IL157816A0 - Steroids as agonists for fxr - Google Patents
Steroids as agonists for fxrInfo
- Publication number
- IL157816A0 IL157816A0 IL15781602A IL15781602A IL157816A0 IL 157816 A0 IL157816 A0 IL 157816A0 IL 15781602 A IL15781602 A IL 15781602A IL 15781602 A IL15781602 A IL 15781602A IL 157816 A0 IL157816 A0 IL 157816A0
- Authority
- IL
- Israel
- Prior art keywords
- fxr
- agonists
- steroids
- compounds
- formula
- Prior art date
Links
- 239000000556 agonist Substances 0.000 title 1
- 150000003431 steroids Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 229940121360 farnesoid X receptor (fxr) agonists Drugs 0.000 abstract 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- A61P9/10—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
-
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- External Artificial Organs (AREA)
- Solid-Sorbent Or Filter-Aiding Compositions (AREA)
- Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27495901P | 2001-03-12 | 2001-03-12 | |
| PCT/EP2002/001832 WO2002072598A1 (en) | 2001-03-12 | 2002-02-21 | Steroids as agonists for fxr |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL157816A0 true IL157816A0 (en) | 2004-03-28 |
Family
ID=23050302
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL15781602A IL157816A0 (en) | 2001-03-12 | 2002-02-21 | Steroids as agonists for fxr |
| IL157816A IL157816A (en) | 2001-03-12 | 2003-09-09 | Bile acids and their persistence with amino acid in FXR agonists |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL157816A IL157816A (en) | 2001-03-12 | 2003-09-09 | Bile acids and their persistence with amino acid in FXR agonists |
Country Status (16)
| Country | Link |
|---|---|
| US (9) | US7138390B2 (enExample) |
| EP (1) | EP1392714B1 (enExample) |
| JP (2) | JP4021327B2 (enExample) |
| AT (1) | ATE303399T1 (enExample) |
| AU (1) | AU2002308295B2 (enExample) |
| BE (1) | BE2017C018I2 (enExample) |
| CA (1) | CA2440680C (enExample) |
| CY (1) | CY2017020I1 (enExample) |
| DE (1) | DE60205891T2 (enExample) |
| DK (1) | DK1392714T3 (enExample) |
| ES (1) | ES2248581T3 (enExample) |
| FR (1) | FR17C0003I2 (enExample) |
| IL (2) | IL157816A0 (enExample) |
| NL (1) | NL300877I2 (enExample) |
| NO (2) | NO326134B1 (enExample) |
| WO (1) | WO2002072598A1 (enExample) |
Families Citing this family (112)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1392714B1 (en) | 2001-03-12 | 2005-08-31 | Intercept Pharmaceuticals, Inc. | Steroids as agonists for fxr |
| US6696473B2 (en) | 2001-12-21 | 2004-02-24 | X-Ceptor Therapeutics, Inc. | Heterocyclic modulators of nuclear receptors |
| 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 |
| ES2533993T3 (es) | 2004-03-12 | 2015-04-16 | Intercept Pharmaceuticals, Inc. | Tratamiento de fibrosis usando ligandos de FXR |
| US10987362B2 (en) | 2004-03-12 | 2021-04-27 | Intercept Pharmaceuticals, Inc. | Treatment of fibrosis using FXR ligands |
| 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 |
| SI2040713T1 (sl) | 2006-06-27 | 2014-11-28 | Intercept Pharmaceuticals, Inc. | Derivati žolčne kisline kot FXR ligandi za preprečevanje ali zdravljenje bolezni ali stanj, posredovanih s FXR |
| 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 |
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| CN104370990A (zh) | 2008-11-19 | 2015-02-25 | 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 |
| WO2010069604A1 (en) | 2008-12-19 | 2010-06-24 | Royal College Of Surgeons In Ireland | Treatment of diarrhoea |
| US9982008B2 (en) | 2012-06-19 | 2018-05-29 | Intercept Pharmaceuticals, Inc. | Preparation and uses of obeticholic acid |
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| BR112015012312A2 (pt) * | 2012-11-28 | 2017-07-11 | Intercept Pharmaceuticals Inc | método de tratamento, redução do risco, prevenção ou alívio de uma afecção ou doença pulmonar em um sujeito; método de redução ou supressão de inflamação no pulmão em um sujeito; e método de promoção de reparo pulmonar em um sujeito |
| AU2014278833A1 (en) | 2013-06-13 | 2016-01-07 | Fast Forward Pharmaceuticals 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. |
| ES2846183T3 (es) * | 2013-09-11 | 2021-07-28 | Inst Nat Sante Rech Med | Métodos y composiciones farmacéuticas para el tratamiento de la infección por el virus de la hepatitis 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 |
| MX388957B (es) * | 2014-05-29 | 2025-03-20 | Bar Pharmaceuticals S R L | Derivados del colano para uso en el tratamiento y/o prevencion de enfermedades en las que intervienen el fxr y el 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 |
| JP6724004B2 (ja) | 2014-11-19 | 2020-07-15 | エヌゼットピー ユーケー リミテッド | ステロイドFXRモジュレーター製造のための中間体としての5β−6−アルキル−7−ヒドロキシ−3−オンステロイド |
| EA034739B1 (ru) * | 2014-11-19 | 2020-03-16 | ЭнЗедПи ЮКей ЛИМИТЕД | 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr |
| EA033427B1 (ru) | 2014-11-19 | 2019-10-31 | Nzp Uk Ltd | 6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr |
| MX381239B (es) | 2014-11-19 | 2025-03-12 | Nzp Uk Ltd | Esteroides de 6.alfa.-alquil-6,7-diona como intermedios para la producción de moduladores esteroideos del receptor x farnesoide (fxr). |
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| KR20170099909A (ko) | 2014-11-26 | 2017-09-01 | 이난타 파마슈티칼스, 인코포레이티드 | Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법 |
| US11578097B2 (en) | 2014-11-26 | 2023-02-14 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof |
| CN105801653B (zh) * | 2014-12-30 | 2018-04-17 | 苏州晶云药物科技有限公司 | 奥贝胆酸的晶型a及其制备方法 |
| CN104672290B (zh) * | 2015-01-05 | 2017-06-06 | 北京普禄德医药科技有限公司 | 一种用于预防或治疗fxr‑介导的疾病的药物及其制备方法和用途 |
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| CN106589039B (zh) * | 2015-10-15 | 2019-12-17 | 苏州朗科生物技术股份有限公司 | 一种奥贝胆酸的制备方法及相关化合物 |
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| ES2901598T3 (es) | 2016-03-31 | 2022-03-23 | Intercept Pharmaceuticals Inc | Comprimido recubierto con película que tiene una alta estabilidad química del ingrediente activo |
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- 2002-02-21 EP EP02750526A patent/EP1392714B1/en not_active Expired - Lifetime
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- 2002-02-21 AU AU2002308295A patent/AU2002308295B2/en active Active
- 2002-02-21 DK DK02750526T patent/DK1392714T3/da active
- 2002-02-21 US US16/448,503 patent/USRE48286E1/en active Active
- 2002-02-21 WO PCT/EP2002/001832 patent/WO2002072598A1/en not_active Ceased
- 2002-02-21 ES ES02750526T patent/ES2248581T3/es not_active Expired - Lifetime
- 2002-02-21 JP JP2002571512A patent/JP4021327B2/ja not_active Expired - Lifetime
- 2002-02-21 AT AT02750526T patent/ATE303399T1/de active
- 2002-02-21 IL IL15781602A patent/IL157816A0/xx unknown
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- 2003-09-09 IL IL157816A patent/IL157816A/en active Protection Beyond IP Right Term
- 2003-09-11 NO NO20034011A patent/NO326134B1/no not_active IP Right Cessation
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- 2006-11-21 US US11/602,307 patent/US7786102B2/en not_active Expired - Lifetime
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- 2007-06-20 JP JP2007162928A patent/JP2007269815A/ja active Pending
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- 2009-08-25 US US12/547,147 patent/US8058267B2/en not_active Expired - Fee Related
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- 2011-11-03 US US13/288,558 patent/US8377916B2/en not_active Expired - Fee Related
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- 2015-02-26 US US14/632,139 patent/US20150166598A1/en not_active Abandoned
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- 2016-02-05 US US15/016,802 patent/US9732117B2/en not_active Expired - Fee Related
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- 2017-06-07 FR FR17C0003C patent/FR17C0003I2/fr active Active
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