TWI772289B - 3-去氧基衍生物及其醫藥組成物與用途 - Google Patents

3-去氧基衍生物及其醫藥組成物與用途 Download PDF

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TWI772289B
TWI772289B TW106107817A TW106107817A TWI772289B TW I772289 B TWI772289 B TW I772289B TW 106107817 A TW106107817 A TW 106107817A TW 106107817 A TW106107817 A TW 106107817A TW I772289 B TWI772289 B TW I772289B
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disease
compound
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amino acid
present
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TW201734031A (zh
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羅伯托 佩里恰裡
安蒂莫 吉奧埃洛
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美商英特賽普醫藥品公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J11/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Cephalosporin Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW106107817A 2016-03-11 2017-03-09 3-去氧基衍生物及其醫藥組成物與用途 TWI772289B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662306914P 2016-03-11 2016-03-11
US62/306,914 2016-03-11

Publications (2)

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TW201734031A TW201734031A (zh) 2017-10-01
TWI772289B true TWI772289B (zh) 2022-08-01

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US (3) US10815267B2 (enExample)
EP (1) EP3426348B1 (enExample)
JP (1) JP6892457B2 (enExample)
KR (1) KR102359191B1 (enExample)
CN (1) CN108883305B (enExample)
AR (1) AR107864A1 (enExample)
AU (1) AU2017229481B2 (enExample)
BR (1) BR112018068278B1 (enExample)
CA (1) CA3016875C (enExample)
EA (1) EA038632B1 (enExample)
ES (1) ES2874682T3 (enExample)
IL (1) IL261548B (enExample)
MX (1) MX384800B (enExample)
PH (1) PH12018501956A1 (enExample)
PL (1) PL3426348T3 (enExample)
PT (1) PT3426348T (enExample)
SG (1) SG11201807784SA (enExample)
SI (1) SI3426348T1 (enExample)
TW (1) TWI772289B (enExample)
WO (1) WO2017156024A1 (enExample)

Families Citing this family (19)

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CA2966885A1 (en) 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Bile acid analogs an 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
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
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
TW201718621A (zh) 2015-10-07 2017-06-01 英特賽普醫藥品公司 法尼醇x受體調節劑
WO2017147159A1 (en) 2016-02-23 2017-08-31 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
US10815267B2 (en) 2016-03-11 2020-10-27 Intercept Pharmaceuticals, Inc. 3-desoxy derivative and pharmaceutical compositions thereof
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
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
KR20230130715A (ko) * 2021-01-14 2023-09-12 엔요 파마 만성 신장 질환의 치료 방법
WO2023288123A1 (en) 2021-07-16 2023-01-19 Interecept Pharmaceuticals, Inc. Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid
WO2023205447A2 (en) * 2022-04-21 2023-10-26 Intercept Pharmaceuticals, Inc. Uses of farnesoid x receptor agonists
EP4611888A1 (en) * 2022-10-31 2025-09-10 Intercept Pharmaceuticals, Inc. Uses of farnesoid x receptor agonists

Citations (2)

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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
CN105377870A (zh) * 2013-05-14 2016-03-02 英特塞普特医药品公司 作为法尼醇x受体调节剂的胆汁酸的11-羟基衍生物及其氨基酸共轭物

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ES2533993T3 (es) * 2004-03-12 2015-04-16 Intercept Pharmaceuticals, Inc. Tratamiento de fibrosis usando ligandos de FXR
US20130261317A1 (en) * 2010-09-27 2013-10-03 Kythera Biopharmaceuticals, Inc. Methods for preparing synthetic bile acids and compositions comprising the same
CN104011064A (zh) 2011-12-29 2014-08-27 诺沃—诺迪斯克有限公司 包含非成蛋白质性的氨基酸的二肽
HK1252688A1 (zh) * 2015-08-07 2019-05-31 英特塞普特医药品公司 制备胆汁酸及其衍生物的方法
US10815267B2 (en) 2016-03-11 2020-10-27 Intercept Pharmaceuticals, Inc. 3-desoxy derivative and pharmaceutical compositions thereof

Patent Citations (2)

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CN105377870A (zh) * 2013-05-14 2016-03-02 英特塞普特医药品公司 作为法尼醇x受体调节剂的胆汁酸的11-羟基衍生物及其氨基酸共轭物
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

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CA3016875C (en) 2023-08-22
US20190002493A1 (en) 2019-01-03
US10815267B2 (en) 2020-10-27
EP3426348A4 (en) 2019-11-20
EA201892007A1 (ru) 2019-01-31
JP2019507781A (ja) 2019-03-22
HK1259145A1 (zh) 2019-11-29
US20170260225A1 (en) 2017-09-14
PT3426348T (pt) 2021-06-28
AU2017229481B2 (en) 2022-06-16
MX2018010983A (es) 2019-01-21
CN108883305A (zh) 2018-11-23
BR112018068278B1 (pt) 2023-12-19
PL3426348T3 (pl) 2022-01-03
AR107864A1 (es) 2018-06-13
WO2017156024A1 (en) 2017-09-14
SG11201807784SA (en) 2018-10-30
SI3426348T1 (sl) 2021-11-30
KR20180117702A (ko) 2018-10-29
EP3426348A1 (en) 2019-01-16
ES2874682T3 (es) 2021-11-05
AU2017229481A1 (en) 2018-09-20
TW201734031A (zh) 2017-10-01
US20210101927A1 (en) 2021-04-08
JP6892457B2 (ja) 2021-06-23
KR102359191B1 (ko) 2022-02-04
EP3426348B1 (en) 2021-05-05
BR112018068278A2 (pt) 2019-04-02
CA3016875A1 (en) 2017-09-14
NZ745980A (en) 2025-03-28
US11319337B2 (en) 2022-05-03
PH12018501956A1 (en) 2019-06-17
IL261548A (en) 2018-11-29
EA038632B1 (ru) 2021-09-27
IL261548B (en) 2021-02-28
CN108883305B (zh) 2021-03-16
MX384800B (es) 2025-03-14

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