PT3458469T - Intermediários para a síntese de derivados de ácido biliar, em particular de ácido obeticólico - Google Patents
Intermediários para a síntese de derivados de ácido biliar, em particular de ácido obeticólicoInfo
- Publication number
- PT3458469T PT3458469T PT177257409T PT17725740T PT3458469T PT 3458469 T PT3458469 T PT 3458469T PT 177257409 T PT177257409 T PT 177257409T PT 17725740 T PT17725740 T PT 17725740T PT 3458469 T PT3458469 T PT 3458469T
- Authority
- PT
- Portugal
- Prior art keywords
- intermediates
- synthesis
- obeticholic
- acid derivatives
- acid
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/008—Ketals at position 17
-
- 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
- C07J33/00—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J33/00—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J33/002—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- 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
- 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
- C07J41/0061—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 one of the carbon atoms being part of an amide group
-
- 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
- C07J41/0088—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing unsubstituted amino radicals
-
- 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
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- 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
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/006—Ketals at position 3
-
- 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)
- Toxicology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1608777.7A GB201608777D0 (en) | 2016-05-18 | 2016-05-18 | Compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PT3458469T true PT3458469T (pt) | 2021-06-11 |
Family
ID=56320629
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PT177257409T PT3458469T (pt) | 2016-05-18 | 2017-05-18 | Intermediários para a síntese de derivados de ácido biliar, em particular de ácido obeticólico |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US10968250B2 (pt) |
| EP (2) | EP3458469B1 (pt) |
| JP (1) | JP7034093B2 (pt) |
| KR (1) | KR102458265B1 (pt) |
| CN (1) | CN109415407B (pt) |
| AU (1) | AU2017266539B2 (pt) |
| BR (1) | BR112018073488A2 (pt) |
| CA (1) | CA3024281A1 (pt) |
| EA (1) | EA037584B1 (pt) |
| ES (1) | ES2878577T3 (pt) |
| GB (1) | GB201608777D0 (pt) |
| HR (1) | HRP20211128T1 (pt) |
| HU (1) | HUE054851T2 (pt) |
| MX (1) | MX2018014164A (pt) |
| PT (1) | PT3458469T (pt) |
| WO (1) | WO2017199033A1 (pt) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201608776D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and compounds |
| EP3431486A1 (en) * | 2017-07-18 | 2019-01-23 | Bionice, S.L.U. | Process and intermediates for the synthesis of obeticholic acid and derivatives thereof |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| CN111138509B (zh) * | 2018-11-02 | 2022-12-06 | 东莞东阳光药物研发有限公司 | 奥贝胆酸的制备方法 |
| CN111072744B (zh) * | 2019-12-03 | 2021-09-14 | 江苏佳尔科药业集团股份有限公司 | 一种以ba为原料合成熊去氧胆酸的方法 |
| CN114315945A (zh) * | 2020-09-28 | 2022-04-12 | 四川澄华生物科技有限公司 | 一种胆甾酸及其衍生物的除杂方法 |
| 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 |
| WO2023081657A2 (en) * | 2021-11-02 | 2023-05-11 | Sandhill One, Llc | High purity non-animal derived udca |
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| US2624748A (en) | 1950-09-09 | 1953-01-06 | Upjohn Co | Bisnorchola-4, 6-dien-3-one-22-al |
| US4289872A (en) | 1979-04-06 | 1981-09-15 | Allied Corporation | Macromolecular highly branched homogeneous compound based on lysine units |
| US5229490A (en) | 1987-05-06 | 1993-07-20 | The Rockefeller University | Multiple antigen peptide system |
| JPH07505915A (ja) | 1992-04-14 | 1995-06-29 | コーネル リサーチ ファウンデーション、インコーポレーテッド | 樹枝状巨大分子およびその製造法 |
| AU6392894A (en) | 1993-02-26 | 1994-09-14 | Magainin Pharmaceuticals, Inc. | Chemical synthesis of squalamine |
| US5643575A (en) | 1993-10-27 | 1997-07-01 | Enzon, Inc. | Non-antigenic branched polymer conjugates |
| US5932462A (en) | 1995-01-10 | 1999-08-03 | Shearwater Polymers, Inc. | Multiarmed, monofunctional, polymer for coupling to molecules and surfaces |
| IL157816A0 (en) | 2001-03-12 | 2004-03-28 | Roberto Pellicciari | Steroids as agonists for fxr |
| US20090062256A1 (en) | 2001-06-01 | 2009-03-05 | Bristol-Myers Squibb Pharma Company | LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF Abeta PROTEIN PRODUCTION |
| AU2002352524B2 (en) | 2001-11-07 | 2007-10-04 | Nektar Therapeutics | Branched polymers and their conjugates |
| EP1568706A1 (en) | 2004-02-26 | 2005-08-31 | Intercept Pharmaceuticals, Inc. | Novel steroid agonist for 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 |
| CN101374854A (zh) * | 2006-01-12 | 2009-02-25 | 三菱化学株式会社 | 甾类化合物的制备方法 |
| JP2007210888A (ja) * | 2006-01-12 | 2007-08-23 | Mitsubishi Chemicals Corp | ステロイド化合物の製造方法 |
| BRPI0707794A2 (pt) | 2006-02-14 | 2011-05-10 | Intercept Pharmaceuticals Inc | compostos derivados de Ácido biliar, formulaÇÕes e composiÇÕes farmacÊuticas, bem como uso de ditos compostos |
| 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 |
| EP2112995B1 (en) | 2007-01-19 | 2013-07-31 | Intercept Pharmaceuticals, Inc. | 23-substituted bile acids as tgr5 modulators and methods of use thereof |
| CN102164940B (zh) | 2008-07-30 | 2015-08-19 | 英特塞普特医药品公司 | Tgr5调节剂及其使用方法 |
| CA2744189C (en) | 2008-11-19 | 2016-10-11 | Intercept Pharmaceuticals, Inc. | Tgr5 modulators and methods of use thereof |
| ES2774368T3 (es) | 2008-11-19 | 2020-07-20 | Intercept Pharmaceuticals Inc | Moduladores de TGR5 y métodos de uso de los mismos |
| CN102482315A (zh) | 2009-07-29 | 2012-05-30 | 芝加哥大学 | 肝x受体激动剂 |
| EP3336097B1 (en) | 2012-06-19 | 2020-08-19 | Intercept Pharmaceuticals, Inc. | Preparation of the non-crystalline form of obeticholic acid |
| ES2655034T3 (es) | 2012-10-26 | 2018-02-16 | Intercept Pharmaceuticals, Inc. | Proceso para preparar derivados del ácido biliar |
| 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 |
| US20140206657A1 (en) * | 2013-01-18 | 2014-07-24 | City Of Hope | Bile acid analog tgr5 agonists |
| ES2671427T3 (es) | 2013-05-14 | 2018-06-06 | Intercept Pharmaceuticals, Inc. | Derivados 11-hidroxil-6-sustituidos de ácidos biliares y conjugados de aminoácidos de los mismos como moduladores de receptores farnesoides X |
| AU2014269961A1 (en) | 2013-05-24 | 2015-11-26 | Société des Produits Nestlé S.A. | Pathway specific markers for diagnosing irritable bowel syndrome |
| WO2015183794A1 (en) | 2014-05-27 | 2015-12-03 | City Of Hope | Tgr5 agonist complexes for treating diabetes and cancer |
| CN106661079B (zh) | 2014-05-29 | 2019-03-01 | 巴尔制药有限公司 | 用于治疗和/或预防fxr和tgr5/gpbar1介导的疾病的胆烷衍生物 |
| RU2017118569A (ru) | 2014-11-06 | 2018-12-06 | Энанта Фармасьютикалс, Инк. | Аналоги желчных кислот как агонисты fxr/tgr5 и способы их применения |
| WO2016079518A1 (en) * | 2014-11-19 | 2016-05-26 | Dextra Laboratories Limited | 5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators |
| WO2016079517A1 (en) * | 2014-11-19 | 2016-05-26 | Dextra Laboratories Limited | 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators |
| EP3221334B1 (en) | 2014-11-19 | 2020-02-19 | Nzp Uk Limited | 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators |
| WO2016079519A1 (en) | 2014-11-19 | 2016-05-26 | Dextra Laboratories Limited | 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| RU2017121457A (ru) | 2014-11-26 | 2018-12-26 | Энанта Фармасьютикалс, Инк. | Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения |
| WO2016086134A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives 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 |
| CN105348365A (zh) | 2014-12-03 | 2016-02-24 | 四川百利药业有限责任公司 | 一种胆酸衍生物及其制备方法、药物组合物和用途 |
| CN106279328A (zh) | 2015-05-20 | 2017-01-04 | 重庆药友制药有限责任公司 | 一种制备6α-烷基鹅去氧胆酸的方法 |
| WO2016205475A2 (en) | 2015-06-19 | 2016-12-22 | Intercept Pharmaceuticals, Inc. | Tgr5 modulators and methods of use thereof |
| CN106397522A (zh) | 2015-07-31 | 2017-02-15 | 中国人民解放军军事医学科学院毒物药物研究所 | 3,7‑二（叔丁基二甲基硅基氧基）‑6‑烯‑5β‑胆烷‑24‑酸甲酯 |
| 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 |
| CN106478756A (zh) | 2015-09-02 | 2017-03-08 | 中美华世通生物医药科技（武汉）有限公司 | Oca-e单晶及其制备方法和用途 |
| CN106518946A (zh) | 2015-09-10 | 2017-03-22 | 上海迪诺医药科技有限公司 | 磺酰脲衍生物、其药物组合物及应用 |
| GB201608779D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and compounds |
| GB201608776D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and compounds |
-
2016
- 2016-05-18 GB GBGB1608777.7A patent/GB201608777D0/en not_active Ceased
-
2017
- 2017-05-18 MX MX2018014164A patent/MX2018014164A/es unknown
- 2017-05-18 EA EA201892514A patent/EA037584B1/ru unknown
- 2017-05-18 EP EP17725740.9A patent/EP3458469B1/en active Active
- 2017-05-18 PT PT177257409T patent/PT3458469T/pt unknown
- 2017-05-18 ES ES17725740T patent/ES2878577T3/es active Active
- 2017-05-18 CA CA3024281A patent/CA3024281A1/en active Pending
- 2017-05-18 HR HRP20211128TT patent/HRP20211128T1/hr unknown
- 2017-05-18 AU AU2017266539A patent/AU2017266539B2/en active Active
- 2017-05-18 BR BR112018073488-8A patent/BR112018073488A2/pt active Search and Examination
- 2017-05-18 WO PCT/GB2017/051385 patent/WO2017199033A1/en unknown
- 2017-05-18 CN CN201780030532.1A patent/CN109415407B/zh active Active
- 2017-05-18 KR KR1020187035834A patent/KR102458265B1/ko active IP Right Grant
- 2017-05-18 EP EP21160246.1A patent/EP3848382B1/en active Active
- 2017-05-18 JP JP2018560597A patent/JP7034093B2/ja active Active
- 2017-05-18 HU HUE17725740A patent/HUE054851T2/hu unknown
- 2017-05-18 US US16/302,059 patent/US10968250B2/en active Active
-
2021
- 2021-02-26 US US17/186,272 patent/US11479577B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP3458469B1 (en) | 2021-04-14 |
| KR102458265B1 (ko) | 2022-10-25 |
| BR112018073488A2 (pt) | 2019-04-09 |
| GB201608777D0 (en) | 2016-06-29 |
| EP3848382B1 (en) | 2023-11-29 |
| AU2017266539A1 (en) | 2018-11-15 |
| EP3848382C0 (en) | 2023-11-29 |
| EP3848382A1 (en) | 2021-07-14 |
| ES2878577T3 (es) | 2021-11-19 |
| EA201892514A1 (ru) | 2019-05-31 |
| US20190284227A1 (en) | 2019-09-19 |
| HUE054851T2 (hu) | 2021-10-28 |
| EA037584B1 (ru) | 2021-04-16 |
| US20210179661A1 (en) | 2021-06-17 |
| US10968250B2 (en) | 2021-04-06 |
| US11479577B2 (en) | 2022-10-25 |
| KR20190009322A (ko) | 2019-01-28 |
| CN109415407B (zh) | 2021-08-17 |
| AU2017266539B2 (en) | 2021-04-15 |
| JP2019516720A (ja) | 2019-06-20 |
| WO2017199033A1 (en) | 2017-11-23 |
| MX2018014164A (es) | 2019-04-01 |
| CA3024281A1 (en) | 2017-11-23 |
| EP3458469A1 (en) | 2019-03-27 |
| JP7034093B2 (ja) | 2022-03-11 |
| CN109415407A (zh) | 2019-03-01 |
| HRP20211128T1 (hr) | 2022-01-07 |
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