TW201700447A - Tgr5調控劑及其用法 - Google Patents

Tgr5調控劑及其用法 Download PDF

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Publication number
TW201700447A
TW201700447A TW105118959A TW105118959A TW201700447A TW 201700447 A TW201700447 A TW 201700447A TW 105118959 A TW105118959 A TW 105118959A TW 105118959 A TW105118959 A TW 105118959A TW 201700447 A TW201700447 A TW 201700447A
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Taiwan
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mmol
compound
reduced pressure
under reduced
solution
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TW105118959A
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Chinese (zh)
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羅伯托 佩里恰裡
安蒂莫 吉奧埃洛
安東尼奧 邁克其魯洛
弗朗索瓦絲 皮洛恩西拉
克勞斯 塞多夫
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英特賽普醫藥品公司
法國施維雅藥廠
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Publication of TW201700447A publication Critical patent/TW201700447A/zh

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    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0016—Oximes
    • 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
    • C07J41/0094—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
TW105118959A 2015-06-19 2016-06-16 Tgr5調控劑及其用法 TW201700447A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562182081P 2015-06-19 2015-06-19
EP15305976 2015-06-24

Publications (1)

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TW201700447A true TW201700447A (zh) 2017-01-01

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TW105118959A TW201700447A (zh) 2015-06-19 2016-06-16 Tgr5調控劑及其用法

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EP (1) EP3310801B1 (enExample)
JP (1) JP6861703B2 (enExample)
KR (1) KR20180043247A (enExample)
CN (1) CN107771180B (enExample)
AU (1) AU2016280806B2 (enExample)
CA (1) CA2989167A1 (enExample)
IL (1) IL256085B (enExample)
MX (1) MX380972B (enExample)
PL (1) PL3310801T3 (enExample)
PT (1) PT3310801T (enExample)
SI (1) SI3310801T1 (enExample)
TW (1) TW201700447A (enExample)
UY (1) UY36738A (enExample)
WO (1) WO2016205475A2 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020041673A1 (en) * 2018-08-23 2020-02-27 President And Fellows Of Harvard College Compositions and methods related to cholic acid-7-sulfate as a treatment for diabetes
WO2020117945A1 (en) * 2018-12-04 2020-06-11 President And Fellows Of Harvard College Synthetic derivatives of cholic acid 7-sulfate and uses thereof

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MX381239B (es) 2014-11-19 2025-03-12 Nzp Uk Ltd Esteroides de 6.alfa.-alquil-6,7-diona como intermedios para la producción de moduladores esteroideos del receptor x farnesoide (fxr).
EA034739B1 (ru) 2014-11-19 2020-03-16 ЭнЗедПи ЮКей ЛИМИТЕД 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
JP6724004B2 (ja) 2014-11-19 2020-07-15 エヌゼットピー ユーケー リミテッド ステロイドＦＸＲモジュレーター製造のための中間体としての５β−６−アルキル−７−ヒドロキシ−３−オンステロイド
EA033427B1 (ru) 2014-11-19 2019-10-31 Nzp Uk Ltd 6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
KR20170099909A (ko) 2014-11-26 2017-09-01 이난타 파마슈티칼스, 인코포레이티드 Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법
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
HK1245100A1 (zh) 2015-02-11 2018-08-24 Enanta Pharmaceuticals, Inc. 作为fxr/tgr5激动剂的胆汁酸类似物及其使用方法
NZ735126A (en) 2015-03-31 2022-10-28 Enanta Pharm Inc Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
EP3290429A1 (en) * 2015-04-28 2018-03-07 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Cholic acid derivative, and preparation method and medical use thereof
US10800807B2 (en) 2015-06-19 2020-10-13 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
US20170196893A1 (en) * 2016-01-07 2017-07-13 The Board Of Trustees Of The Leland Stanford Junior University Treatment of inflammatory demyelinating disease with agonists of farnesoid x receptor
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
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
AU2017368069B2 (en) 2016-11-29 2021-07-08 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonylurea bile acid derivatives
WO2018152171A1 (en) 2017-02-14 2018-08-23 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr agonists and methods of use thereof
JP7136802B2 (ja) 2017-04-07 2022-09-13 エナンタ ファーマシューティカルズ インコーポレイテッド スルホニルカルバマート胆汁酸誘導体の調製のためのプロセス
CN109134572A (zh) * 2017-06-19 2019-01-04 中国科学院上海药物研究所 胆酸衍生物及其制备方法和用途
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
WO2021046678A1 (zh) * 2019-09-09 2021-03-18 邦泰生物工程(深圳)有限公司 一种合成鹅去氧胆酸的方法及其应用
JP2022552655A (ja) 2019-10-07 2022-12-19 キャリーオペ，インク． Ｇｐｒ１１９アゴニスト
TW202140440A (zh) 2020-02-28 2021-11-01 美商克力歐普股份有限公司 Gpr40激動劑
CN112341512A (zh) * 2020-04-13 2021-02-09 苏州恩泰新材料科技有限公司 由海豹胆酸制备鹅去氧胆酸的方法
CN112300237A (zh) * 2020-04-13 2021-02-02 苏州恩泰新材料科技有限公司 海豹胆酸的制备方法及其应用
AU2021275038A1 (en) 2020-05-19 2022-12-22 Kallyope, Inc. AMPK activators
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
CN114276402B (zh) * 2022-01-05 2023-11-14 厦门大学 一种甾体衍生物及其在制备抗肿瘤药物中的应用
CN120271652B (zh) * 2025-05-27 2025-10-03 华南理工大学 噁二唑-甾体化合物、药物组合物和用途

Family Cites Families (9)

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Publication number Priority date Publication date Assignee Title
CN101679476B (zh) * 2007-01-19 2014-05-07 英特塞普特医药品公司 23取代的胆汁酸作为tgr5调节剂及其使用方法
EP1947108A1 (en) * 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CN104370990A (zh) * 2008-11-19 2015-02-25 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
CN106661364A (zh) * 2014-06-25 2017-05-10 3M创新有限公司 包含三嗪基团的共聚物以及包含它们的组合物
US10208081B2 (en) * 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
KR20170099909A (ko) * 2014-11-26 2017-09-01 이난타 파마슈티칼스, 인코포레이티드 Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법
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
EP3290429A1 (en) * 2015-04-28 2018-03-07 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Cholic acid derivative, and preparation method and medical use thereof
CN107531743B (zh) * 2015-04-29 2020-05-05 正大天晴药业集团股份有限公司 鹅去氧胆酸衍生物

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020041673A1 (en) * 2018-08-23 2020-02-27 President And Fellows Of Harvard College Compositions and methods related to cholic acid-7-sulfate as a treatment for diabetes
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
WO2020117945A1 (en) * 2018-12-04 2020-06-11 President And Fellows Of Harvard College Synthetic derivatives of cholic acid 7-sulfate and uses thereof
US12419897B2 (en) 2018-12-04 2025-09-23 President And Fellows Of Harvard College Synthetic derivatives of cholic acid 7-sulfate and uses thereof

Also Published As

Publication number Publication date
AU2016280806B2 (en) 2021-01-28
UY36738A (es) 2017-01-31
MX2017016611A (es) 2018-05-15
IL256085B (en) 2021-02-28
EP3310801A2 (en) 2018-04-25
MX380972B (es) 2025-03-12
KR20180043247A (ko) 2018-04-27
PL3310801T3 (pl) 2021-11-22
AU2016280806A1 (en) 2018-01-04
CN107771180B (zh) 2021-03-23
CN107771180A (zh) 2018-03-06
PT3310801T (pt) 2021-06-18
JP6861703B2 (ja) 2021-04-21
JP2018518537A (ja) 2018-07-12
EP3310801B1 (en) 2021-04-07
WO2016205475A2 (en) 2016-12-22
WO2016205475A3 (en) 2017-02-23
SI3310801T1 (sl) 2021-10-29
CA2989167A1 (en) 2016-12-22
IL256085A (en) 2018-02-28

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