BE2017C018I2 - - Google Patents
Download PDFInfo
- Publication number
- BE2017C018I2 BE2017C018I2 BE2017C018C BE2017C018C BE2017C018I2 BE 2017C018 I2 BE2017C018 I2 BE 2017C018I2 BE 2017C018 C BE2017C018 C BE 2017C018C BE 2017C018 C BE2017C018 C BE 2017C018C BE 2017C018 I2 BE2017C018 I2 BE 2017C018I2
- Authority
- BE
- Belgium
- Prior art keywords
- compounds
- formula
- solvates
- allyl
- propyl
- Prior art date
Links
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Solid-Sorbent Or Filter-Aiding Compositions (AREA)
- External Artificial Organs (AREA)
- Immobilizing And Processing Of Enzymes And Microorganisms (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 |
---|---|
BE2017C018I2 true BE2017C018I2 (enrdf_load_stackoverflow) | 2021-02-04 |
Family
ID=23050302
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BE2017C018C BE2017C018I2 (enrdf_load_stackoverflow) | 2001-03-12 | 2017-06-06 |
Country Status (16)
Families Citing this family (111)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
USRE48286E1 (en) | 2001-03-12 | 2020-10-27 | Intercept Pharmaceuticals, Inc. | Steroids as agonists for FXR |
WO2003060078A2 (en) | 2001-12-21 | 2003-07-24 | 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 |
US10987362B2 (en) | 2004-03-12 | 2021-04-27 | Intercept Pharmaceuticals, Inc. | Treatment of fibrosis using FXR ligands |
PT1734970E (pt) | 2004-03-12 | 2015-03-11 | Intercept Pharmaceuticals Inc | Tratamento de fibrose utilizando ligandos de rfx |
JPWO2005092328A1 (ja) * | 2004-03-29 | 2008-02-07 | 財団法人ヒューマンサイエンス振興財団 | 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 |
JP5222846B2 (ja) * | 2006-06-27 | 2013-06-26 | インターセプト ファーマシューティカルズ, インコーポレイテッド | Fxr媒介疾患または状態の予防または治療のためのfxrリガンドとしての胆汁酸誘導体 |
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 |
CN105037476B (zh) | 2008-07-30 | 2018-06-12 | 英特塞普特医药品公司 | Tgr5调节剂及其使用方法 |
SG10201400162QA (en) | 2008-11-19 | 2014-05-29 | Intercept Pharmaceuticals Inc | Tgr5 modulators and methods of use thereof |
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 |
SG10201607230SA (en) * | 2012-06-19 | 2016-10-28 | Intercept Pharmaceuticals Inc | Preparation, Uses And Solid Forms Of Obeticholic Acid |
JP6272888B2 (ja) | 2012-10-26 | 2018-01-31 | インターセプト ファーマシューティカルズ, インコーポレイテッド | 胆汁酸誘導体を調製するためのプロセス |
MX2015006710A (es) * | 2012-11-28 | 2016-01-15 | Intercept Pharmaceuticals Inc | Tratamiento de las enfermedades pulmonares. |
US20160151486A1 (en) | 2013-06-13 | 2016-06-02 | Fast Foward 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 |
EP3043865B1 (en) | 2013-09-11 | 2020-11-04 | Institut National de la Sante et de la Recherche Medicale (INSERM) | Methods and pharmaceutical compositions for the treatment of hepatitis b virus infection |
WO2015075557A2 (en) | 2013-11-22 | 2015-05-28 | Mina Alpha Limited | C/ebp alpha 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 |
SI3626725T1 (sl) * | 2014-05-29 | 2023-04-28 | Bar Pharmaceuticals S.R.L. | Derivati holana za uporabo pri zdravljenju in/ali preprečevanju bolezni, posredovanih s FXR in 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 |
KR20170094184A (ko) | 2014-11-06 | 2017-08-17 | 이난타 파마슈티칼스, 인코포레이티드 | Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법 |
CN111944006B (zh) * | 2014-11-17 | 2021-12-17 | 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 |
TWI686401B (zh) * | 2014-11-19 | 2020-03-01 | 英商Nzp英國有限公司 | 化合物(三) |
MX375864B (es) | 2014-11-19 | 2025-03-07 | Nzp Uk Ltd | Esteroides de 5.beta-6-alquil-7-hidroxi-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr) |
CA2968309A1 (en) | 2014-11-19 | 2016-05-26 | NZP UK Limited | 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators |
KR102527821B1 (ko) | 2014-11-19 | 2023-05-02 | 엔제트피 유케이 리미티드 | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드 |
AU2015353473A1 (en) | 2014-11-26 | 2017-06-08 | Enanta Pharmaceuticals, Inc. | Bile acid analogs as FXR/TGR5 agonists and methods of use thereof |
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 |
US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives 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 |
WO2016127019A2 (en) | 2015-02-06 | 2016-08-11 | Intercept Pharmaceuticals, Inc. | Pharmaceutical compositions for combination therapy |
BR112017017238A2 (pt) | 2015-02-11 | 2018-04-10 | Enanta Pharm Inc | análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos |
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 |
EP3277286B1 (en) | 2015-03-31 | 2021-04-21 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
TN2017000426A1 (en) | 2015-04-07 | 2019-04-12 | Intercept Pharmaceuticals Inc | Pharmaceutical compositions for combination therapy |
PE20180690A1 (es) | 2015-04-27 | 2018-04-23 | Intercept Pharmaceuticals Inc | Composiciones de acido obeticolico y metodos de uso |
CN106290594B (zh) * | 2015-05-27 | 2020-07-17 | 中美华世通生物医药科技(武汉)有限公司 | 测定奥贝胆酸片溶出含量的方法 |
CZ2015504A3 (cs) | 2015-07-16 | 2017-01-25 | Zentiva, K.S. | Krystalické formy obeticholové kyseliny |
CN105085597B (zh) * | 2015-08-28 | 2017-03-29 | 成都百裕制药股份有限公司 | 一种无定型奥贝胆酸的制备方法 |
CN106478759A (zh) * | 2015-08-31 | 2017-03-08 | 陕西合成药业股份有限公司 | 奥贝胆酸衍生物及其制备方法和用途 |
CA2998876A1 (en) | 2015-09-21 | 2017-03-30 | Intercept Pharmaceuticals, Inc. | Methods of promoting hepatic regeneration |
CA2999302A1 (en) | 2015-09-24 | 2017-03-30 | Intercept Pharmaceuticals, Inc. | Methods and intermediates for the preparation bile acid derivatives |
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 |
CN106632564B (zh) * | 2015-10-30 | 2021-04-13 | 苏州泽璟生物制药股份有限公司 | 奥贝胆酸盐及其无定形物和药物组合物 |
AU2016350690C1 (en) * | 2015-11-06 | 2020-04-23 | Intercept Pharmaceuticals, Inc. | Methods for the preparation of obeticholic acid and derivatives thereof |
CN106749466B (zh) * | 2015-11-23 | 2019-05-21 | 南京济群医药科技股份有限公司 | 一种高纯度奥贝胆酸的制备方法 |
CN106854229A (zh) * | 2015-12-08 | 2017-06-16 | 陈剑 | 一类脂肪酸盐,其制备及其在医药上的应用 |
WO2017115324A1 (en) | 2016-01-01 | 2017-07-06 | Lupin Limited | Solid forms of obeticholic acid and processes thereof |
CN109071593B (zh) | 2016-01-28 | 2021-01-15 | 正大天晴药业集团股份有限公司 | 甾体类衍生物fxr激动剂 |
ES2909907T3 (es) * | 2016-02-10 | 2022-05-10 | Dr Reddys Laboratories Ltd | Proceso de purificación que implica la sal de amina del ácido obeticólico |
WO2017147174A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Heteroaryl containing bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
US10364267B2 (en) | 2016-02-23 | 2019-07-30 | Enanta Pharmaceuticals, Inc. | Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
WO2017147137A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Benzoic acid derivatives of bile acid as fxr/tgr5 agonists and methods of use thereof |
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 |
CN105541953B (zh) * | 2016-03-15 | 2017-11-21 | 成都市新功生物科技有限公司 | 一种高纯度奥贝胆酸的重结晶纯化方法 |
CN107188917A (zh) * | 2016-03-15 | 2017-09-22 | 正大天晴药业集团股份有限公司 | 奥贝胆酸盐及其药物组合物 |
US11419878B2 (en) | 2016-03-28 | 2022-08-23 | Intercept Pharmaceuticals, Inc. | Medicine obtained by combining FXR agonist and ARB |
WO2017170858A1 (ja) * | 2016-03-31 | 2017-10-05 | 大日本住友製薬株式会社 | 溶出性に優れた経口製剤 |
CN109195607A (zh) * | 2016-03-31 | 2019-01-11 | 英特塞普特医药品公司 | 具有活性成分的高化学稳定性的薄膜包衣片剂 |
EP3440092A1 (en) | 2016-04-04 | 2019-02-13 | Dipharma Francis S.r.l. | Method for preparing a farnesoid x receptor agonist |
ITUA20162272A1 (it) * | 2016-04-04 | 2017-10-04 | Dipharma Francis Srl | Procedimento per la preparazione di un agonista del recettore farnesoide x |
EP3228306A1 (en) | 2016-04-04 | 2017-10-11 | ratiopharm GmbH | Complex compound comprising obeticholic acid and cyclodextrin and pharmaceutical formulation comprising the complex compound |
CN109071452A (zh) | 2016-04-13 | 2018-12-21 | 英特塞普特医药品公司 | 治疗癌症的方法 |
TW201738254A (zh) | 2016-04-19 | 2017-11-01 | 英特賽普醫藥品公司 | 奧貝膽酸及其衍生物之製備方法 |
EA038580B9 (ru) * | 2016-05-18 | 2021-10-05 | Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд. | Агонист fxr, представляющий собой производное стероидов |
GB201608777D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Compounds |
GB201608776D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and compounds |
WO2017207648A1 (en) | 2016-05-31 | 2017-12-07 | Bionice, S.L.U | Process and intermediates for the preparation of obeticholic acid and derivatives thereof |
WO2017208165A1 (en) | 2016-06-01 | 2017-12-07 | Dr. Reddy’S Laboratories Limited | Process for preparation of obeticholic acid |
CZ2016385A3 (cs) | 2016-06-28 | 2018-01-10 | Zentiva, K.S. | Způsoby přípravy intermediátů pro syntézu Obeticholové kyseliny |
TWI606565B (zh) * | 2016-08-31 | 2017-11-21 | 金寶電子工業股份有限公司 | 封裝結構及其製作方法 |
EP3293196A1 (en) | 2016-09-09 | 2018-03-14 | Hexal AG | Process for purifying obeticholic acid |
US10450306B2 (en) | 2016-10-04 | 2019-10-22 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
EP3305799A3 (en) | 2016-10-07 | 2018-06-20 | Lupin Limited | Salts of obeticholic acid |
JP7057783B2 (ja) | 2016-11-29 | 2022-04-20 | エナンタ ファーマシューティカルズ インコーポレイテッド | スルホニル尿素胆汁酸誘導体の調製方法 |
CN108264532B (zh) * | 2016-12-30 | 2021-02-26 | 上海现代制药股份有限公司 | 一种奥贝胆酸的制备方法及其中间体 |
US10472386B2 (en) | 2017-02-14 | 2019-11-12 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR agonists and methods of use thereof |
WO2018153933A1 (en) | 2017-02-21 | 2018-08-30 | Genfit | Combination of a ppar agonist with a fxr agonist |
CN110944635A (zh) | 2017-03-30 | 2020-03-31 | 国家医疗保健研究所 | 用于减少附加体病毒的持久性和表达的方法和药物组合物 |
BR112019020780A2 (pt) | 2017-04-07 | 2020-04-28 | Enanta Pharm Inc | processo para preparação de derivados de ácido biliar de carbamato de sulfonila |
CZ2017298A3 (cs) | 2017-05-26 | 2018-12-05 | Zentiva, K.S. | Amorfní formy obeticholové kyseliny |
CN109134572A (zh) * | 2017-06-19 | 2019-01-04 | 中国科学院上海药物研究所 | 胆酸衍生物及其制备方法和用途 |
US11189472B2 (en) * | 2017-07-17 | 2021-11-30 | Applied Materials, Inc. | Cathode assembly having a dual position magnetron and centrally fed coolant |
EP3431486A1 (en) | 2017-07-18 | 2019-01-23 | Bionice, S.L.U. | Process and intermediates for the synthesis of obeticholic acid and derivatives thereof |
CA3075205A1 (en) | 2017-09-08 | 2019-03-14 | Mina Therapeutics Limited | Stabilized hnf4a sarna compositions and methods of use |
US10611793B1 (en) | 2017-11-27 | 2020-04-07 | Teva Czech Industries S.R.O. | Solid state forms of obeticholic acid salts |
WO2019106043A1 (en) | 2017-11-29 | 2019-06-06 | Hexal Ag | Pharmaceutical composition comprising obeticholic acid |
US10689391B2 (en) * | 2017-12-12 | 2020-06-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
WO2019160813A1 (en) | 2018-02-14 | 2019-08-22 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
ES2779985B2 (es) | 2019-02-20 | 2021-03-04 | Moehs Iberica Sl | Sal de dietilamina del ácido 3alfa-tetrahidropiraniloxi-6alfa-etil-7alfa-hidroxi-5ß-colánico |
GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
US20210261599A1 (en) | 2018-08-24 | 2021-08-26 | Solara Active Pharma Sciences Limited | Process for the Preparation of Obeticholic Acid and Intermediates Used In the Process Thereof |
CN111718388A (zh) | 2019-03-19 | 2020-09-29 | 苏州泽璟生物制药股份有限公司 | 鹅去氧胆酸衍生物的制备方法 |
CN110025591A (zh) * | 2019-04-29 | 2019-07-19 | 郑州泰丰制药有限公司 | 一种奥贝胆酸自乳化制剂及其软胶囊 |
WO2020231917A1 (en) | 2019-05-13 | 2020-11-19 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
WO2020243590A1 (en) | 2019-05-30 | 2020-12-03 | Intercept Pharmaceuticals, Inc. | Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease |
CA3139291A1 (en) | 2019-07-18 | 2021-01-21 | Jacky Vonderscher | Method for decreasing adverse-effects of interferon |
JP2023510274A (ja) | 2020-01-15 | 2023-03-13 | アンセルム(アンスティチュート・ナシオナル・ドゥ・ラ・サンテ・エ・ドゥ・ラ・ルシェルシュ・メディカル) | D型肝炎ウイルスによる感染を処置するためのfxrアゴニストの使用 |
CN112341516B (zh) * | 2020-11-14 | 2022-07-15 | 湖南科瑞生物制药股份有限公司 | 5,6-环氧类固醇类化合物及其制备方法和应用 |
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 |
CA3213217A1 (en) | 2021-04-28 | 2022-11-03 | Raphael Darteil | Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment |
WO2024104960A1 (en) | 2022-11-15 | 2024-05-23 | Synthon B.V. | Stable formulation comprising obeticholic acid |
Family Cites Families (76)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2615902A (en) | 1950-10-24 | 1952-10-28 | Merck & Co Inc | Chemical compounds and processes for preparing the same |
US3859437A (en) | 1972-06-02 | 1975-01-07 | Intellectual Property Dev Corp | Reducing cholesterol levels |
US4072695A (en) | 1972-09-21 | 1978-02-07 | Intellectual Property Development Corporation | 3α,7α-Dihydroxy-cholanic acid derivatives |
FR2444048B1 (enrdf_load_stackoverflow) | 1978-12-15 | 1981-08-14 | Roussel Uclaf | |
FR2457302A1 (fr) | 1979-05-23 | 1980-12-19 | Roussel Uclaf | Nouveau procede de purification de l'acide ursodesoxycholique |
IT1165252B (it) | 1979-07-12 | 1987-04-22 | Blasinachim Spa | Procedimento di purificazione dell'acido ursodesossicolico attraverso nuovi derivati |
DE3003607C2 (de) | 1980-02-01 | 1984-01-05 | Dr.-Ing. Rudolf Hell Gmbh, 2300 Kiel | Schaltungsanordnung zur partiellen Nachkorrektur von Farberkennungsräumen bei der Farberkennung |
IT1137459B (it) | 1981-04-14 | 1986-09-10 | Erregierre Spa | Prodesso per la preparazione di acido ursodeossicolico ad alta purezza |
EP0101554B1 (en) | 1982-07-29 | 1986-10-15 | Lehner A.G. | 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. |
US4721709A (en) | 1984-07-26 | 1988-01-26 | Pyare Seth | Novel pharmaceutical compositions containing hydrophobic practically water-insoluble drugs adsorbed on pharmaceutical excipients as carrier; process for their preparation and the use of said compositions |
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 |
FR2627696B1 (fr) | 1988-02-26 | 1991-09-13 | Fournier Innovation Synergie | Nouvelle forme galenique du fenofibrate |
IT1229570B (it) | 1989-04-17 | 1991-09-04 | Giuliani Spa | Derivati fluorurati 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 |
US4982868A (en) * | 1989-11-07 | 1991-01-08 | Robbins Edward S Iii | Bail type pitcher for thin walled container |
DE69018592T2 (de) * | 1989-12-13 | 1995-10-05 | Mitsubishi Chem Corp | Pyrazolylacrylsäure-Derivate, verwendbar als systemische Fungiziden in Pflanzen- und Materialschutz. |
JPH04250093A (ja) | 1991-01-18 | 1992-09-04 | Kanzaki Paper Mfg Co Ltd | 感熱記録体 |
WO1997028149A1 (en) | 1996-02-02 | 1997-08-07 | 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 |
TR199900056T2 (xx) | 1996-07-12 | 1999-04-21 | Smithkline Beecham P.L.C. | Leptin direncinin yeni tedavisi. |
US6060465A (en) | 1997-02-06 | 2000-05-09 | Miljkovic; Dusan | Bile acids and their derivatives as glycoregulatory agents |
US6008237A (en) | 1997-12-19 | 1999-12-28 | Merck & Co., Inc. | Arylthiazolidinedione derivatives |
CA2318731C (en) | 1998-01-29 | 2012-05-29 | Tularik Inc. | Ppar-gamma modulators |
US6639057B1 (en) * | 1998-03-26 | 2003-10-28 | Kyowa Hakko Kogyo Co., Ltd. | Monoclonal antibody against human telomerase catalytic subunit |
AU1229000A (en) | 1998-10-23 | 2000-05-15 | Glaxo Group Limited | Assays for ligands for nuclear receptors |
DE69931279T2 (de) | 1998-11-09 | 2007-04-12 | Atherogenics, Inc. | Methode und zusammensetzungen zum vermindern des cholesterolspiegels im plasma |
UA74141C2 (uk) | 1998-12-09 | 2005-11-15 | Дж.Д. Сірл Енд Ко. | Фармацевтична композиція на основі тонкоподрібненого еплеренону (варіанти), спосіб її одержання та спосіб лікування розладів, опосередкованих альдостероном (варіанти) |
ES2326850T3 (es) | 1998-12-23 | 2009-10-20 | Glaxo Group Limited | Ensayos para ligandos de receptores nucleares. |
US6465258B1 (en) | 1999-01-07 | 2002-10-15 | Tularik, Inc. | FXR receptor-mediated modulation cholesterol metabolism |
EP1473042B1 (en) | 1999-03-26 | 2006-06-21 | City of Hope | Screening for FXR receptor modulators |
DE60029029T2 (de) | 1999-03-26 | 2007-06-14 | City Of Hope, Duarte | Screenen nach FXR-Rezeptormodulatoren |
US20020132223A1 (en) | 1999-03-26 | 2002-09-19 | City Of Hope | Methods for modulating activity of the FXR nuclear receptor |
AU768806B2 (en) | 1999-06-11 | 2004-01-08 | Allergan, 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 |
EP1284728A4 (en) | 1999-10-22 | 2004-05-19 | Merck & Co Inc | MEDICINES FOR TREATING ADDICTIC ADDICTION |
US6627636B2 (en) | 2000-06-15 | 2003-09-30 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors and method |
WO2002020463A2 (en) | 2000-09-05 | 2002-03-14 | Tularik Inc. | Fxr modulators |
US20020119958A1 (en) | 2001-02-13 | 2002-08-29 | Shinichiro Tojo | Therapeutic agent for hyperlipidemia |
USRE48286E1 (en) | 2001-03-12 | 2020-10-27 | Intercept Pharmaceuticals, Inc. | Steroids as agonists for FXR |
EP1378749A4 (en) | 2001-04-12 | 2005-05-11 | Takeda Pharmaceutical | SCREENING METHOD |
ATE381542T1 (de) | 2001-08-13 | 2008-01-15 | Phenex Pharmaceuticals Ag | Nr1h4-kern-rezeptor-bindende verbindungen |
US20070010562A1 (en) | 2001-08-13 | 2007-01-11 | Ulrike Bauer | Nr1h4 nuclear receptor binding compounds |
WO2003015777A1 (en) | 2001-08-13 | 2003-02-27 | Lion Bioscience Ag | Nr1h4 nuclear receptor binding compounds |
US7112340B2 (en) | 2001-10-19 | 2006-09-26 | Baxter International Inc. | Compositions of and method for preparing stable particles in a frozen aqueous matrix |
US20030144360A1 (en) | 2001-11-19 | 2003-07-31 | Allergan Sales, Inc. | Composition and method for modulating BAR/FXR receptor activity |
US20050107475A1 (en) | 2002-03-21 | 2005-05-19 | Jones Stacey A. | Methods of using farnesoid x receptor (frx) agonists |
EP1494533A2 (en) | 2002-04-12 | 2005-01-12 | 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 |
ITMI20021532A1 (it) | 2002-07-12 | 2004-01-12 | Roberto Pellicciari | Composti chimici |
EP1562915A1 (en) | 2002-11-22 | 2005-08-17 | SmithKline Beecham Corporation | Farnesoid x receptor agonists |
US6993380B1 (en) | 2003-06-04 | 2006-01-31 | Cleveland Medical Devices, Inc. | Quantitative sleep analysis method and system |
WO2005032549A1 (en) | 2003-09-26 | 2005-04-14 | 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 |
TW200603818A (en) | 2004-03-11 | 2006-02-01 | Fresenius Kabi De Gmbh | Conjugates of hydroxyethyl starch and erythropoietin |
PT1734970E (pt) | 2004-03-12 | 2015-03-11 | Intercept Pharmaceuticals Inc | Tratamento de fibrose utilizando ligandos de rfx |
US20060252670A1 (en) | 2004-10-14 | 2006-11-09 | Intercept Pharmaceuticals Inc. | Method of reducing drug-induced adverse side effects in a patient |
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 |
WO2007095174A2 (en) | 2006-02-14 | 2007-08-23 | Intercept Pharmaceuticals, Inc. | Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions |
JP5222846B2 (ja) | 2006-06-27 | 2013-06-26 | インターセプト ファーマシューティカルズ, インコーポレイテッド | Fxr媒介疾患または状態の予防または治療のためのfxrリガンドとしての胆汁酸誘導体 |
US20100239661A1 (en) | 2006-10-26 | 2010-09-23 | Sunilendu Bhushan Roy | Pharmaceutical compositions of ursodiol |
EP1947108A1 (en) | 2007-01-19 | 2008-07-23 | Intercept Pharmaceuticals, Inc. | TGR5 modulators and methods of use thereof |
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 |
SG10201400162QA (en) | 2008-11-19 | 2014-05-29 | Intercept Pharmaceuticals Inc | Tgr5 modulators and methods of use thereof |
UA110773C2 (uk) | 2009-04-24 | 2016-02-25 | Айсьютіка Пті Лтд | Спосіб одержання порошків, що містять нано- і мікрочастинки |
EP2468762A1 (en) | 2010-11-30 | 2012-06-27 | Dr. Falk Pharma Gmbh | Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size |
WO2013037482A1 (en) | 2011-09-15 | 2013-03-21 | Phenex Pharmaceuticals Ag | Farnesoid x receptor agonists for cancer treatment and prevention |
FR2981572B1 (fr) | 2011-10-21 | 2018-01-19 | Inopharm Limited | Compositions pharmaceutiques d'acide ursodesoxycholique |
SG10201607230SA (en) | 2012-06-19 | 2016-10-28 | Intercept Pharmaceuticals Inc | Preparation, Uses And Solid Forms Of Obeticholic Acid |
SG11201509352XA (en) | 2013-05-14 | 2015-12-30 | Intercept Pharmaceuticals Inc | 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators |
-
2002
- 2002-02-21 US US16/448,503 patent/USRE48286E1/en active Active
- 2002-02-21 WO PCT/EP2002/001832 patent/WO2002072598A1/en active IP Right Grant
- 2002-02-21 AT AT02750526T patent/ATE303399T1/de active
- 2002-02-21 ES ES02750526T patent/ES2248581T3/es not_active Expired - Lifetime
- 2002-02-21 CA CA2440680A patent/CA2440680C/en not_active Expired - Lifetime
- 2002-02-21 AU AU2002308295A patent/AU2002308295B2/en active Active
- 2002-02-21 US US10/471,549 patent/US7138390B2/en not_active Ceased
- 2002-02-21 EP EP02750526A patent/EP1392714B1/en not_active Expired - Lifetime
- 2002-02-21 DK DK02750526T patent/DK1392714T3/da active
- 2002-02-21 DE DE60205891T patent/DE60205891T2/de not_active Expired - Lifetime
- 2002-02-21 IL IL15781602A patent/IL157816A0/xx unknown
- 2002-02-21 JP JP2002571512A patent/JP4021327B2/ja not_active Expired - Lifetime
-
2003
- 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
-
2006
- 2006-11-21 US US11/602,307 patent/US7786102B2/en not_active Expired - Lifetime
-
2007
- 2007-06-20 JP JP2007162928A patent/JP2007269815A/ja active Pending
-
2009
- 2009-08-25 US US12/547,147 patent/US8058267B2/en not_active Expired - Fee Related
-
2011
- 2011-11-03 US US13/288,558 patent/US8377916B2/en not_active Expired - Fee Related
-
2013
- 2013-02-07 US US13/761,889 patent/US8969330B2/en not_active Expired - Fee Related
-
2015
- 2015-02-26 US US14/632,139 patent/US20150166598A1/en not_active Abandoned
-
2016
- 2016-02-05 US US15/016,802 patent/US9732117B2/en not_active Expired - Lifetime
-
2017
- 2017-05-26 NO NO2017022C patent/NO2017022I2/no unknown
- 2017-05-29 CY CY2017020C patent/CY2017020I2/el unknown
- 2017-06-06 BE BE2017C018C patent/BE2017C018I2/fr unknown
- 2017-06-07 FR FR17C0003C patent/FR17C0003I2/fr active Active
- 2017-06-09 NL NL300877C patent/NL300877I2/nl unknown
- 2017-07-10 US US15/645,136 patent/US10421772B2/en not_active Expired - Fee Related
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
BE2017C018I2 (enrdf_load_stackoverflow) | ||
MXPA02012033A (es) | Derivados de 2-aminocarbonil-9h-purina. | |
TNSN03144A1 (en) | Pyrrolopyrimidines as protein kinase inhibitors | |
WO2003006425A3 (en) | Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents | |
MXPA02003977A (es) | Inhibidores de adhesion de celula mediada por al°2. | |
WO2004007521A3 (en) | Bile acid derivatives as agonists of the farnesoid x receptor | |
AP2003002929A0 (en) | Pyrrolopyrimidines as protein kinase inhibitors | |
NO20043016L (no) | 6-aminomorfinan-derivater, fremgangsmate for fremstilling og anvendelse derav | |
IL150061A0 (en) | Purine derivatives | |
MXPA04006041A (es) | Antivirales de piridoquinoxalina. | |
AU2001263278A1 (en) | Cyclic gmp-specific phosphodiesterase inhibitors | |
MXPA04005809A (es) | Inhibidores de proteinas quinasas. | |
DK1204658T3 (da) | Benzofurylpiperazin-serotoninagonister | |
DE60201074D1 (en) | Pyrazolopyridinderivate | |
AU2002357740A1 (en) | Pyrazolo-pyridine derivatives as antiherpes agents | |
AU2001296699A1 (en) | Condensed pyrazindione derivatives as pde inhibitors | |
MXPA03008248A (es) | Agentes colorantes para fibras de queratina que contienen derivados de n-heteroarilmetil-m-fenilendiamina, asi como nuevos derivados de n-heteroarilmetil-m-fenilendiamina. | |
PT1651596E (pt) | Novos derivados de 4,4?-ditiobis-(3-aminobutano-1-sulfonatos) e composições que os contêm | |
MXPA03006057A (es) | Proceso para preparar (+) trans-4-p-fluorofenil -3 hidroximetil. | |
DE69827614D1 (de) | Chinoxalindionen | |
EP1057829A4 (en) | Condensed pyrimidine derivatives and pharmaceutical compositions containing them | |
IL159493A0 (en) | Pharmaceutical formulation containing an ltb4 antagonist | |
MY128457A (en) | 2-aminocarbonyl-9h-purine derivatives |