BR112018073488A2 - 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
- BR112018073488A2 BR112018073488A2 BR112018073488-8A BR112018073488A BR112018073488A2 BR 112018073488 A2 BR112018073488 A2 BR 112018073488A2 BR 112018073488 A BR112018073488 A BR 112018073488A BR 112018073488 A2 BR112018073488 A2 BR 112018073488A2
- Authority
- BR
- Brazil
- Prior art keywords
- intermediates
- synthesis
- obeticolic
- acid
- acid derivatives
- Prior art date
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 239000000543 intermediate Substances 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical class C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 title 1
- 239000002253 acid Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003613 bile acid Substances 0.000 abstract 1
- 208000019423 liver disease Diseases 0.000 abstract 1
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
- C07J21/006—Ketals at position 3
-
- 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
- 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
-
- 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
- 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
Abstract
a invenção refere-se a compostos de fórmula geral (i): (i) em que r1, r2, r3, r4, r5, r6 e y são como definidos aqui. os compostos são intermediates na síntese de ácidos biliares sintéticos que são úteis no tratamento de condições tal como doença hepática.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB1608777.7A GB201608777D0 (en) | 2016-05-18 | 2016-05-18 | Compounds |
GB1608777.7 | 2016-05-18 | ||
PCT/GB2017/051385 WO2017199033A1 (en) | 2016-05-18 | 2017-05-18 | Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112018073488A2 true BR112018073488A2 (pt) | 2019-04-09 |
Family
ID=56320629
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112018073488-8A BR112018073488A2 (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 |
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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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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 |
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JP6861703B2 (ja) | 2015-06-19 | 2021-04-21 | 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 | Tgr5修飾物質およびその使用方法 |
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 |
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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 CN CN201780030532.1A patent/CN109415407B/zh active Active
- 2017-05-18 US US16/302,059 patent/US10968250B2/en active Active
- 2017-05-18 CA CA3024281A patent/CA3024281A1/en active Pending
- 2017-05-18 JP JP2018560597A patent/JP7034093B2/ja active Active
- 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 EA EA201892514A patent/EA037584B1/ru unknown
- 2017-05-18 EP EP17725740.9A patent/EP3458469B1/en active Active
- 2017-05-18 ES ES17725740T patent/ES2878577T3/es active Active
- 2017-05-18 HU HUE17725740A patent/HUE054851T2/hu unknown
- 2017-05-18 HR HRP20211128TT patent/HRP20211128T1/hr unknown
- 2017-05-18 WO PCT/GB2017/051385 patent/WO2017199033A1/en unknown
- 2017-05-18 KR KR1020187035834A patent/KR102458265B1/ko active IP Right Grant
- 2017-05-18 PT PT177257409T patent/PT3458469T/pt unknown
- 2017-05-18 EP EP21160246.1A patent/EP3848382B1/en active Active
- 2017-05-18 MX MX2018014164A patent/MX2018014164A/es unknown
-
2021
- 2021-02-26 US US17/186,272 patent/US11479577B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
ES2878577T3 (es) | 2021-11-19 |
EA037584B1 (ru) | 2021-04-16 |
EA201892514A1 (ru) | 2019-05-31 |
EP3848382B1 (en) | 2023-11-29 |
CN109415407A (zh) | 2019-03-01 |
US20210179661A1 (en) | 2021-06-17 |
HRP20211128T1 (hr) | 2022-01-07 |
AU2017266539A1 (en) | 2018-11-15 |
CA3024281A1 (en) | 2017-11-23 |
KR102458265B1 (ko) | 2022-10-25 |
MX2018014164A (es) | 2019-04-01 |
EP3458469B1 (en) | 2021-04-14 |
EP3848382A1 (en) | 2021-07-14 |
GB201608777D0 (en) | 2016-06-29 |
US10968250B2 (en) | 2021-04-06 |
US11479577B2 (en) | 2022-10-25 |
AU2017266539B2 (en) | 2021-04-15 |
EP3458469A1 (en) | 2019-03-27 |
KR20190009322A (ko) | 2019-01-28 |
JP7034093B2 (ja) | 2022-03-11 |
CN109415407B (zh) | 2021-08-17 |
HUE054851T2 (hu) | 2021-10-28 |
US20190284227A1 (en) | 2019-09-19 |
WO2017199033A1 (en) | 2017-11-23 |
EP3848382C0 (en) | 2023-11-29 |
JP2019516720A (ja) | 2019-06-20 |
PT3458469T (pt) | 2021-06-11 |
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