JP2024088648A - フッ素化胆汁酸誘導体 - Google Patents

フッ素化胆汁酸誘導体 Download PDF

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Publication number
JP2024088648A
JP2024088648A JP2024038682A JP2024038682A JP2024088648A JP 2024088648 A JP2024088648 A JP 2024088648A JP 2024038682 A JP2024038682 A JP 2024038682A JP 2024038682 A JP2024038682 A JP 2024038682A JP 2024088648 A JP2024088648 A JP 2024088648A
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compound
ethyl
fluoro
cholan
general formula
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Japanese (ja)
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JP2024088648A5 (enExample
Inventor
チャールズ ウェイマウス‐ウイルソン アレクサンダー
Charles Weymouth-Wilson Alexander
パッカー ゲマ
PACKER Gemma
ジャン ポル リンクラウ ブルーノ
Jan Pol LINCLAU Bruno
キッド‐シンクレアー ダニエル
Kydd-Sinclair Dannielle
アン ワトソン キンバリー
Ann Watson Kimberly
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Nzp Uk Ltd
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Nzp Uk Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/64Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal 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
    • C07J41/0061Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J11/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • C07J9/005Normal 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
JP2024038682A 2018-07-30 2024-03-13 フッ素化胆汁酸誘導体 Pending JP2024088648A (ja)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB1812382.8 2018-07-30
GBGB1812382.8A GB201812382D0 (en) 2018-07-30 2018-07-30 Compounds
PCT/GB2019/052127 WO2020025942A1 (en) 2018-07-30 2019-07-30 Fluorinated bile acid derivatives
JP2021529531A JP7805783B2 (ja) 2018-07-30 2019-07-30 フッ素化胆汁酸誘導体

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
JP2021529531A Division JP7805783B2 (ja) 2018-07-30 2019-07-30 フッ素化胆汁酸誘導体

Publications (2)

Publication Number Publication Date
JP2024088648A true JP2024088648A (ja) 2024-07-02
JP2024088648A5 JP2024088648A5 (enExample) 2026-01-22

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JP2024038682A Pending JP2024088648A (ja) 2018-07-30 2024-03-13 フッ素化胆汁酸誘導体

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US (1) US11517577B2 (enExample)
EP (1) EP3830103B8 (enExample)
JP (1) JP2024088648A (enExample)
CN (1) CN112771063B (enExample)
ES (1) ES2968881T3 (enExample)
GB (1) GB201812382D0 (enExample)
WO (1) WO2020025942A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201820887D0 (en) * 2018-12-20 2019-02-06 Nzp Uk Ltd Compounds
CN118660883A (zh) * 2021-11-15 2024-09-17 海湃泰克(北京)生物医药科技有限公司 多环化合物及其方法
CN115819491A (zh) * 2022-12-22 2023-03-21 江苏佳尔科药业集团股份有限公司 7-酮基石胆酸及熊去氧胆酸的合成方法
TW202508555A (zh) * 2023-07-27 2025-03-01 大陸商珂闌(上海)醫藥科技有限公司 甾類化合物、其製備方法和應用
WO2025020190A1 (zh) * 2023-07-27 2025-01-30 珂阑(上海)医药科技有限公司 甾类化合物、其制备方法和应用
CN119371475B (zh) * 2023-07-27 2025-11-04 珂阑(上海)医药科技有限公司 甾类化合物、其制备方法和应用

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CA2253593C (en) 1996-05-23 2008-07-08 Novartis Ag Prevention and treatment of colorectal cancer by 6-fluoroursodeoxycholic acid (6-fudca)
IL157816A0 (en) 2001-03-12 2004-03-28 Roberto Pellicciari Steroids as agonists for fxr
EP1450816A4 (en) 2001-11-08 2008-02-13 Univ Chicago METHOD OF TREATING DISORDERS RELATED TO HIGH CHOLESTEROL RATE
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
HUE024952T2 (en) 2004-03-12 2016-02-29 Intercept Pharmaceuticals Inc Treatment of fibrosis using FXR ligands
US7276585B2 (en) 2004-03-24 2007-10-02 Xencor, Inc. Immunoglobulin variants outside the Fc region
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
JP2010517931A (ja) 2006-02-14 2010-05-27 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媒介性の疾患または状態の予防または治療用のfxrリガンドとしての胆汁酸誘導体
CA2656320C (en) 2006-06-27 2015-04-28 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions
EP2112995B1 (en) 2007-01-19 2013-07-31 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as tgr5 modulators and methods of use thereof
BRPI0916735B8 (pt) 2008-07-30 2021-05-25 Intercept Pharmaceuticals Inc compostos moduladores de tgr5, composições farmacêuticas compreendendo os mesmos e seus usos
KR101789960B1 (ko) 2008-11-19 2017-10-25 인터셉트 파마슈티컬즈, 인크. Tgr5 조절제 및 그의 사용 방법
CN102282157B (zh) 2008-11-19 2017-02-22 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
EP3336097B1 (en) 2012-06-19 2020-08-19 Intercept Pharmaceuticals, Inc. Preparation of the non-crystalline form 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
US20140206657A1 (en) 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
IL286970B2 (en) 2013-03-13 2024-11-01 Sage Therapeutics Inc Neuroactive steroids and methods of use thereof
SI3360881T1 (sl) 2013-05-14 2021-06-30 Intercept Pharmaceuticals, Inc. 11-hidroksil-6-substituirani derivati žolčnih kislin in aminokislinski konjugati le-teh kot modulatorji receptorja farnezoid X
WO2015085474A1 (zh) 2013-12-10 2015-06-18 华为终端有限公司 一种注册方法和相关节点以及注册系统
CN106999551A (zh) * 2014-11-06 2017-08-01 英安塔制药有限公司 作为fxr/tgr5激动剂的胆汁酸类似物和其使用方法
EP3221333B1 (en) 2014-11-19 2019-07-24 NZP UK Limited 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators
WO2016079520A1 (en) 2014-11-19 2016-05-26 Dextra Laboratories Limited 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators
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
WO2016086134A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
WO2016086115A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof
CN107231795A (zh) 2014-11-26 2017-10-03 英安塔制药有限公司 作为fxr/tgr5激动剂的胆汁酸类似物及其使用方法
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives 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
TN2017000344A1 (en) 2015-02-06 2019-01-16 Intercept Pharmaceuticals Inc Pharmaceutical compositions for combination therapy
SG11201706089RA (en) 2015-02-11 2017-09-28 Enanta Pharm Inc Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
CA2978916A1 (en) 2015-03-09 2016-09-15 Intercept Pharmaceuticals, Inc. Methods for modulating bone density
WO2016145216A1 (en) 2015-03-10 2016-09-15 Metselex, Inc. Fluorinated and alkylated bile acids
US20160279393A1 (en) 2015-03-25 2016-09-29 Covidien Lp Guidewire retrieval catheter
US10457703B2 (en) 2015-03-31 2019-10-29 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
CR20170456A (es) 2015-04-07 2018-06-13 Intercept Pharmaceuticals Inc Composiciones farmacéuticas para terapias combinadas
PE20180690A1 (es) 2015-04-27 2018-04-23 Intercept Pharmaceuticals Inc Composiciones de acido obeticolico y metodos de uso
CN106083978A (zh) 2015-04-28 2016-11-09 上海迪诺医药科技有限公司 磺酰基氨基羰基衍生物、其药物组合物及应用
CN111116699B (zh) 2015-04-28 2023-02-28 江苏豪森药业集团有限公司 胆酸衍生物及其制备方法和医药用途
WO2016173524A1 (zh) 2015-04-29 2016-11-03 正大天晴药业集团股份有限公司 鹅去氧胆酸衍生物
CN106210599B (zh) 2015-04-30 2021-02-12 中兴通讯股份有限公司 一种多画面调整方法、装置及多点控制单元
KR20180043247A (ko) 2015-06-19 2018-04-27 인터셉트 파마슈티컬즈, 인크. Tgr5 조절제 및 이를 사용하는 방법
BR112018001869A2 (pt) 2015-07-30 2018-09-18 Intercept Pharmaceuticals Inc método para preparação de ácidos biliares e derivados dos mesmos
EP3331896A4 (en) 2015-08-07 2019-08-14 Intercept Pharmaceuticals, Inc. PROCESS FOR THE PRODUCTION OF GALLENIC ACID AND DERIVATIVES THEREOF
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
EP3352768B1 (en) 2015-09-21 2022-11-02 Intercept Pharmaceuticals, Inc. Methods of promoting hepatic regeneration
KR20180052756A (ko) 2015-09-24 2018-05-18 인터셉트 파마슈티컬즈, 인크. 담즙산 유도체 제조를 위한 방법 및 중간체
BR112018006892B1 (pt) 2015-10-07 2023-04-11 Intercept Pharmaceuticals, Inc Composto, composição farmacêutica do mesmo e seus usos como moduladores do receptor farnesoide x
AU2016350690C1 (en) 2015-11-06 2020-04-23 Intercept Pharmaceuticals, Inc. Methods for the preparation of obeticholic acid and derivatives thereof
CA3009149A1 (en) 2015-12-22 2017-06-29 Intercept Pharmaceuticals, Inc. Polymorphic crystalline forms of obeticholic acid
CN105646634A (zh) 2016-01-29 2016-06-08 中国药科大学 奥贝胆酸杂质的制备方法
US10364267B2 (en) 2016-02-23 2019-07-30 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
US10323061B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Heteroaryl containing bile acid analogs as FXR/TGR5 agonists and methods of use thereof
US10323060B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof
PL3426348T3 (pl) 2016-03-11 2022-01-03 Intercept Pharmaceuticals, Inc. Pochodna 3-dezoksylowa i jej kompozycje farmaceutyczne
GB201608776D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
GB201608779D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds

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Publication number Publication date
CN112771063A (zh) 2021-05-07
WO2020025942A1 (en) 2020-02-06
EP3830103B1 (en) 2023-11-08
EP3830103A1 (en) 2021-06-09
US11517577B2 (en) 2022-12-06
EP3830103B8 (en) 2023-12-20
GB201812382D0 (en) 2018-09-12
JP2021533206A (ja) 2021-12-02
EP3830103C0 (en) 2023-11-08
CN112771063B (zh) 2023-10-27
US20210299148A1 (en) 2021-09-30
ES2968881T3 (es) 2024-05-14

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