ES2663948T3 - Moduladores de TGR5 y método de uso de los mismos - Google Patents
Moduladores de TGR5 y método de uso de los mismos Download PDFInfo
- Publication number
- ES2663948T3 ES2663948T3 ES13192394T ES13192394T ES2663948T3 ES 2663948 T3 ES2663948 T3 ES 2663948T3 ES 13192394 T ES13192394 T ES 13192394T ES 13192394 T ES13192394 T ES 13192394T ES 2663948 T3 ES2663948 T3 ES 2663948T3
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- groups
- alkyl
- hydrogen
- unsubstituted
- substituted
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- IGRCWJPBLWGNPX-UHFFFAOYSA-N 3-(2-chlorophenyl)-n-(4-chlorophenyl)-n,5-dimethyl-1,2-oxazole-4-carboxamide Chemical compound C=1C=C(Cl)C=CC=1N(C)C(=O)C1=C(C)ON=C1C1=CC=CC=C1Cl IGRCWJPBLWGNPX-UHFFFAOYSA-N 0.000 title 1
- 102100025353 G-protein coupled bile acid receptor 1 Human genes 0.000 title 1
- 101000857733 Homo sapiens G-protein coupled bile acid receptor 1 Proteins 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910006069 SO3H Inorganic materials 0.000 abstract 1
- 125000001931 aliphatic group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052736 halogen Chemical group 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- 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
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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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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- 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
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- 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
-
- 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
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- 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
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un compuesto de fórmula IIIA: **(Ver fórmula)** o una sal, solvato, o hidrato del mismo, en la que: R1 es hidrógeno, hidroxilo, o halógeno; R3 es hidroxilo, NH(CH2)mSO3H, o NH(CH2)nCO2H; R5 es alquilo sin sustituir o sustituido, o arilo; R6 es hidrógeno; o R5 y R6 tomados junto con los carbonos a los que están unidos forman un anillo con un tamaño de 3, 4, 5 o 6 átomos; R7 es hidrógeno, alquilo sin sustituir o sustituido, o hidroxilo; R8 es hidrógeno, o alquilo sin sustituir o sustituido; R9 es hidrógeno, o alquilo sin sustituir o sustituido; o R8 y R9 tomados junto con el átomo de carbono al que están unidos forman un carbonilo; R10 es R3 o SO3H; m es un número entero 0, 1, 2, 3, 4 o 5; y n es un número entero 0, 1, 2, 3, 4 o 5, en el que dicho alquilo incluye grupos alifáticos saturados, incluyendo grupos alquilo de cadena lineal, grupos alquilo de cadena ramificada, grupos cicloalquilo, grupos cicloalquilo sustituidos con alquilo, y grupos alquilo sustituidos con cicloalquilo, y en el que dicho arilo incluye grupos con aromaticidad, grupos arilo multicíclicos y heteroarilos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08169462 | 2008-11-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2663948T3 true ES2663948T3 (es) | 2018-04-17 |
Family
ID=41668454
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES13192394T Active ES2663948T3 (es) | 2008-11-19 | 2009-11-19 | Moduladores de TGR5 y método de uso de los mismos |
| ES09760057.1T Active ES2458168T3 (es) | 2008-11-19 | 2009-11-19 | Moduladores de TGR5 y método de uso de los mismos |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES09760057.1T Active ES2458168T3 (es) | 2008-11-19 | 2009-11-19 | Moduladores de TGR5 y método de uso de los mismos |
Country Status (23)
| Country | Link |
|---|---|
| US (5) | US8114862B2 (es) |
| EP (2) | EP2698375B1 (es) |
| JP (5) | JP5535233B2 (es) |
| KR (2) | KR101667436B1 (es) |
| CN (2) | CN102325784B (es) |
| AU (1) | AU2009316566B9 (es) |
| BR (1) | BRPI0921983B8 (es) |
| CA (1) | CA2744189C (es) |
| DK (2) | DK2376519T3 (es) |
| EA (2) | EA030681B1 (es) |
| ES (2) | ES2663948T3 (es) |
| HK (1) | HK1205132A1 (es) |
| HU (1) | HUE039171T2 (es) |
| IL (3) | IL212969A (es) |
| LT (1) | LT2698375T (es) |
| MX (1) | MX2011005295A (es) |
| NO (1) | NO2698375T3 (es) |
| PL (2) | PL2376519T3 (es) |
| PT (2) | PT2698375T (es) |
| SG (1) | SG10201400162QA (es) |
| SI (1) | SI2698375T1 (es) |
| WO (1) | WO2010059853A1 (es) |
| ZA (1) | ZA201104077B (es) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1392714T3 (da) | 2001-03-12 | 2006-01-09 | Intercept Pharmaceuticals Inc | Steroider som agonister for FXR |
| ES2609395T5 (es) | 2004-03-12 | 2021-08-06 | Intercept Pharmaceuticals Inc | Tratamiento de la fibrosis usando ligandos de Fxr |
| US10987362B2 (en) | 2004-03-12 | 2021-04-27 | Intercept Pharmaceuticals, Inc. | Treatment of fibrosis using FXR ligands |
| ITMI20050912A1 (it) | 2005-05-19 | 2006-11-20 | Erregierre Spa | Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici |
| EP2112995B1 (en) | 2007-01-19 | 2013-07-31 | Intercept Pharmaceuticals, Inc. | 23-substituted bile acids as tgr5 modulators and methods of use thereof |
| AU2009276507B2 (en) | 2008-07-30 | 2015-11-19 | Intercept Pharmaceuticals, Inc. | TGR5 modulators and methods of use thereof |
| ES2663948T3 (es) * | 2008-11-19 | 2018-04-17 | Intercept Pharmaceuticals, Inc. | Moduladores de TGR5 y método de uso de los mismos |
| US8318663B2 (en) | 2008-11-26 | 2012-11-27 | Satiogen Pharmaceuticals, Inc. | Methods of treating diabetes and/or obesity using an enteroendocrine peptide secretion enhancing agent |
| JP2012509891A (ja) | 2008-11-26 | 2012-04-26 | サティオゲン ファーマシューティカルズ，インク． | 肥満症及び糖尿病を治療するための胆汁酸再循環阻害剤 |
| ES2552657T3 (es) | 2010-05-26 | 2015-12-01 | Satiogen Pharmaceuticals, Inc. | Inhibidores del reciclado de ácidos biliares y saciógenos para el tratamiento de diabetes, obesidad, y afecciones gastrointestinales inflamatorias |
| MX382960B (es) | 2011-10-28 | 2025-03-13 | Shire Human Genetic Therapies | Inhibidores de la recirculación de ácidos biliares para el tratamiento de hipercolemia y enfermedad hepática colestásica. |
| EA030839B1 (ru) | 2011-10-28 | 2018-10-31 | ЛУМЕНА ФАРМАСЬЮТИКАЛС ЭлЭлСи | Ингибиторы рециклинга желчных кислот при лечении холестатических заболеваний печени у детей |
| WO2013192097A1 (en) | 2012-06-19 | 2013-12-27 | Intercept Pharmaceuticals, Inc. | Preparation, uses and solid forms of obeticholic acid |
| US9982008B2 (en) | 2012-06-19 | 2018-05-29 | Intercept Pharmaceuticals, Inc. | Preparation and uses of obeticholic acid |
| EP2906197A1 (en) | 2012-10-09 | 2015-08-19 | The Procter & Gamble Company | Method of identifying synergistic cosmetic combinations |
| EP2906946A1 (en) | 2012-10-09 | 2015-08-19 | The Procter & Gamble Company | Method of identifying or evaluating beneficial actives and compositions containing the same |
| EP3004132A4 (en) * | 2013-06-06 | 2017-01-18 | Yissum, Research Development Company of the Hebrew | Bile acid-basic amino acid conjugates and uses thereof |
| WO2014200349A1 (en) | 2013-06-13 | 2014-12-18 | Fast Forward Pharmaceutical B.V. | Cd40 signalling inhibitor and a further compound, wherein the further compound is a bile acid, a bile acid derivative, an tgr5-receptor agonist, an fxr agonist or a combination thereof, for the treatment of chronic inflammation, and the prevention of gastrointestinal cancer or fibrosis. |
| SI3071696T1 (sl) | 2013-11-22 | 2019-11-29 | Mina Therapeutics Ltd | C/EBP alfa kratko delujoči RNA sestavki in postopki uporabe |
| HRP20230170T1 (hr) * | 2014-05-29 | 2023-03-31 | Bar Pharmaceuticals S.R.L. | Derivati kolana za uporabu u liječenju i/ili prevenciji bolesti povezanih s fxr i tgr5/gpbar1 |
| US20180236064A1 (en) * | 2014-10-03 | 2018-08-23 | Mayo Foundation For Medical Education And Research | Targeting tgr5 to treat disease |
| WO2016073767A1 (en) * | 2014-11-06 | 2016-05-12 | Enanta Pharmaceuticals, Inc. | Bile acid analogs an fxr/tgr5 agonists and methods of use thereof |
| PT3221331T (pt) | 2014-11-19 | 2019-12-23 | Nzp Uk Ltd | Esteroides 6-alquil-7-hidroxi-4-en-3-ona como intermediários para a produção de moduladores de fxr esteroidais |
| US10538550B2 (en) | 2014-11-19 | 2020-01-21 | NZP UK Limited | 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal FXR modulators |
| WO2016079520A1 (en) | 2014-11-19 | 2016-05-26 | Dextra Laboratories Limited | 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators |
| CN107108687B (zh) | 2014-11-19 | 2019-10-29 | Nzp英国有限公司 | 作为制备类固醇FXR调节剂的中间体的5β-6-烷基-7-羟基-3-酮类固醇 |
| CN105985396A (zh) * | 2015-02-16 | 2016-10-05 | 苏州泽璟生物制药有限公司 | 氘代鹅去氧胆酸衍生物以及包含该化合物的药物组合物 |
| EP3290429A1 (en) * | 2015-04-28 | 2018-03-07 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Cholic acid derivative, and preparation method and medical use thereof |
| US10800807B2 (en) * | 2015-06-19 | 2020-10-13 | Intercept Pharmaceuticals, Inc. | TGR5 modulators and methods of use thereof |
| TW201700447A (zh) * | 2015-06-19 | 2017-01-01 | 英特賽普醫藥品公司 | Tgr5調控劑及其用法 |
| WO2017053826A1 (en) * | 2015-09-24 | 2017-03-30 | Intercept Pharmaceuticals, Inc. | Methods and intermediates for the preparation bile acid derivatives |
| EP3981779A1 (en) * | 2015-10-07 | 2022-04-13 | Intercept Pharmaceuticals, Inc. | Farnesoid x receptor modulators |
| CN109467585A (zh) * | 2016-03-11 | 2019-03-15 | 深圳市塔吉瑞生物医药有限公司 | 用于预防或治疗fxr-介导疾病的胆烷酸化合物 |
| US10369160B2 (en) | 2016-04-13 | 2019-08-06 | Intercept Pharmaceuticals, Inc. | Methods of treating cancer |
| GB201608777D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Compounds |
| EP3465218A4 (en) | 2016-05-29 | 2020-06-17 | Human Metabolomics Institute, Inc. | BIOMARKERS RELATED TO HEPATIC DISEASES AND METHODS OF USE |
| US10654834B2 (en) * | 2016-07-01 | 2020-05-19 | Venenum Biodesign, LLC | Non-systemic TGR5 agonists |
| WO2018222701A1 (en) * | 2017-05-30 | 2018-12-06 | Intercept Pharmaceuticals, Inc. | Treatment of renal diseases with a bile acid derivative |
| CN109021056B (zh) * | 2017-06-09 | 2021-03-09 | 博瑞生物医药（苏州）股份有限公司 | 法尼酯x受体激动剂 |
| BR112020001362A2 (pt) | 2017-07-24 | 2020-08-11 | Intercept Pharmaceuticals, Inc. | derivados de ácido biliar isotopicamente marcados |
| EP3679138B1 (en) | 2017-09-08 | 2023-03-22 | MiNA Therapeutics Limited | Hnf4a sarna compositions and methods of use |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| WO2020163201A1 (en) * | 2019-02-04 | 2020-08-13 | Intercept Pharmaceuticals, Inc. | Treatment and prevention of intestinal inflammatory diseases with a bile acid derivative |
| CN116925168A (zh) * | 2019-08-23 | 2023-10-24 | 深圳云合医药科技合伙企业(有限合伙) | 胆汁酸衍生物及其组合物和应用 |
| MX2022004142A (es) | 2019-10-07 | 2022-09-21 | Kallyope Inc | Agonistas de gpr119. |
| TW202140440A (zh) | 2020-02-28 | 2021-11-01 | 美商克力歐普股份有限公司 | Gpr40激動劑 |
| WO2021236617A1 (en) | 2020-05-19 | 2021-11-25 | Kallyope, Inc. | Ampk activators |
| CA3183575A1 (en) | 2020-06-26 | 2021-12-30 | Iyassu Sebhat | Ampk activators |
| KR102693566B1 (ko) * | 2020-07-03 | 2024-08-08 | 주식회사 큐라클 | 지방간 질환의 예방 또는 치료를 위한 약학적 조성물 |
| CN113774142A (zh) * | 2021-10-11 | 2021-12-10 | 北京化工大学 | Tgr5在制备治疗肠癌药物及诊断性试剂盒中的应用 |
Family Cites Families (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3366932D1 (en) | 1982-07-29 | 1986-11-20 | Lehner Ag | New derivatives of biliary acids, process for the production thereof and pharmaceutical compositions containing the same |
| IT1206112B (it) | 1983-04-29 | 1989-04-14 | Lehner Ag | Nuovi derivati di acidi biliari, procedimento per la loro preparazione e relative composizioni farmaceutiche. |
| IT1212835B (it) | 1983-08-18 | 1989-11-30 | Lehner Ag | Derivati di acidi biliari, procedimento per la loro preparazione e relative composizioni farmaceutiche. |
| US4892868A (en) * | 1984-08-17 | 1990-01-09 | Gipharmex, S.P.A. | Derivatives of biliary acids, process for the production thereof and corresponding pharmaceutical compositions |
| IT1196377B (it) | 1984-12-21 | 1988-11-16 | Lehner Ag | Derivati di acidi biliari,procedimento per la loro preparazione e relative composizioni farmaceutiche |
| IT1223313B (it) | 1987-10-20 | 1990-09-19 | Gipharmex Spa | Derivati di acidi biliari loro preparazione e composizioni farmaceutiche che li contengono |
| US5175320A (en) | 1989-04-17 | 1992-12-29 | Giuliani S.P.A. | Fluorinated bile acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them |
| IT1229570B (it) | 1989-04-17 | 1991-09-04 | Giuliani Spa | Derivati fluorurati di acidi biliari, loro preparazione e composizioni farmaceutiche che li contengono. |
| DE69018592T2 (de) | 1989-12-13 | 1995-10-05 | Mitsubishi Chem Corp | Pyrazolylacrylsäure-Derivate, verwendbar als systemische Fungiziden in Pflanzen- und Materialschutz. |
| AU1856997A (en) | 1996-02-02 | 1997-08-22 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
| GB9604242D0 (en) | 1996-02-28 | 1996-05-01 | Glaxo Wellcome Inc | Chemical compounds |
| GB9606805D0 (en) | 1996-03-30 | 1996-06-05 | Glaxo Wellcome Inc | Medicaments |
| US5689791A (en) | 1996-07-01 | 1997-11-18 | Xerox Corporation | Electrically conductive fibers |
| JP2000514807A (ja) | 1996-07-12 | 2000-11-07 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | レプチン耐性の新規な治療 |
| US6008237A (en) | 1997-12-19 | 1999-12-28 | Merck & Co., Inc. | Arylthiazolidinedione derivatives |
| WO1999038845A1 (en) | 1998-01-29 | 1999-08-05 | Tularik Inc. | Ppar-gamma modulators |
| AU1229000A (en) | 1998-10-23 | 2000-05-15 | Glaxo Group Limited | Assays for ligands for nuclear receptors |
| JP2002532729A (ja) | 1998-12-23 | 2002-10-02 | グラクソ グループ リミテッド | 核内受容体のリガンドのアッセイ |
| AU2409600A (en) | 1999-01-07 | 2000-07-24 | Tularik Inc. | Fxr receptor-mediated modulation of cholesterol metabolism |
| US20020132223A1 (en) | 1999-03-26 | 2002-09-19 | City Of Hope | Methods for modulating activity of the FXR nuclear receptor |
| EP1473042B1 (en) | 1999-03-26 | 2006-06-21 | City of Hope | Screening for FXR receptor modulators |
| WO2000057915A1 (en) | 1999-03-26 | 2000-10-05 | City Of Hope | Method of affecting cholesterol catabolism using nuclear bile acid receptor |
| WO2000076523A1 (en) | 1999-06-11 | 2000-12-21 | Allergan Sales, Inc. | Methods for modulating fxr receptor activity |
| US6906057B1 (en) | 1999-06-11 | 2005-06-14 | Allergan, Inc. | Methods for modulating FXR receptor activity |
| US6559188B1 (en) | 1999-09-17 | 2003-05-06 | Novartis Ag | Method of treating metabolic disorders especially diabetes, or a disease or condition associated with diabetes |
| WO2001030343A1 (en) | 1999-10-22 | 2001-05-03 | Merck & Co., Inc. | Pharmaceuticals for treating obesity |
| CA2401290A1 (en) | 2000-04-12 | 2001-10-18 | Takeda Chemical Industries, Ltd. | Novel g protein-coupled receptor protein and dna thereof |
| US6627636B2 (en) | 2000-06-15 | 2003-09-30 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors and method |
| AU2001288623A1 (en) | 2000-09-05 | 2002-03-22 | Tularik, Inc. | Fxr modulators |
| US20020119958A1 (en) | 2001-02-13 | 2002-08-29 | Shinichiro Tojo | Therapeutic agent for hyperlipidemia |
| DK1392714T3 (da) | 2001-03-12 | 2006-01-09 | Intercept Pharmaceuticals Inc | Steroider som agonister for FXR |
| US7354726B2 (en) | 2001-04-12 | 2008-04-08 | Takeda Pharmaceutical Company Limited | Screening method |
| US20070010562A1 (en) | 2001-08-13 | 2007-01-11 | Ulrike Bauer | Nr1h4 nuclear receptor binding compounds |
| ATE381542T1 (de) | 2001-08-13 | 2008-01-15 | Phenex Pharmaceuticals Ag | Nr1h4-kern-rezeptor-bindende verbindungen |
| EP1423113A4 (en) | 2001-08-13 | 2007-04-18 | Phenex Pharmaceuticals Ag | NR1H4 NUCLEAR RECEPTOR BINDING COMPOUNDS |
| US20030144360A1 (en) | 2001-11-19 | 2003-07-31 | Allergan Sales, Inc. | Composition and method for modulating BAR/FXR receptor activity |
| AU2003225903A1 (en) | 2002-03-21 | 2003-10-08 | Curagen Corporation | Methods of using farnesoid x receptor (fxr) agonists |
| WO2003086303A2 (en) | 2002-04-12 | 2003-10-23 | The University Of Chicago | Farnesoid x-activated receptor agonists |
| US6987121B2 (en) | 2002-04-25 | 2006-01-17 | Smithkline Beecham Corporation | Compositions and methods for hepatoprotection and treatment of cholestasis |
| RU2310620C2 (ru) | 2002-06-19 | 2007-11-20 | Аваилвс Корпорейшн | Стеновой материал из искусственного камня |
| ITMI20021532A1 (it) | 2002-07-12 | 2004-01-12 | Roberto Pellicciari | Composti chimici |
| US7319109B2 (en) | 2002-11-22 | 2008-01-15 | Smith Kline Beecham Corporation | Farnesoid X receptor agonists |
| WO2004067008A1 (ja) | 2003-01-28 | 2004-08-12 | Takeda Pharmaceutical Company Limited | 受容体作動薬 |
| US20070015796A1 (en) | 2003-09-26 | 2007-01-18 | Smithkline Beecham Corporation | Compositions and methods for treatment of fibrosis |
| EP1568706A1 (en) | 2004-02-26 | 2005-08-31 | Intercept Pharmaceuticals, Inc. | Novel steroid agonist for FXR |
| ES2609395T5 (es) | 2004-03-12 | 2021-08-06 | Intercept Pharmaceuticals Inc | Tratamiento de la fibrosis usando ligandos de Fxr |
| ITMI20050912A1 (it) | 2005-05-19 | 2006-11-20 | Erregierre Spa | Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici |
| AU2007265457C1 (en) | 2006-06-27 | 2012-11-29 | Intercept Pharmaceuticals, Inc. | Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions |
| EP2112995B1 (en) * | 2007-01-19 | 2013-07-31 | Intercept Pharmaceuticals, Inc. | 23-substituted bile acids as tgr5 modulators and methods of use thereof |
| EP1947108A1 (en) | 2007-01-19 | 2008-07-23 | Intercept Pharmaceuticals, Inc. | TGR5 modulators and methods of use thereof |
| ES2663948T3 (es) * | 2008-11-19 | 2018-04-17 | Intercept Pharmaceuticals, Inc. | Moduladores de TGR5 y método de uso de los mismos |
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