DK3221333T3 - 6-alfa-alkyl-3,7-dionsteroider som mellemprodukter til fremstilling af steroide FXR-modulatorer - Google Patents

6-alfa-alkyl-3,7-dionsteroider som mellemprodukter til fremstilling af steroide FXR-modulatorer Download PDF

Info

Publication number
DK3221333T3
DK3221333T3 DK15800911.8T DK15800911T DK3221333T3 DK 3221333 T3 DK3221333 T3 DK 3221333T3 DK 15800911 T DK15800911 T DK 15800911T DK 3221333 T3 DK3221333 T3 DK 3221333T3
Authority
DK
Denmark
Prior art keywords
intermediates
alpha
alkyl
preparation
fxr modulators
Prior art date
Application number
DK15800911.8T
Other languages
Danish (da)
English (en)
Inventor
Alexander Weymouth-Wilson
Zofia Komsta
James Boydell
Laura Wallis
Rhys Batchelor
Carl Otter
Ieuan Davies
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 GBGB1505676.5A external-priority patent/GB201505676D0/en
Application filed by Nzp Uk Ltd filed Critical Nzp Uk Ltd
Application granted granted Critical
Publication of DK3221333T3 publication Critical patent/DK3221333T3/da

Links

Classifications

    • 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
    • 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
    • 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)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
DK15800911.8T 2014-11-19 2015-11-19 6-alfa-alkyl-3,7-dionsteroider som mellemprodukter til fremstilling af steroide FXR-modulatorer DK3221333T3 (da)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GBGB1420594.2A GB201420594D0 (en) 2014-11-19 2014-11-19 Compounds
GBGB1420593.4A GB201420593D0 (en) 2014-11-19 2014-11-19 Compounds
GBGB1505676.5A GB201505676D0 (en) 2015-04-01 2015-04-01 Compounds
PCT/GB2015/053518 WO2016079519A1 (en) 2014-11-19 2015-11-19 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators

Publications (1)

Publication Number Publication Date
DK3221333T3 true DK3221333T3 (da) 2019-09-30

Family

ID=54704021

Family Applications (1)

Application Number Title Priority Date Filing Date
DK15800911.8T DK3221333T3 (da) 2014-11-19 2015-11-19 6-alfa-alkyl-3,7-dionsteroider som mellemprodukter til fremstilling af steroide FXR-modulatorer

Country Status (13)

Country Link
US (1) US10538550B2 (enExample)
EP (1) EP3221333B1 (enExample)
JP (1) JP6735748B2 (enExample)
KR (1) KR102546748B1 (enExample)
CN (1) CN107108688B (enExample)
CA (1) CA2968305A1 (enExample)
DK (1) DK3221333T3 (enExample)
EA (1) EA034739B1 (enExample)
ES (1) ES2748692T3 (enExample)
MX (1) MX375865B (enExample)
PL (1) PL3221333T3 (enExample)
TW (1) TWI686401B (enExample)
WO (1) WO2016079519A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI686400B (zh) 2014-11-19 2020-03-01 英商Ｎｚｐ英國有限公司 化合物（二）
MX375863B (es) 2014-11-19 2025-03-07 Nzp Uk Ltd Esteroides de 6-alquil-7-hidroxi-4-en-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr)
EA033603B1 (ru) 2014-11-19 2019-11-08 Nzp Uk Ltd 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
EA201891491A1 (ru) * 2015-12-22 2018-11-30 Интерсепт Фармасьютикалз, Инк. Полиморфные кристаллические формы обетихолевой кислоты
GB201608776D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
GB201608779D0 (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
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
US12186329B2 (en) 2018-08-23 2025-01-07 President And Fellows Of Harvard College Compositions and methods related to cholic acid 7-sulfate as a treatment for diabetes
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
EP3890745B1 (en) * 2018-12-04 2025-11-19 President and Fellows of Harvard College Synthetic derivatives of cholic acid 7-sulfate and uses thereof

Family Cites Families (42)

* 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
WO1993021259A1 (en) 1992-04-14 1993-10-28 Cornell Research Foundation Inc. Dendritic based macromolecules and method of production
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
US7138390B2 (en) * 2001-03-12 2006-11-21 Intercept Pharmaceuticals 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
KR100948532B1 (ko) 2001-11-07 2010-03-23 넥타르 테라퓨틱스 분지형 중합체 및 그의 공액체
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
WO2008002573A2 (en) 2006-06-27 2008-01-03 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
EA020310B1 (ru) * 2008-07-30 2014-10-30 Интерсепт Фармасьютикалз, Инк. Модуляторы рецептора tgr5 и их применение
ES2592452T3 (es) * 2008-11-19 2016-11-30 Intercept Pharmaceuticals, Inc. Moduladores de TGR5 y métodos de uso de los mismos
AU2009316566B9 (en) 2008-11-19 2014-05-15 Intercept Pharmaceuticals, Inc. TGR5 modulators and method of use thereof
US8829213B2 (en) 2009-07-29 2014-09-09 The University Of Chicago Liver X receptor agonists
ES2822375T3 (es) * 2012-06-19 2021-04-30 Intercept Pharmaceuticals Inc Preparación de la forma no cristalina del ácido obeticólico
WO2014066819A1 (en) 2012-10-26 2014-05-01 Intercept Pharmaceuticals, Inc. Process for preparing bile acid derivatives
KR102106186B1 (ko) * 2012-11-28 2020-05-04 인터셉트 파마슈티컬즈, 인크. 폐 질환의 치료
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
HRP20180931T1 (hr) 2013-05-14 2018-10-05 Intercept Pharmaceuticals, Inc. 11-hidroksil-6-supstituirani-derivati žučnih kiselina i njihovi aminokiselinski konjugati kao modulatori receptora za farnezoid x
RU2015155552A (ru) 2013-05-24 2017-06-27 Нестек С.А. Путеспецифические способы прогнозирования диагноза синдрома раздраженного кишечника
WO2015183794A1 (en) 2014-05-27 2015-12-03 City Of Hope Tgr5 agonist complexes for treating diabetes and cancer
ES2938874T3 (es) 2014-05-29 2023-04-17 Bar Pharmaceuticals S R L Derivados de colano para su uso en el tratamiento y/o prevención de enfermedades mediadas por FXR y TGR5/GPBAR1
CA2966885A1 (en) 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
MX375863B (es) 2014-11-19 2025-03-07 Nzp Uk Ltd Esteroides de 6-alquil-7-hidroxi-4-en-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr)
EA033603B1 (ru) 2014-11-19 2019-11-08 Nzp Uk Ltd 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
TWI686400B (zh) 2014-11-19 2020-03-01 英商Ｎｚｐ英國有限公司 化合物（二）
WO2016086134A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid derivatives 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
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
HK1244708A1 (zh) 2014-11-26 2018-08-17 英安塔制药有限公司 作爲fxr/tgr5激动剂的胆汁酸类似物及其使用方法
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
PL3310801T3 (pl) 2015-06-19 2021-11-22 Intercept Pharmaceuticals, Inc. Modulatory tgr5 i sposoby ich stosowania
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

Also Published As

Publication number Publication date
EP3221333A1 (en) 2017-09-27
TWI686401B (zh) 2020-03-01
TW201632538A (zh) 2016-09-16
KR102546748B1 (ko) 2023-06-22
KR20170104453A (ko) 2017-09-15
US20180340006A1 (en) 2018-11-29
HK1244287A1 (en) 2018-08-03
WO2016079519A1 (en) 2016-05-26
JP6735748B2 (ja) 2020-08-05
MX2017006565A (es) 2018-01-26
MX375865B (es) 2025-03-07
CA2968305A1 (en) 2016-05-26
US10538550B2 (en) 2020-01-21
EA201790879A1 (ru) 2017-11-30
EA034739B1 (ru) 2020-03-16
CN107108688B (zh) 2019-10-29
JP2017538690A (ja) 2017-12-28
CN107108688A (zh) 2017-08-29
ES2748692T3 (es) 2020-03-17
WO2016079519A9 (en) 2018-08-09
PL3221333T3 (pl) 2020-01-31
EP3221333B1 (en) 2019-07-24

Similar Documents

Publication Publication Date Title
DK3221333T3 (da) 6-alfa-alkyl-3,7-dionsteroider som mellemprodukter til fremstilling af steroide FXR-modulatorer
DK3221331T3 (da) 6-alkyl-7-hydroxy-4-en-3-on-steroider som mellemprodukter til fremstilling af steroide fxr-modulatorer
DK3096741T3 (da) Fremgangsmåde til fremstillingen af hybridosomer
DK3122403T3 (da) Mekanisme til aftrækning af hylster
PL3074011T3 (pl) Połączone fuzyjnie oktahydro związki azadekaliny jako modulatory receptora glukokortykoidowego
BR112017004535A2 (pt) esteroides neuroativos, composições e utilizações deste
DK3192902T3 (da) Fremgangsmåde til fremstilling af graphenholdige viscosefibre
DK3174858T3 (da) Fremgangsmåde til fremstilling af pyrazoler
DK3757214T3 (da) Sammensætninger til modulering af sod-1-ekspression
DK3178817T3 (da) Amorf form af tetracyklisk forbindelse
DK3338781T3 (da) Heteroaryl-keton-kondenseret azadecalin som modulatorer af glucocorticoidreceptorer
DK3372584T3 (da) Fremgangsmåde til fremstillingen af en diarylthiohydantoin-forbindelse
DK3998070T3 (da) Mir-124 som biomarkør til behandling af inflammatoriske sygdomme
DK3294720T3 (da) Fremgangsmåde til fremstilling af terpinolenepoxid
EP3175497A4 (en) Photolithographic patterning of devices
EP3175495A4 (en) Photolithographic patterning of devices
DK3221332T3 (da) Fremstilling af steroide fxr-modulatorer
EP3145893A4 (en) Combined set-delayed cement compositions
IL252724B (en) Modular architecture optimized for making microsatellites
DK3536324T3 (da) 4-oxo-3,4-dihydro-1,2,3-benzotriaziner som modulatorer af gpr139
DK3233813T3 (da) Fremgangsmåder til fremstilling af oxathiazin-lignende forbindelser
DK3010895T3 (da) Fremgangsmåde til fremstilling af 4-propargyleret aminobenzoxazinoner
DK3134410T3 (da) Hæmning af ionkanalen af overgangsreceptorpotentialet A1
BR112016026046A2 (pt) Uso de compostos de tienotriazolodiazepina
DK3183237T3 (da) Fremgangsmåde til fremstilling af 5-fluor-1h-pyrazoler startende ud fra hexafluorpropen