PL3310801T3 - Modulatory tgr5 i sposoby ich stosowania - Google Patents

Modulatory tgr5 i sposoby ich stosowania

Info

Publication number
PL3310801T3
PL3310801T3 PL16762910T PL16762910T PL3310801T3 PL 3310801 T3 PL3310801 T3 PL 3310801T3 PL 16762910 T PL16762910 T PL 16762910T PL 16762910 T PL16762910 T PL 16762910T PL 3310801 T3 PL3310801 T3 PL 3310801T3
Authority
PL
Poland
Prior art keywords
methods
tgr5 modulators
tgr5
modulators
Prior art date
Application number
PL16762910T
Other languages
English (en)
Inventor
Roberto Pellicciari
Antimo GIOIELLO
Antonio Macchiarulo
Françoise PERRON-SIERRA
Klaus Seedorf
Original Assignee
Intercept Pharmaceuticals, Inc.
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
Application filed by Intercept Pharmaceuticals, Inc. filed Critical Intercept Pharmaceuticals, Inc.
Publication of PL3310801T3 publication Critical patent/PL3310801T3/pl

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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
PL16762910T 2015-06-19 2016-06-16 Modulatory tgr5 i sposoby ich stosowania PL3310801T3 (pl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562182081P 2015-06-19 2015-06-19
EP15305976 2015-06-24
EP16762910.4A EP3310801B1 (en) 2015-06-19 2016-06-16 Tgr5 modulators and methods of use thereof
PCT/US2016/037812 WO2016205475A2 (en) 2015-06-19 2016-06-16 Tgr5 modulators and methods of use thereof

Publications (1)

Publication Number Publication Date
PL3310801T3 true PL3310801T3 (pl) 2021-11-22

Family

ID=53489911

Family Applications (1)

Application Number Title Priority Date Filing Date
PL16762910T PL3310801T3 (pl) 2015-06-19 2016-06-16 Modulatory tgr5 i sposoby ich stosowania

Country Status (14)

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

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* Cited by examiner, † Cited by third party
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ES2748692T3 (es) 2014-11-19 2020-03-17 Nzp Uk Ltd Esteroides 6.alfa.-alquil-3,7-diona como intermedios para la producción de moduladores FXR de esteroides
KR102526632B1 (ko) 2014-11-19 2023-04-27 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 5β-6-알킬-7-하이드록시-3-온 스테로이드
JP6698085B2 (ja) 2014-11-19 2020-05-27 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6α−アルキル−6,7−ジオン−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
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
RU2017121457A (ru) 2014-11-26 2018-12-26 Энанта Фармасьютикалс, Инк. Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения
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
AU2016219266A1 (en) 2015-02-11 2017-08-10 Enanta Pharmaceuticals, Inc. Bile acid analogs as FXR/TGR5 agonists and methods of use thereof
RU2712099C2 (ru) 2015-03-31 2020-01-24 Энанта Фармасьютикалс, Инк. Производные желчных кислот в качестве агонистов fxr/tgr5 и способы их применения
WO2016173397A1 (zh) * 2015-04-28 2016-11-03 上海翰森生物医药科技有限公司 胆酸衍生物及其制备方法和医药用途
DK3310801T3 (da) 2015-06-19 2021-06-21 Intercept Pharmaceuticals Inc Tgr5-modulatorer og fremgangsmåder til anvendelse deraf
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
WO2017147174A1 (en) 2016-02-23 2017-08-31 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
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof
MX388300B (es) 2017-04-07 2025-03-19 Enanta Pharm Inc Proceso para la preparación de derivados de ácidos biliares de sulfonil carbamato
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
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
CN120757601A (zh) 2019-05-10 2025-10-10 哈佛大学的校长及成员们 肠道细菌胆汁酸代谢的小分子调节剂
CN112334476B (zh) * 2019-09-09 2022-03-15 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
MX2022010548A (es) 2020-02-28 2022-09-23 Kallyope Inc Agonistas de gpr40.
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
MX2022014505A (es) 2020-05-19 2022-12-13 Kallyope Inc Activadores de la ampk.
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1947108A1 (en) * 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CA2928178C (en) * 2007-01-19 2019-09-10 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
HUE039171T2 (hu) * 2008-11-19 2018-12-28 Intercept Pharmaceuticals Inc TGR5 modulátorok és azok alkalmazási eljárása
WO2015200669A1 (en) * 2014-06-25 2015-12-30 3M Innovative Properties Company Pressure sensitive adhesive composition including ultraviolet light-absorbing oligomer
RU2017121457A (ru) * 2014-11-26 2018-12-26 Энанта Фармасьютикалс, Инк. Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения
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
US10208081B2 (en) * 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
WO2016173397A1 (zh) * 2015-04-28 2016-11-03 上海翰森生物医药科技有限公司 胆酸衍生物及其制备方法和医药用途
TW201704251A (zh) * 2015-04-29 2017-02-01 正大天晴藥業集團股份有限公司 鵝去氧膽酸衍生物

Also Published As

Publication number Publication date
WO2016205475A3 (en) 2017-02-23
CA2989167A1 (en) 2016-12-22
JP6861703B2 (ja) 2021-04-21
AU2016280806A1 (en) 2018-01-04
EP3310801A2 (en) 2018-04-25
MX380972B (es) 2025-03-12
PT3310801T (pt) 2021-06-18
IL256085A (en) 2018-02-28
EP3310801B1 (en) 2021-04-07
TW201700447A (zh) 2017-01-01
KR20180043247A (ko) 2018-04-27
MX2017016611A (es) 2018-05-15
CN107771180B (zh) 2021-03-23
JP2018518537A (ja) 2018-07-12
IL256085B (en) 2021-02-28
CN107771180A (zh) 2018-03-06
SI3310801T1 (sl) 2021-10-29
UY36738A (es) 2017-01-31
AU2016280806B2 (en) 2021-01-28
WO2016205475A2 (en) 2016-12-22

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