ES2248581T3 - Esteroides como agonistas de fxr. - Google Patents
Esteroides como agonistas de fxr.Info
- Publication number
- ES2248581T3 ES2248581T3 ES02750526T ES02750526T ES2248581T3 ES 2248581 T3 ES2248581 T3 ES 2248581T3 ES 02750526 T ES02750526 T ES 02750526T ES 02750526 T ES02750526 T ES 02750526T ES 2248581 T3 ES2248581 T3 ES 2248581T3
- Authority
- ES
- Spain
- Prior art keywords
- compound
- formula
- baselineskip
- ethyl
- compound according
- 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.)
- Expired - Lifetime
Links
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Classifications
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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
- C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
- C07C215/08—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
- C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
- C07C215/10—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
- C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
- C07C215/12—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic the nitrogen atom of the amino group being further bound to hydrocarbon groups substituted by hydroxy groups
-
- 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
- C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- 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
Landscapes
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- Engineering & Computer Science (AREA)
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- Hematology (AREA)
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- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
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- Gastroenterology & Hepatology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
- External Artificial Organs (AREA)
- Solid-Sorbent Or Filter-Aiding Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
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| US27495901P | 2001-03-12 | 2001-03-12 | |
| US274959P | 2001-03-12 |
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| ES2248581T3 true ES2248581T3 (es) | 2006-03-16 |
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| Application Number | Title | Priority Date | Filing Date |
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| ES02750526T Expired - Lifetime ES2248581T3 (es) | 2001-03-12 | 2002-02-21 | Esteroides como agonistas de fxr. |
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| Country | Link |
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| US (9) | USRE48286E1 (OSRAM) |
| EP (1) | EP1392714B1 (OSRAM) |
| JP (2) | JP4021327B2 (OSRAM) |
| AT (1) | ATE303399T1 (OSRAM) |
| AU (1) | AU2002308295B2 (OSRAM) |
| BE (1) | BE2017C018I2 (OSRAM) |
| CA (1) | CA2440680C (OSRAM) |
| CY (1) | CY2017020I1 (OSRAM) |
| DE (1) | DE60205891T2 (OSRAM) |
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| ES (1) | ES2248581T3 (OSRAM) |
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| IL (2) | IL157816A0 (OSRAM) |
| NL (1) | NL300877I2 (OSRAM) |
| NO (2) | NO326134B1 (OSRAM) |
| WO (1) | WO2002072598A1 (OSRAM) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| DE60205891T2 (de) * | 2001-03-12 | 2006-06-22 | Intercept Pharmaceuticals, Inc. | Steroide als agonisten für fxr |
| ATE521599T1 (de) | 2001-12-21 | 2011-09-15 | X Ceptor Therapeutics Inc | Heterocyclische modulatoren von nukleären rezeptoren |
| US6987121B2 (en) * | 2002-04-25 | 2006-01-17 | Smithkline Beecham Corporation | Compositions and methods for hepatoprotection and treatment of cholestasis |
| ITMI20021532A1 (it) * | 2002-07-12 | 2004-01-12 | Roberto Pellicciari | Composti chimici |
| US10987362B2 (en) | 2004-03-12 | 2021-04-27 | Intercept Pharmaceuticals, Inc. | Treatment of fibrosis using FXR ligands |
| ES2609395T5 (es) | 2004-03-12 | 2021-08-06 | Intercept Pharmaceuticals Inc | Tratamiento de la fibrosis usando ligandos de Fxr |
| WO2005092328A1 (ja) * | 2004-03-29 | 2005-10-06 | Japan Health Sciences Foundation | Ｆｘｒ活性化化合物 |
| 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 |
| US7618956B2 (en) | 2005-05-31 | 2009-11-17 | The Gillette Company | Reduction of hair growth |
| EP2040713B1 (en) | 2006-06-27 | 2014-06-18 | Intercept Pharmaceuticals Inc. | Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated deseases or conditions |
| EP1886685A1 (en) | 2006-08-11 | 2008-02-13 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods, uses and compositions for modulating replication of hcv through the farnesoid x receptor (fxr) activation or inhibition |
| KR100846441B1 (ko) * | 2006-12-22 | 2008-07-16 | 재단법인서울대학교산학협력재단 | 스테롤 계 유도체를 함유하는 약제학적 조성물, 건강식품조성물, 화장품 조성물 및 파나소이드 엑스 핵 수용체 활성억제제 조성물 |
| CN101679476B (zh) | 2007-01-19 | 2014-05-07 | 英特塞普特医药品公司 | 23取代的胆汁酸作为tgr5调节剂及其使用方法 |
| US8338628B2 (en) * | 2007-08-28 | 2012-12-25 | City Of Hope | Method of synthesizing alkylated bile acid derivatives |
| AU2009276507B2 (en) | 2008-07-30 | 2015-11-19 | Intercept Pharmaceuticals, Inc. | TGR5 modulators and methods of use thereof |
| CN102325784B (zh) | 2008-11-19 | 2014-11-19 | 英特塞普特医药品公司 | G蛋白偶联受体5(tgr5)调节剂及其使用方法 |
| US20110257139A1 (en) | 2008-12-19 | 2011-10-20 | Royal College Of Surgeons In Ireland | Treatment of diarrhoea |
| CN104781272A (zh) | 2012-06-19 | 2015-07-15 | 英特塞普特医药品公司 | 奥贝胆酸的制备、用途和固体形式 |
| US9982008B2 (en) | 2012-06-19 | 2018-05-29 | Intercept Pharmaceuticals, Inc. | Preparation and uses of obeticholic acid |
| US9777038B2 (en) * | 2012-10-26 | 2017-10-03 | Intercept Pharmaceuticals, Inc. | Process for preparing bile acid derivatives |
| AU2013352288B2 (en) * | 2012-11-28 | 2017-11-23 | Intercept Pharmaceuticals, Inc. | Treatment of pulmonary disease |
| CN105636984A (zh) | 2013-06-13 | 2016-06-01 | 法斯特弗沃德制药有限公司 | 用于治疗慢性炎症和预防胃肠道癌或纤维化的cd40信号转导抑制剂和其他化合物，该其他化合物是胆汁酸、胆汁酸衍生物、tgr5受体激动剂、fxr激动剂或其组合 |
| HRP20201953T1 (hr) * | 2013-09-11 | 2021-04-30 | Institut National De La Santé Et De La Recherche Médicale (Inserm) | Postupci i farmaceutski pripravci za liječenje virusne infekcije hepatitisom b |
| EP3985118A1 (en) | 2013-11-22 | 2022-04-20 | MiNA Therapeutics Limited | C/ebp alpha short activating rna compositions and methods of use |
| CN104876995B (zh) * | 2014-02-27 | 2016-09-07 | 人福医药集团股份公司 | 鹅去氧胆酸衍生物的制备方法 |
| ES2938874T3 (es) | 2014-05-29 | 2023-04-17 | Bar Pharmaceuticals S R L | Derivados de colano para su uso en el tratamiento y/o prevención de enfermedades mediadas por FXR y TGR5/GPBAR1 |
| EP3006557A1 (en) | 2014-10-07 | 2016-04-13 | Heinrich-Heine-Universität Düsseldorf | Bile acids for inducing hepatic differentiation |
| CN105585603B (zh) * | 2014-10-21 | 2019-05-24 | 重庆医药工业研究院有限责任公司 | 一种制备奥贝胆酸中间体的方法 |
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| CN105669811B (zh) * | 2014-11-17 | 2020-09-04 | 正大天晴药业集团股份有限公司 | 新的7-酮-6β-烷基胆烷酸衍生物在制备奥贝胆酸以及其在医药领域的用途 |
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