CN107207558B - 作为制备类固醇FXR调节剂的中间体的6α-烷基-6,7-二酮类固醇 - Google Patents

作为制备类固醇FXR调节剂的中间体的6α-烷基-6,7-二酮类固醇 Download PDF

Info

Publication number
CN107207558B
CN107207558B CN201580062901.6A CN201580062901A CN107207558B CN 107207558 B CN107207558 B CN 107207558B CN 201580062901 A CN201580062901 A CN 201580062901A CN 107207558 B CN107207558 B CN 107207558B
Authority
CN
China
Prior art keywords
alkyl
compound
general formula
compounds
logical formula
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201580062901.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN107207558A (zh
Inventor
A·韦茅斯-威尔逊
Z·科姆斯塔
J·博伊德尔
L·沃利斯
C·奥特
I·戴维斯
R·克拉克森
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nzp Uk Ltd
Original Assignee
Nzp Uk Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB1420594.2A external-priority patent/GB201420594D0/en
Priority claimed from GBGB1420593.4A external-priority patent/GB201420593D0/en
Priority claimed from GBGB1505675.7A external-priority patent/GB201505675D0/en
Application filed by Nzp Uk Ltd filed Critical Nzp Uk Ltd
Publication of CN107207558A publication Critical patent/CN107207558A/zh
Application granted granted Critical
Publication of CN107207558B publication Critical patent/CN107207558B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201580062901.6A 2014-11-19 2015-11-19 作为制备类固醇FXR调节剂的中间体的6α-烷基-6,7-二酮类固醇 Active CN107207558B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GBGB1420594.2A GB201420594D0 (en) 2014-11-19 2014-11-19 Compounds
GB1420594.2 2014-11-19
GBGB1420593.4A GB201420593D0 (en) 2014-11-19 2014-11-19 Compounds
GB1420593.4 2014-11-19
GB1505675.7 2015-04-01
GBGB1505675.7A GB201505675D0 (en) 2015-04-01 2015-04-01 Compounds
PCT/GB2015/053519 WO2016079520A1 (en) 2014-11-19 2015-11-19 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators

Publications (2)

Publication Number Publication Date
CN107207558A CN107207558A (zh) 2017-09-26
CN107207558B true CN107207558B (zh) 2019-10-29

Family

ID=54704022

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580062901.6A Active CN107207558B (zh) 2014-11-19 2015-11-19 作为制备类固醇FXR调节剂的中间体的6α-烷基-6,7-二酮类固醇

Country Status (10)

Country Link
US (2) US20170327531A1 (enExample)
EP (1) EP3221334B1 (enExample)
JP (1) JP6698085B2 (enExample)
KR (1) KR102527821B1 (enExample)
CN (1) CN107207558B (enExample)
CA (1) CA2968310A1 (enExample)
EA (1) EA033603B1 (enExample)
MX (1) MX381239B (enExample)
TW (1) TWI688571B (enExample)
WO (1) WO2016079520A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI688571B (zh) 2014-11-19 2020-03-21 英商Ｎｚｐ英國有限公司 化合物（四）
PL3221331T3 (pl) 2014-11-19 2020-03-31 NZP UK Limited Steroidy, 6-alkilo-7-hydroksy-4-en-3-ony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr
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
CN107108688B (zh) 2014-11-19 2019-10-29 Nzp英国有限公司 作为制备类固醇FXR调节剂的中间体的6α-烷基-3,7-二酮类固醇
CA3009149A1 (en) * 2015-12-22 2017-06-29 Intercept Pharmaceuticals, Inc. Polymorphic crystalline forms of obeticholic acid
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
CN106046093A (zh) * 2016-05-30 2016-10-26 华东师范大学 一种石胆酸的合成方法
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
CN111285914B (zh) * 2018-12-10 2023-02-17 江西青峰药业有限公司 一种奥贝胆酸的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010059859A1 (en) * 2008-11-19 2010-05-27 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
CN102164940A (zh) * 2008-07-30 2011-08-24 英特塞普特医药品公司 Tgr5调节剂及其使用方法
US20140148428A1 (en) * 2012-11-28 2014-05-29 Intercept Pharmaceuticals, Inc. Treatment of Pulmonary Disease
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO1994019366A1 (en) 1993-02-26 1994-09-01 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
AU2002308295B2 (en) 2001-03-12 2007-08-23 Intercept Pharmaceuticals, Inc. 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
JP4758608B2 (ja) 2001-11-07 2011-08-31 ネクター セラピューティックス 分枝ポリマーおよびそれらの結合体
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
JP2007210888A (ja) * 2006-01-12 2007-08-23 Mitsubishi Chemicals Corp ステロイド化合物の製造方法
CN101395170A (zh) 2006-02-14 2009-03-25 英特塞普特药品公司 用于预防或治疗fxr介导的疾病或状态的作为fxr配体的胆汁酸衍生物
EP2040713B1 (en) 2006-06-27 2014-06-18 Intercept Pharmaceuticals Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated deseases or conditions
CA2928178C (en) 2007-01-19 2019-09-10 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
NO2698375T3 (enExample) 2008-11-19 2018-07-21
US8829213B2 (en) 2009-07-29 2014-09-09 The University Of Chicago Liver X receptor agonists
CA2877122C (en) 2012-06-19 2020-04-28 Intercept Pharmaceuticals, Inc. Preparation, uses and solid forms of obeticholic acid
KR102068381B1 (ko) 2012-10-26 2020-01-20 인터셉트 파마슈티컬즈, 인크. 담즙산 유도체의 제조 방법
EP2997035B8 (en) 2013-05-14 2018-05-23 Intercept Pharmaceuticals, Inc. 11-hydroxyl-6-substituted-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators
BR112015029318A2 (pt) 2013-05-24 2017-07-25 Nestec Sa marcadores específicos de caminhos para diagnóstico da síndrome do intestino irritável
WO2015183794A1 (en) * 2014-05-27 2015-12-03 City Of Hope Tgr5 agonist complexes for treating diabetes and cancer
EP3149019B1 (en) 2014-05-29 2019-12-04 Bar Pharmaceuticals S.r.l. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
HK1243930A1 (zh) 2014-11-06 2018-07-27 英安塔制药有限公司 作爲fxr/tgr5激动剂的胆汁酸类似物和其使用方法
CN107108688B (zh) 2014-11-19 2019-10-29 Nzp英国有限公司 作为制备类固醇FXR调节剂的中间体的6α-烷基-3,7-二酮类固醇
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
PL3221331T3 (pl) 2014-11-19 2020-03-31 NZP UK Limited Steroidy, 6-alkilo-7-hydroksy-4-en-3-ony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr
TWI688571B (zh) 2014-11-19 2020-03-21 英商Ｎｚｐ英國有限公司 化合物（四）
MX2017006833A (es) 2014-11-26 2018-02-13 Enanta Pharm Inc Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos.
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
WO2016086134A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
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
TW201700447A (zh) 2015-06-19 2017-01-01 英特賽普醫藥品公司 Tgr5調控劑及其用法
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
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102164940A (zh) * 2008-07-30 2011-08-24 英特塞普特医药品公司 Tgr5调节剂及其使用方法
WO2010059859A1 (en) * 2008-11-19 2010-05-27 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
US20140148428A1 (en) * 2012-11-28 2014-05-29 Intercept Pharmaceuticals, Inc. Treatment of Pulmonary Disease
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists

Also Published As

Publication number Publication date
US10597423B2 (en) 2020-03-24
US20170327531A1 (en) 2017-11-16
HK1244286A1 (en) 2018-08-03
WO2016079520A1 (en) 2016-05-26
TWI688571B (zh) 2020-03-21
EP3221334B1 (en) 2020-02-19
MX381239B (es) 2025-03-12
EA033603B1 (ru) 2019-11-08
JP2017534669A (ja) 2017-11-24
JP6698085B2 (ja) 2020-05-27
KR102527821B1 (ko) 2023-05-02
CA2968310A1 (en) 2016-05-26
CN107207558A (zh) 2017-09-26
US20190077827A1 (en) 2019-03-14
KR20170099896A (ko) 2017-09-01
MX2017006567A (es) 2018-01-26
EA201790885A1 (ru) 2017-11-30
TW201632539A (zh) 2016-09-16
EP3221334A1 (en) 2017-09-27

Similar Documents

Publication Publication Date Title
CN107207558B (zh) 作为制备类固醇FXR调节剂的中间体的6α-烷基-6,7-二酮类固醇
CN107207559B (zh) 作为制备类固醇fxr调节剂的中间体的6-烷基-7-羟基-4-烯-3-酮类固醇
CN107108688B (zh) 作为制备类固醇FXR调节剂的中间体的6α-烷基-3,7-二酮类固醇
CN107108687B (zh) 作为制备类固醇FXR调节剂的中间体的5β-6-烷基-7-羟基-3-酮类固醇
HK1244285A1 (en) 5.beta -6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
HK1244286B (en) 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators
HK1244287B (en) 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators
HK1246801B (en) 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
CB02 Change of applicant information
CB02 Change of applicant information

Address after: English: fusuri

Applicant after: NZP UK Ltd

Address before: Hakuhoku County, England

Applicant before: NZP UK Ltd

GR01 Patent grant
GR01 Patent grant