) | 2019-09-06 | 2021-03-11 | Novartis Ag | Methods of treating liver disease using lta4h 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 |
| CN113387828A (zh) * | 2020-03-14 | 2021-09-14 | 江巨东 | 一种阿利克仑中间体的制备方法 |
| WO2022037663A1 (zh) * | 2020-08-21 | 2022-02-24 | 苏州晶云药物科技股份有限公司 | 苯甲酸衍生物的新晶型及其制备方法 |
| JP2024502673A (ja) | 2021-01-14 | 2024-01-22 | ウエヌイグレックオ・ファーマ | Ｈｂｖ感染の処置のためのｆｘｒアゴニストとｉｆｎの相乗効果 |
| 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 |
| UY40374A (es) | 2022-08-03 | 2024-02-15 | Novartis Ag | Inhibidores de inflamasoma nlrp3 |
| IL319132A (en) * | 2022-08-26 | 2025-04-01 | Celmatix Inc | New FSHR modulators and their uses |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050143449A1 (en) * | 2002-11-15 | 2005-06-30 | The Salk Institute For Biological Studies | Non-steroidal farnesoid X receptor modulators and methods for the use thereof |
| CN101448791B (zh) * | 2006-05-24 | 2011-11-16 | 伊莱利利公司 | Fxr激动剂 |
| WO2008033534A2 (en) * | 2006-09-15 | 2008-03-20 | Thales Avionics, Inc. | System and method for wirelessly transferring content to and from an aircraft |
| TW200906823A (en) * | 2007-07-16 | 2009-02-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
| 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 |
| BR112016009630B1 (pt) | 2013-11-05 | 2021-02-09 | Novartis Ag | receptores de farnesoide x, seus usos, combinação e composição farmacêutica |
| 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 |
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- 2018-08-07 US US16/056,881 patent/US10683271B2/en active Active
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2021
- 2021-04-21 US US17/236,596 patent/US20210253534A1/en not_active Abandoned
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11344540B2 (en) | 2016-02-22 | 2022-05-31 | Novartis Ag | Methods for treating liver disorders using FXR agonists |
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