KR102068381B1 - 담즙산 유도체의 제조 방법 - Google Patents

담즙산 유도체의 제조 방법 Download PDF

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Publication number
KR102068381B1
KR102068381B1 KR1020157012805A KR20157012805A KR102068381B1 KR 102068381 B1 KR102068381 B1 KR 102068381B1 KR 1020157012805 A KR1020157012805 A KR 1020157012805A KR 20157012805 A KR20157012805 A KR 20157012805A KR 102068381 B1 KR102068381 B1 KR 102068381B1
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formula
compound
idd
pharmaceutically acceptable
ibb
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KR20150074062A (ko
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로베르토 펠리치아리
안티모 지오이엘로
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인터셉트 파마슈티컬즈, 인크.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C305/00—Esters of sulfuric acids
    • C07C305/02—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C305/12—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to acyclic carbon atoms of a carbon skeleton being saturated and containing rings
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B45/00—Formation or introduction of functional groups containing sulfur
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020157012805A 2012-10-26 2013-10-25 담즙산 유도체의 제조 방법 Expired - Fee Related KR102068381B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261718966P 2012-10-26 2012-10-26
US61/718,966 2012-10-26
PCT/US2013/066917 WO2014066819A1 (en) 2012-10-26 2013-10-25 Process for preparing bile acid derivatives

Publications (2)

Publication Number Publication Date
KR20150074062A KR20150074062A (ko) 2015-07-01
KR102068381B1 true KR102068381B1 (ko) 2020-01-20

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KR1020157012805A Expired - Fee Related KR102068381B1 (ko) 2012-10-26 2013-10-25 담즙산 유도체의 제조 방법

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US (2) US9777038B2 (enExample)
EP (1) EP2912013B1 (enExample)
JP (1) JP6272888B2 (enExample)
KR (1) KR102068381B1 (enExample)
CN (2) CN105102425B (enExample)
AU (1) AU2013334122B2 (enExample)
BR (1) BR112015009395A2 (enExample)
CA (1) CA2889592A1 (enExample)
CY (1) CY1119731T1 (enExample)
DK (1) DK2912013T3 (enExample)
ES (1) ES2655034T3 (enExample)
HK (1) HK1253301A1 (enExample)
HU (1) HUE036887T2 (enExample)
IL (1) IL238454B (enExample)
MX (1) MX361653B (enExample)
NO (1) NO2968302T3 (enExample)
NZ (2) NZ707389A (enExample)
PL (1) PL2912013T3 (enExample)
PT (1) PT2912013T (enExample)
SG (1) SG11201503247UA (enExample)
SM (1) SMT201700602T1 (enExample)
WO (1) WO2014066819A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022059948A1 (ko) 2020-09-18 2022-03-24 서울대학교 산학협력단 소디움 타우로디옥시콜레이트의 대량 생산 방법

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112015009395A2 (pt) 2012-10-26 2017-07-04 Intercept Pharmaceuticals Inc processo para preparação de derivados do ácido biliar
WO2015181275A1 (en) * 2014-05-29 2015-12-03 Bar Pharmaceuticals S.R.L. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
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
MX375864B (es) 2014-11-19 2025-03-07 Nzp Uk Ltd Esteroides de 5.beta-6-alquil-7-hidroxi-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr)
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
KR102526631B1 (ko) 2014-11-19 2023-04-27 엔제트피 유케이 리미티드 스테로이드 fxr 조절인자를 제조하기 위한 중간체로서의 6-알킬-7-하이드록시-4-엔-3-온 스테로이드
CN104672290B (zh) * 2015-01-05 2017-06-06 北京普禄德医药科技有限公司 一种用于预防或治疗fxr‑介导的疾病的药物及其制备方法和用途
AR103624A1 (es) 2015-02-06 2017-05-24 Intercept Pharmaceuticals Inc Composiciones farmacéuticas para terapia de combinación
HK1254057A1 (zh) * 2015-09-24 2019-07-12 英特塞普特医药品公司 用於制备胆汁酸衍生物的方法和中间体
EP3370728A4 (en) * 2015-11-06 2019-07-10 Intercept Pharmaceuticals, Inc. PROCESS FOR THE PREPARATION OF OBETICHOLIC ACID AND DERIVATIVES THEREOF
US20200262865A1 (en) * 2016-02-15 2020-08-20 Alexander Khoruts Compositions and methods for treating clostridium associated diseases
CN109071452A (zh) 2016-04-13 2018-12-21 英特塞普特医药品公司 治疗癌症的方法
TW201738254A (zh) * 2016-04-19 2017-11-01 英特賽普醫藥品公司 奧貝膽酸及其衍生物之製備方法
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
KR20190057108A (ko) * 2016-09-30 2019-05-27 인터셉트 파마슈티컬즈, 인크. 담즙산 유도체의 결정형
CA3070837A1 (en) 2017-07-24 2019-01-31 Intercept Pharmaceuticals, Inc. Isotopically labeled bile acid derivatives
CN110869381B (zh) * 2017-07-26 2021-11-19 正大天晴药业集团股份有限公司 甾体类衍生物fxr激动剂的制备方法
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
EA202193334A1 (ru) 2019-05-30 2022-03-14 Интерсепт Фармасьютикалз, Инк. Фармацевтические композиции, содержащие агонист fxr и фибрат, для применения при лечении холестатического заболевания печени
JP2022552655A (ja) 2019-10-07 2022-12-19 キャリーオペ，インク． Ｇｐｒ１１９アゴニスト
PH12022552277A1 (en) 2020-02-28 2024-03-04 Kallyope Inc Gpr40 agonists
JP2023526625A (ja) 2020-05-19 2023-06-22 キャリーオペ，インク． Ａｍｐｋアクチベーター
CN116390925A (zh) 2020-06-26 2023-07-04 卡尔优普公司 Ampk活化剂

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080182832A1 (en) 2006-06-27 2008-07-31 Intercept Pharmaceuticals, Inc. Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
US20110172198A1 (en) 2008-07-30 2011-07-14 Intercept Pharmaceuticals, Inc. TGR5 Modulators And Methods Of Use Thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5216015A (en) 1991-02-05 1993-06-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having hypocholesterolemic properties
EP1392714B1 (en) 2001-03-12 2005-08-31 Intercept Pharmaceuticals, Inc. Steroids as agonists for fxr
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
US9943614B2 (en) 2008-06-17 2018-04-17 Brigham Young University Cationic steroid antimicrobial diagnostic, detection, screening and imaging methods
EP2373673B1 (en) * 2008-11-19 2016-07-27 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
BR112015009395A2 (pt) 2012-10-26 2017-07-04 Intercept Pharmaceuticals Inc processo para preparação de derivados do ácido biliar

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080182832A1 (en) 2006-06-27 2008-07-31 Intercept Pharmaceuticals, Inc. Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
US20110172198A1 (en) 2008-07-30 2011-07-14 Intercept Pharmaceuticals, Inc. TGR5 Modulators And Methods Of Use Thereof

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
J. Med. Chem.(2004), 47, pp.4559~4569
J. Org. Chem. 2001, 66, pp.4814~4818
Molecular Pharmacology, 2010, Vol.78, No.4, pp.617~630

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022059948A1 (ko) 2020-09-18 2022-03-24 서울대학교 산학협력단 소디움 타우로디옥시콜레이트의 대량 생산 방법

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JP2015533852A (ja) 2015-11-26
HK1214239A1 (zh) 2016-07-22
HUE036887T2 (hu) 2018-08-28
DK2912013T3 (en) 2018-01-15
EP2912013A4 (en) 2016-06-01
AU2013334122B2 (en) 2017-11-02
SMT201700602T1 (it) 2018-03-08
BR112015009395A2 (pt) 2017-07-04
MX361653B (es) 2018-12-13
US20150291653A1 (en) 2015-10-15
SG11201503247UA (en) 2015-06-29
US20180079776A1 (en) 2018-03-22
NZ707389A (en) 2018-08-31
CN105102425B (zh) 2018-04-10
PL2912013T3 (pl) 2018-05-30
US10202414B2 (en) 2019-02-12
NZ745013A (en) 2019-08-30
WO2014066819A1 (en) 2014-05-01
CA2889592A1 (en) 2014-05-01
NO2968302T3 (enExample) 2018-02-03
ES2655034T3 (es) 2018-02-16
IL238454A0 (en) 2015-06-30
CN108250264A (zh) 2018-07-06
KR20150074062A (ko) 2015-07-01
IL238454B (en) 2018-11-29
AU2013334122A1 (en) 2015-05-14
HK1253301A1 (zh) 2019-06-14
CY1119731T1 (el) 2018-06-27
US9777038B2 (en) 2017-10-03
MX2015005286A (es) 2015-10-29
PT2912013T (pt) 2018-01-03
EP2912013B1 (en) 2017-10-11
JP6272888B2 (ja) 2018-01-31
CN105102425A (zh) 2015-11-25
EP2912013A1 (en) 2015-09-02

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